Category

Archives

Apoptosis

Proteomic and Phosphoproteomic Profiling Reveals the Oncogenic Role of Protein Kinase D Family Kinases in Cholangiocarcinoma

735 | Feb 15 2024

The comprehensive analysis of protein and phosphorylation signatures in cholangiocarcinoma revealed the PRKD family's pivotal role, highlighting their potential as novel treatment targets validated by the inhibitory effects of 1-naphthyl PP1 on CCA cell proliferation, migration, and invasion. [Read the Full Post]

Treatment of CHO cells with Taxol and reversine improves micronucleation and microcell-mediated chromosome transfer efficiency

155 | Feb 13 2024

The synergistic combination of Taxol and reversine has revolutionized chromosomal transfer protocols, significantly enhancing efficiency across various cell lines and paving the way for accelerated advancements in genetic and regenerative medical research. [Read the Full Post]

Reduced Zn2+ promotes retinal ganglion cells survival and optic nerve regeneration after injury through inhibiting autophagy mediated by ROS/Nrf2

191 | Feb 13 2024

Reduced mobile zinc (Zn2+) promotes retinal ganglion cell (RGC) survival and axonal regeneration post-optic nerve crush (ONC) injury by decreasing reactive oxygen species (ROS), activating Nrf2, and inhibiting autophagy, highlighting a potential therapeutic strategy via Zn2+ reduction using TPEN or conditional knockout of ZnT-3 in amacrine cells (ACs) for treating optic nerve damage. [Read the Full Post]

Natural Guanine Derivatives Exert PARP-Inhibitory and Cytoprotective Effects in a Model of Cardiomyocyte Damage under Oxidative Stress

154 | Feb 13 2024

The compelling findings reveal the potential of guanine derivatives, particularly 7-methylguanine and 8-hydroxy-7-methylguanine, as potent inhibitors of PARP activation, offering promising avenues for therapeutic development in conditions associated with oxidative stress and inflammation. [Read the Full Post]

Enhancing or Quenching of a Mitochondria-Targeted AIEgens-Floxuridine Sensor by the Regulation of pH-Dependent Self-assembly, Efficient Recognition of Hg2+, and Stimulated Response of GSH

391 | Feb 03 2024

The versatile TPE-FdU fluorescent probe, exhibiting pH-responsive behavior, selective Hg2+ ion detection, and intracellular mitochondrial visualization, represents a promising advancement with diverse applications in cell imaging, environmental monitoring, and biomedical research. [Read the Full Post]

The m6A reader IGF2BP2 regulates glutamine metabolism and represents a therapeutic target in acute myeloid leukemia

150 | Jan 30 2024

The study underscores the pivotal role of IGF2BP2 in acute myeloid leukemia, revealing its association with unfavorable prognosis, promotion of leukemia cell development through m6A-dependent regulation of key metabolic targets, and the promising therapeutic potential of the identified small-molecule compound (CWI1-2) in targeting IGF2BP2 for AML treatment. [Read the Full Post]

First-in-Class NADH/Ubiquinone Oxidoreductase Core Subunit S7 (NDUFS7) Antago

248 | Jan 26 2024

Inhibiting oxidative phosphorylation via the NDUFS7 antagonist DX2-201 presents a promising and novel therapeutic strategy for pancreatic cancer, demonstrating efficacy, direct targeting of drug resistance mechanisms, and synergistic potential with metabolic and PARP inhibitors. [Read the Full Post]

Antitumor effect of a small-molecule inhibitor of KRASG12D in xenograft models of mucinous appendicular neoplasms

373 | Jan 25 2024

The profound inhibition of tumor growth in a high-grade PMP xenograft mouse model carrying a KRASG12D mutation by the small-molecule KRASG12D inhibitor MRTX1133 underscores its potent efficacy and supports its potential for clinical translation in treating PMP. [Read the Full Post]

CRISPR screening identifies mechanisms of resistance to KRASG12C and SHP2 inhibitor combinations in non-small cell lung cancer

338 | Jan 23 2024

The study uncovers that while KRASG12C inhibitors initially exhibit promising responses, combining them with SHP2, PI3K, and CDK4/6 inhibitors extends regression in preclinical models, yet resistance emerges via KRASG12C amplification and MAPK/PI3K pathway alterations, with FGFR1 loss sensitizing and PTEN loss rescuing against the KRASG12C/SHP2 inhibition. [Read the Full Post]

Isolinderalactone Induces Apoptosis, Autophagy, Cell Cycle Arrest and MAPK Activation through ROS-Mediated Signaling in Colorectal Cancer Cell Lines

491 | Jan 23 2024

Isolinderalactone demonstrates significant potential as a therapeutic agent for colorectal cancer by inducing G2/M phase arrest, apoptosis, autophagy, and MAPK pathway activation via ROS-mediated signaling in human CRC cells. [Read the Full Post]

Chaetocin-mediated SUV39H1 inhibition targets stemness and oncogenic networks of diffuse midline gliomas and synergizes with ONC201

473 | Jan 22 2024

Targeting the SUV39H1-H3K9me3 pathway in DIPG cells with chaetocin, and combining it with a DRD2 antagonist like ONC201, presents a promising strategy for effective treatment by exploiting vulnerabilities and overcoming resistance mechanisms. [Read the Full Post]

Synthesis and structure-activity relationship of new nicotinamide phosphoribosyltransferase inhibitors with antitumor activity on solid and haematological cancer

213 | Jan 21 2024

The synthesized compounds, particularly 35a, 39a, and 47, exhibit potent nanomolar/sub-nanomolar cytotoxicity against a range of cancer cell lines, showcasing promising anti-cancer potential via NAMPT inhibition and subsequent disruption of the NAD+ pathway, leading to cell death. [Read the Full Post]

Gastrodin overcomes chemoresistance via inhibiting Skp2-mediated glycolysis

259 | Jan 18 2024

The study highlights the potential of targeting the Skp2-Akt axis and utilizing gastrodin, inhibiting HK2-mediated glucose metabolism and promoting apoptosis, as a promising combined therapeutic approach for overcoming cisplatin resistance in oral squamous cell carcinoma (OSCC). [Read the Full Post]

CYD0281, a Bcl-2 BH4 domain antagonist, inhibits tumor angiogenesis and breast cancer tumor growth

155 | Jan 17 2024

CYD0281, a newly discovered Bcl-2-BH4 antagonist, demonstrates remarkable potential as an anti-angiogenic therapy for breast cancer by inducing a conformational shift in Bcl-2, converting it into a pro-apoptotic molecule and inhibiting tumor growth. [Read the Full Post]

Lactate Dehydrogenase Gene Family in Spirometra mansoni (Cestoda: Diphyllobothriidea)-Phylogenetic Patterns and Molecular Characteristics

258 | Jan 16 2024

This study on Spirometra mansoni identified 19 novel LDH members, delineated their expression patterns across developmental stages, characterized their structural features, enzymatic properties, and inhibition, providing fundamental insights into the diverse roles of LDHs in this parasite and related taxa. [Read the Full Post]

Percutaneous coronary intervention with ridaforolimus-eluting stents in long lesions: the BIONICS 38 mm prospective trial

339 | Jan 08 2024

The study evaluating the 38 mm ridaforolimus-eluting stent in percutaneous coronary intervention for long lesions demonstrated high efficacy, low rates of major adverse cardiovascular events, and successful treatment outcomes, supporting its safety and effectiveness in this patient group. [Read the Full Post]

Sertad1 Induces Neurological Injury after Ischemic Stroke via the CDK4/p-Rb Pathway

680 | Jan 06 2024

Sertad1, upregulated in ischemic conditions, exacerbates neurological injury by activating the CDK4/p-Rb pathway, promoting cell cycle dysregulation and apoptotic cell death. [Read the Full Post]

Mechanism of RIP2 enhancing stemness of glioma cells induces temozolomide resistance

307 | Jan 06 2024

The study elucidates that the receptor-interacting protein 2 (RIP2) mediates temozolomide (TMZ) resistance in gliomas by regulating stemness through the NF-κB pathway, potentially offering a novel therapeutic target for overcoming drug resistance in these tumors. [Read the Full Post]

Herbal compound cepharanthine attenuates inflammatory arthritis by blocking macrophage M1 polarization

204 | Jan 04 2024

Cepharanthine (CEP) exhibits promising potential as a rheumatoid arthritis treatment by effectively reducing joint inflammation, inhibiting M1 macrophage polarization, and modulating key signaling pathways and metabolic processes associated with the disease. [Read the Full Post]

Runx3 Restoration Regresses K-Ras-Activated Mouse Lung Cancers and Inhibits Recurrence

364 | Jan 02 2024

The study's findings suggest that the restoration of RUNX3 presents a promising therapeutic avenue for effectively treating K-RAS-activated lung cancers by regressing tumors and suppressing recurrence through multifaceted pathways, potentially offering a durable response. [Read the Full Post]

Identification of upregulated genes in glioblastoma and glioblastoma cancer stem cells using bioinformatics analysis

427 | Dec 29 2023

This comprehensive study uncovered potential therapeutic targets for glioblastoma by identifying highly coexpressed genes in cancer stem cells, highlighting DUSP6 and SOX2 as prognostically relevant hub genes and proposing (E/Z)-BCI and BCI compounds as promising anti-cancer agents via strong binding interactions with DUSP6's ERK2 binding domain. [Read the Full Post]

Role of parthenolide in paclitaxel-induced oxidative stress injury and impaired reproductive function in rat testicular tissue

623 | Dec 28 2023

Parthenolide treatment in rats demonstrated a dose-dependent mitigation of oxidative stress-induced testicular damage caused by paclitaxel, showing promise as a potential therapeutic avenue for addressing testicular toxicity and supporting reproductive function. [Read the Full Post]

Adaptive c-Met-PLXDC2 Signaling Axis Mediates Cancer Stem Cell Plasticity to Confer Radioresistance-associated Aggressiveness in Head and Neck Cancer

291 | Dec 27 2023

The identification of c-Met phosphorylation as a pivotal mechanism driving radioresistance-associated aggressiveness in HNSCC cells offers a promising therapeutic strategy by targeting this pathway with inhibitors like SU11274 to enhance the efficacy of radiotherapy. [Read the Full Post]

PM2.5 induces cardiac malformations via PI3K/akt2/mTORC1 signaling pathway in zebrafish larvae

417 | Dec 27 2023

Exposure to PM2.5 triggers a complex cascade involving PI3K/akt2/mTORC1 signaling through AHR/ROS-induced PTEN suppression, leading to mitochondrial-mediated intrinsic apoptosis, Wnt signaling suppression, and ultimately contributing to cardiac defects in zebrafish larvae. [Read the Full Post]

Potential role of Acanthamoeba Rab7

393 | Dec 26 2023

The study elucidates the pivotal role of AcRab7 in Acanthamoeba castellanii's phagocytosis, endosomal delivery, and cellular physiology, demonstrating its influence on energy production, cell proliferation, and potential implications for understanding related parasitic diseases. [Read the Full Post]

Myo/Nog Cells: The Jekylls and Hydes of the Lens

190 | Dec 26 2023

This comprehensive study unveils the versatile behavior of Myo/Nog cells from embryonic development to adulthood, elucidating their crucial roles in eye formation, lens structure, and potential therapeutic avenues for preventing fibrotic diseases in ocular tissues. [Read the Full Post]

Hepatocyte growth factor attenuates high glucose-disturbed mitochondrial dynamics in podocytes by decreasing ARF6-dependent DRP1 translocation

134 | Dec 23 2023

This study illuminates the pivotal role of HGF in preserving mitochondrial homeostasis in diabetic podocytes via ARF6 activation, offering a novel pathway for mitigating renal damage in diabetic nephropathy. [Read the Full Post]

Exercise attenuates neuronal degeneration in Parkinson's disease rat model by regulating the level of adenosine 2A receptor

649 | Dec 23 2023

Exercise appears to mitigate Parkinson's disease symptoms in rats by reducing neurodegeneration through a-synuclein aggregation reduction and adenosine 2A receptor modulation, although the co-administration of an adenosine A2A receptor agonist reverses these beneficial effects. [Read the Full Post]

MCL1 Inhibition Overcomes the Aggressiveness Features of Triple-Negative Breast Cancer MDA-MB-231 Cells

95 | Dec 22 2023

Inhibiting MCL1 through A-1210477 in triple-negative breast cancer (TNBC) MDA-MB-231 cells induces anoikis, impedes focal adhesion-mediated survival signaling pathways, diminishes migratory and invasive capabilities, reverses epithelial-mesenchymal transition (EMT) features, and suppresses stemness markers, suggesting a critical role for MCL1 in regulating TNBC aggressiveness and metastatic potential. [Read the Full Post]

Degradation of MK2 with natural compound andrographolide: A new modality for anti-inflammatory therapy

247 | Dec 22 2023

Andrographolide, a natural compound, demonstrates anti-inflammatory effects by selectively inhibiting and promoting proteasome-mediated degradation of MK2 within the p38MAPK-MK2 signaling axis, offering a novel therapeutic approach for inflammatory diseases. [Read the Full Post]

Improving Speed and Affordability without Compromising Accuracy: Standard Binding Free-Energy Calculations Using an Enhanced Sampling Algorithm, Multiple-Time Stepping, and Hydrogen Mass Repartitioning

219 | Dec 21 2023

The study proposes an accelerated computational strategy, combining longer time steps with hydrogen-mass repartitioning and multiple time-stepping, to efficiently calculate protein-ligand binding free energies using well-tempered metadynamics, significantly reducing computational time without compromising accuracy. [Read the Full Post]

Predictive model for treatment outcomes of peripheral T-cell lymphoma, not otherwise specified, in Taiwanese patients

392 | Dec 20 2023

In this retrospective study of 104 peripheral T-cell lymphoma-not otherwise specified (PTCL-NOS) patients in Taiwan, the investigation revealed a poor prognosis, highlighted the potential efficacy of pralatrexate as salvage chemotherapy for eligible patients, identified adverse prognostic factors, and proposed a novel predictive index with distinct risk groups, emphasizing the need for further validation and exploration of improved treatment strategies. [Read the Full Post]

The Ubiquitin-Proteasome System Facilitates Membrane Fusion and Uncoating during Coronavirus Entry

201 | Dec 19 2023

Inhibiting the ubiquitin-proteasome system (UPS) at the early infection stage severely impairs the infectivity of Infectious Bronchitis Virus (IBV) and Porcine Epidemic Diarrhea Virus (PEDV) by preventing membrane fusion, uncoating, initial translation, and replication events, highlighting the UPS as a potential target for antiviral therapies against coronaviruses. [Read the Full Post]

GPER1 contributes to T3-induced osteogenesis by mediating glycolysis in osteoblast precursors

213 | Dec 13 2023

T3 promotes osteogenesis in MC3T3-E1 cells by enhancing GPER1-mediated glycolysis, as evidenced by increased osteogenic activities, which are reversed by GPER1 inhibition and glycolysis blockade. [Read the Full Post]

Glucose metabolic upregulation via phosphorylation of S6 ribosomal protein affects tumor progression in distal cholangiocarcinoma

381 | Dec 13 2023

In summary, the study reveals that inhibiting phosphorylated S6 ribosomal protein, a marker of mTORC1 activity, suppresses glucose metabolism pathways and reduces cell proliferation, suggesting mTORC1 as a potential therapeutic target in distal cholangiocarcinoma. [Read the Full Post]

The Multikinase Inhibitor AD80 Induces Mitotic Catastrophe and Autophagy in Pancreatic Cancer Cells

361 | Dec 10 2023

The study reveals that AD80, a multikinase inhibitor, exerts potent antineoplastic effects in pancreatic cancer cells by inducing mitotic aberrations, DNA damage, autophagy, and apoptosis, providing crucial insights into potential targeted therapeutic strategies for this deadly disease. [Read the Full Post]

Topical Management of Pediatric Psoriasis: A Review of New Developments and Existing Therapies

167 | Dec 09 2023

The recent approval of topical agents like Roflumilast and Tapinarof, along with ongoing research into various targeted therapies and optimized formulations, represents a promising shift in the management of pediatric psoriasis, offering diverse and potentially more effective treatment options for young patients. [Read the Full Post]

Targeted Regulation of Osteoblasts and Osteoclasts in Osteosarcoma Patients by CSF3R Receptor Inhibition of Osteolysis Caused by Tumor Inflammation Based on Transcriptional Spectrum Analysis and Drug Library Screening

235 | Dec 08 2023

**In summary, the study identifies CSF3R as a key regulator in osteosarcoma progression, influencing bone destruction and patient prognosis by modulating the inflammatory response of osteoblasts and osteoclasts, with Leucovorin and Methotrexate identified as potential therapeutic compounds.** [Read the Full Post]

Transcriptomics-Guided In Silico Drug Repurposing: Identifying New Candidates with Dual-Stage Antiplasmodial Activity

432 | Dec 08 2023

The research effort identified two promising compounds, HSP-990 and silvestrol aglycone, demonstrating potent inhibitory activity at nanomolar concentrations against the asexual blood stage of Plasmodium falciparum, with silvestrol aglycone showing low cytotoxicity and transmission-blocking potential, indicating their potential as dual-acting antimalarial and transmission-blocking candidates for malaria control. [Read the Full Post]

PFKFB3 Increases IL-1 β and TNF- α in Intestinal Epithelial Cells to Promote Tumorigenesis in Colitis-Associated Colorectal Cancer

240 | Dec 07 2023

Elevated expression of PFKFB3 in colitis-associated colorectal cancer promotes tumorigenesis by inducing phospho-p65 and the expression of pro-inflammatory cytokines IL-1β and TNF-α, highlighting PFKFB3 as a potential therapeutic target. [Read the Full Post]

Dnmt3a is downregulated by Stat5a and mediates G0/G1 arrest by suppressing the miR-17-5p/Cdkn1a axis in Jak2V617F cells

330 | Dec 06 2023

**In Jak2V617F positive classical myeloproliferative neoplasms, aberrant activation of Stat5a downregulates Dnmt3a through binding to its promoter, leading to dysregulation of the miR-17-5p/Cdkn1a axis and G0/G1 cell cycle arrest, providing a potential therapeutic target.** [Read the Full Post]

UMI-77 Modulates the Complement Cascade Pathway and Inhibits Inflammatory Factor Storm in Sepsis Based on TMT Proteomics and Inflammation Array Glass Chip

113 | Dec 05 2023

UMI-77, administered at 7.0 mg/kg, significantly improves the survival rate of septic mice by suppressing inflammatory storm-related cytokines and modulating the complement cascade pathway, revealing its potential as a treatment for sepsis. [Read the Full Post]

Development of a Once-Daily Modified-Release Formulation for the Short Half-Life RIPK1 Inhibitor GSK2982772 using DiffCORE Technology

166 | Dec 05 2023

The study confirmed the efficacy of GSK proprietary DiffCORE™ technology in creating a stable once-daily pharmacokinetic profile for GSK2982772, overcoming susceptibility to food effects observed in the previous matrix monolithic formulation and leading to the selection of the MR-16 h formulation for further clinical development. [Read the Full Post]

Regional regulatory harmonisation initiatives: Their potential contribution to the newly established African medicines agency

557 | Nov 30 2023

The study highlights the foundational role of regional medicines regulatory harmonization programs, such as the African Medicines Regulatory Harmonisation (AMRH) and East African Community Medicines Regulatory Harmonisation (EAC-MRH) initiatives, in supporting the operationalization of the African Medicine Agency (AMA), emphasizing the importance of strong national regulatory authorities and increased ratification of the AMA Treaty for ensuring access to essential medical products and technologies for the African people. [Read the Full Post]

Finding Lead Compounds for Dengue Antivirals from a Collection of Old Drugs through In Silico Target Prediction and Subsequent In Vitro Validation

195 | Nov 30 2023

This study utilized ligand-based and proteochemometric prediction models, coupled with experimental assays and molecular docking, to identify and validate potential DENV NS3 inhibitors, highlighting five promising lead compounds (ziltri, zilool, zileuton, linalool, and trimethadione) for further development as antiviral treatments. [Read the Full Post]

Imidazole-4-N-acetamide Derivatives as a Novel Scaffold for Selective Targeting of Cyclin Dependent Kinases

130 | Nov 28 2023

The study explored imidazole-4-N-acetamide substituted derivatives of the pan-CDK inhibitor PHA-793887 and demonstrated a strong correlation between calculated binding parameters using non-equilibrium thermodynamics and inhibitory potencies in in vitro kinase assays, highlighting the method's effectiveness in predicting the activity of potential anticancer drug candidates. [Read the Full Post]

Cytoplasmic Hsp70s promote EcR transport into the nucleus by responding to various stimuli

385 | Nov 27 2023

This study reveals that cytoplasmic Hsp70s facilitate the transport of the ecdysone receptor (EcR) into the nucleus in response to diverse stimuli, shedding light on the intricate mechanisms underlying insect metamorphosis and highlighting potential applications in pest control and broader biological research. [Read the Full Post]

HDAC11 mediates the ubiquitin-dependent degradation of p53 and inhibits the anti-leukemia effect of PD0166285

144 | Nov 23 2023

The study demonstrates the potential of the WEE1 inhibitor PD0166285 as a promising chemotherapeutic drug for acute myeloid leukemia, highlighting the negative correlation between HDAC11 expression and AML patient survival, and revealing HDAC11's impact on p53 stability and MAPK pathway phosphorylation levels. [Read the Full Post]

Direct Differentiation of Bone Marrow Mononucleated Cells Into Insulin-Producing Cells Using 4 Specific Soluble Factors

300 | Nov 23 2023

The study developed a differentiation method using a unique combination of four differentiation-inducing factors to transform bone marrow-derived stem cells into mature insulin-producing cells, offering a potential novel approach for cell-based therapy in diabetes mellitus. [Read the Full Post]

Heat shock factor 1 is a promising therapeutic target against adult T-cell leukemia

477 | Nov 18 2023

Targeting the overexpressed heat shock factor 1 (HSF1) with the inhibitor KRIBB11 inhibits proliferation, induces apoptosis, disrupts essential signaling pathways, and sensitizes adult T-cell leukemia cells to HSP90 inhibition, offering a potential therapeutic approach for ATL. [Read the Full Post]

Use of RIP1 Kinase Small-Molecule Inhibitors in Studying Necroptosis

132 | Nov 18 2023

The careful selection and application of small-molecule inhibitors, considering parameters such as potency, selectivity, in vivo efficacy, and potential limitations, are essential for unraveling the complex biology of RIP1 kinase and its role in inflammation and disease pathogenesis. [Read the Full Post]

Hydrogen Sulfide Improves Outcomes in a Murine Model of Necrotizing Enterocolitis via the Cys440 Residue on Endothelial Nitric Oxide Synthase

431 | Nov 17 2023

GYY4137 administration improves clinical outcomes, attenuates intestinal and lung injury, and enhances perfusion in a murine model of necrotizing enterocolitis, with these protective effects being contingent upon the presence of the Cys440 residue in endothelial nitric oxide synthase (eNOS). [Read the Full Post]

FASN inhibition targets multiple drivers of NASH by reducing steatosis, inflammation and fibrosis in preclinical models

171 | Nov 15 2023

FASN inhibition demonstrates promising potential as a therapeutic strategy for NASH by targeting multiple hallmarks of the disease, including reducing hepatic fat accumulation, mitigating inflammation, and attenuating fibrosis. [Read the Full Post]

IL-17 Is a Key Regulator of Mucin-Galectin-3 Interactions in Asthma

302 | Nov 15 2023

Galectin-3 (Gal-3) appears to play a pivotal role in the pathogenesis of asthma by regulating airway inflammation and mucin gene expression, suggesting that targeting Gal-3 could be a promising therapeutic strategy for the disease. [Read the Full Post]

Analysis of the ERK Pathway Cysteinome for Targeted Covalent Inhibition of RAF and MEK Kinases

0 | Nov 14 2023

This research investigates the potential for covalent inhibitors targeting specific cysteine residues in key kinases of the ERK pathway to overcome resistance mechanisms and enhance the efficacy of cancer treatment. [Read the Full Post]

Scutellarin suppresses the metastasis of triple-negative breast cancer via targeting TNFα/TNFR2-RUNX1-triggered G-CSF expression in endothelial cells

654 | Nov 13 2023

Scutellarin (SC) inhibits metastasis in triple-negative breast cancer (TNBC) by disrupting the TNFα/TNFR2-initiated RUNX1 activation and subsequent G-CSF production in TNBC-associated endothelial cells (ECs). [Read the Full Post]

Tumor-associated astrocytes promote tumor progression of Sonic Hedgehog medulloblastoma by secreting lipocalin-2

517 | Nov 12 2023

The research reveals that tumor-associated astrocytes (TAAs) secrete lipocalin-2 (LCN2) through the STAT3 signaling pathway, promoting the progression of Sonic Hedgehog (SHH) subgroup medulloblastoma (MB) and indicating LCN2's potential as a prognostic marker and therapeutic target. [Read the Full Post]

Segmental Zoster Paresis Accompanied by Horner's Syndrome

556 | Nov 11 2023

In this case, a 90-year-old immunocompromised woman developed right upper limb weakness and Horner's syndrome following oral therapy for zoster on the right T2 dermatome, with aggressive intravenous treatment leading to improvement in the former but persistence of the latter. [Read the Full Post]

Senolytic Combination Treatment Is More Potent Than Single Drugs in Reducing Inflammatory and Senescence Burden in Cells from Painful Degenerating IVDs

237 | Nov 09 2023

Combining the senolytic drugs o-Vanillin and RG-7112 effectively removes senescent cells, reduces inflammation and pain mediators, and inhibits neuronal sprouting, offering promise as a potential treatment for low back pain associated with intervertebral disc degeneration. [Read the Full Post]

Combined inhibition of aurora kinases and Bcl-xL induces apoptosis through select BH3-only proteins

0 | Nov 08 2023

The study demonstrates that combining small-molecule inhibitors of AURK with BH3-mimetic inhibitors targeting Bcl-xL potently induces apoptosis and may overcome resistance to AURK inhibitors in colon cancer cells. [Read the Full Post]

Efficacy and safety of irinotecan combined with raltitrexed or irinotecan monotherapy for salvage chemotherapy of esophageal squamous cell cancer: A prospective, open label, randomized phase II study

285 | Nov 08 2023

The combination of irinotecan and raltitrexed may lead to better progression-free survival and overall survival compared to irinotecan monotherapy, especially in the second-line treatment of metastatic esophageal squamous cell cancer. [Read the Full Post]

Targeting GSTP1 as Therapeutic Strategy against Lung Adenocarcinoma Stemness and Resistance to Tyrosine Kinase Inhibitors

326 | Nov 07 2023

The study reveals that upregulation of Glutathione S-transferase pi (GSTP1) in lung adenocarcinoma (LUAD) supports cancer stem cells, tumor self-renewal, metastasis, and resistance to targeted therapies, making it a promising therapeutic target for long-term control of LUAD. [Read the Full Post]

The expanding role of IAP antagonists for the treatment of head and neck cancer

225 | Nov 07 2023

IAP antagonists, also known as SMAC mimetics, have shown promising results in preclinical and clinical studies as potential anti-cancer therapeutics for head and neck squamous cell carcinomas (HNSCC), particularly when combined with radiation therapy. [Read the Full Post]

Experimental and Theoretical Estimations of Atrazine's Adsorption in Mangosteen-Peel-Derived Nanoporous Carbons

192 | Nov 06 2023

This study investigated the removal of atrazine using nanoporous carbons derived from mangosteen-peel chars, focusing on the role of nitrogen groups and surface chemistry, and elucidating the importance of micropores and mesopores in the adsorption process. [Read the Full Post]

Acetaminophen impairs ferroptosis in the hippocampus of septic mice by regulating glutathione peroxidase 4 and ferroptosis suppressor protein 1 pathways

98 | Nov 05 2023

Acetaminophen (APAP) inhibits neuronal ferroptosis in the hippocampal tissues of septic mice through the GPX4 and FSP1 pathways, leading to improved cognitive function and increased survival rate. [Read the Full Post]

Production of highly pure R,R-2,3-butanediol for biological plant growth promoting agent using carbon feeding control of Paenibacillus polymyxa MDBDO

370 | Nov 03 2023

The study demonstrates the potential of Paenibacillus polymyxa MDBDO as a biological plant growth promoting agent and outlines a fermentation strategy for the production of highly pure R,R-2,3-butanediol (R,R-2,3-BDO) at high concentrations, which significantly stimulates the growth of soybean and strawberry seedlings. [Read the Full Post]

Iron overload due to SLC40A1 mutation of type 4 hereditary hemochromatosis

233 | Oct 30 2023

The reported case of hereditary hemochromatosis type 4B involving a SLC40A1 gene mutation was effectively treated with monthly red blood cell apheresis followed by oral deferasirox therapy. [Read the Full Post]

Identification of novel inhibitors for trigger factor (TF) of M. tb: an in silico investigation

201 | Oct 29 2023

A computational model of the Mycobacterium tuberculosis trigger factor protein was developed and two potential inhibitors, HTS02984 and S06856, were identified through virtual screening, offering potential avenues for the development of tuberculosis therapies. [Read the Full Post]

BTBBCL6 dimers as building blocks for reversible drug-induced protein oligomerization

240 | Oct 29 2023

This study characterized the BTB domain of the transcription factor BCL6 as a small-molecule-controlled, reversible oligomerization switch, enabling precise control over protein function and demonstrating its potential for synthetic biology applications. [Read the Full Post]

Tumor lysates-constructed hydrogel to potentiate tumor immunotherapy

185 | Oct 29 2023

An injectable tumor lysates-constructed hydrogel has been developed to address the challenges of T cell-based immunotherapy, providing a robust antigen reservoir, preventing T cell exhaustion, and suppressing immune evasion, thereby enhancing the effectiveness of tumor treatment. [Read the Full Post]

Inhibiting STAT5 significantly attenuated Ang II-induced cardiac dysfunction and inflammation

239 | Oct 28 2023

Inhibition of STAT5 using STAT5-IN-1 effectively reduces cardiac hypertrophy in Ang II-induced mice by decreasing inflammation, suggesting a potential therapeutic strategy for mitigating hypertrophy. [Read the Full Post]

The effectiveness of tivantinib for MET-high hepatocellular carcinoma: A protocol for meta analysis

169 | Oct 27 2023

The meta-analysis findings suggest that tivantinib does not appear to confer a significant benefit for the treatment of MET-high hepatocellular carcinoma, and it is associated with an increased risk of grade ≥3 neutropenia and leukopenia. [Read the Full Post]

Tenuifolin in the prevention of Alzheimer's disease-like phenotypes: Investigation of the mechanisms from the perspectives of calpain system, ferroptosis, and apoptosis

192 | Oct 26 2023

Tenuifolin (Ten), an active component of Polygala tenuifolia, prevents Alzheimer's disease (AD)-like phenotypes through multiple mechanisms, including regulation of synaptic plasticity, apoptosis, calcium signaling, oxidative stress, and ferroptosis. [Read the Full Post]

Genome-wide CRISPR screening reveals key genes and pathways associated with 20-hydroxyecdysone signal transduction in the silkworm (Bombyx mori)

388 | Oct 26 2023

This study utilized a genome-wide CRISPR/Cas9-based library to identify key genes involved in the 20E signaling pathway in the silkworm, shedding light on the mechanisms underlying metamorphosis and hormone regulation. [Read the Full Post]

Tryptophan metabolism induced by TDO2 promotes prostatic cancer chemotherapy resistance in a AhR/c-Myc dependent manner

542 | Oct 25 2023

Elevated expression of tryptophan 2,3-dioxygenase 2 (TDO2) promotes tryptophan metabolism and kynurenine production, activating the AhR/c-Myc/ABC-SLC transporters signaling pathway and contributing to chemoresistance in prostatic cancer. [Read the Full Post]

EGR1-mediated metabolic reprogramming to oxidative phosphorylation contributes to ibrutinib resistance in B cell lymphoma

337 | Oct 24 2023

The study identifies EGR1-mediated metabolic reprogramming to oxidative phosphorylation as a key mechanism driving ibrutinib resistance in B cell malignancies, suggesting that targeting this pathway with agents like metformin or IM156 could provide a potential therapeutic strategy to overcome acquired drug resistance in relapsed/refractory DLBCL or MCL. [Read the Full Post]

Pak1 pathway hyper-activation mediates resistance to endocrine therapy and CDK4/6 inhibitors in ER+ breast cancer

270 | Oct 23 2023

This study demonstrates that p21-activated kinase 1 (Pak1) plays a crucial role in resistance to estrogen receptor antagonists and CDK4/6 inhibitors in estrogen receptor-positive (ER+) breast cancer, suggesting the potential for Pak1 inhibitors as a therapeutic approach for patients with ER+ breast cancer who have become resistant to current treatments. [Read the Full Post]

[p53 regulates primordial follicle activation through the mTOR signaling pathway]

538 | Oct 22 2023

This study demonstrated that p53 inhibits primordial follicle activation through the mTOR signaling pathway, thereby maintaining the reserve of primordial follicles. [Read the Full Post]

[Efficacy of Tyrosine Kinase Inhibitor Combined with Decitabine, Homoharringtonine, Interferon in the Maintenance Therapy of Blast Phase Chronic Myeloid Leukemia]

247 | Oct 21 2023

The combination of tyrosine kinase inhibitor (TKI) with decitabine, homoharringtonine, and interferon as maintenance therapy significantly prolongs event-free survival, duration of remission, and overall survival in blast phase chronic myeloid leukemia (CML-BP) patients who have achieved a major hematological response compared to TKI combined with conventional chemotherapy. [Read the Full Post]

Purine Antimetabolites associated Pneumocystis Jiroveci Pneumonia

426 | Oct 20 2023

The retrospective disproportionality analysis of the FDA Adverse Event Reporting System (FAERS) database revealed a significant safety signal for pneumocystis jiroveci pneumonia (PJP) associated with purine antimetabolites, particularly fludarabine and thioguanine, among populations with autoimmune disorders and cancer. [Read the Full Post]

Improved antitumor activity against prostate cancer via synergistic targeting of Myc and GFAT-1

220 | Oct 19 2023

Simultaneous targeting of Myc and GFAT-1 using inhibitors and a nanocarrier delivery system shows promise as a novel strategy for the treatment of prostate cancer. [Read the Full Post]

Targeting the DNA Damage Response and DNA Repair Pathways to Enhance Radiosensitivity in Colorectal Cancer

198 | Oct 17 2023

Targeting DNA damage response and repair pathways with inhibitors of cell-cycle checkpoint proteins represents a promising strategy to overcome radioresistance and improve the sensitivity of colorectal cancer cells to radiotherapy, with potential for combination therapies involving immunotherapy. [Read the Full Post]

Bioactive components and molecular mechanisms of Salvia miltiorrhiza Bunge in promoting blood circulation to remove blood stasis

447 | Oct 16 2023

Salvia miltiorrhiza Bunge (SM) contains phenolic acids and tanshinones that synergistically target multiple signaling pathways to enhance blood circulation and alleviate blood stasis, making it an effective herbal medicine for the treatment of blood stasis syndrome. [Read the Full Post]

Coordination-Driven Self-Assembly of Biomedicine to Enhance Photodynamic Therapy by Inhibiting Proteasome and Bcl-2

141 | Oct 16 2023

BSC, a self-delivery biomedicine formed through the coordination-driven self-assembly of BTZ, Sab, and Ce6, combines proteasome and Bcl-2 inhibitions with photodynamic therapy, exhibiting superior efficacy in tumor treatment and controlled drug release in the acidic tumor microenvironment. [Read the Full Post]

VPS34-IN1 induces apoptosis of ER+ breast cancer cells via activating PERK/ATF4/CHOP pathway

367 | Oct 14 2023

VPS34-IN1, a selective inhibitor of Class III Phosphatidylinositol 3-kinase (PI3K), exhibits an antitumor effect in estrogen receptor positive (ER+) breast cancer by activating the PERK/ATF4/CHOP pathway of endoplasmic reticulum (ER) stress to induce apoptosis in breast cancer cells. [Read the Full Post]

PTK2B regulates immune responses of neutrophils and protects mucosal inflammation in ulcerative colitis

358 | Oct 14 2023

Proline-rich tyrosine kinase 2B (PTK2B) plays a role in the pathogenesis of ulcerative colitis (UC) by promoting neutrophil migration and inhibiting mucosal inflammation, making it a potential therapeutic target for UC treatment. [Read the Full Post]

Potential New Therapeutic Approaches for Cisplatin-Resistant Testicular Germ Cell Tumors

245 | Oct 14 2023

The proteasome inhibitor MG-132 shows promise as a potential new drug for treating cisplatin-resistant testicular germ cell tumors (TGCTs), enhancing sensitivity to cisplatin and inducing apoptosis in both parental and resistant cell lines. [Read the Full Post]

Construction and Validation of Protein Expression-related Prognostic Models in Clear Cell Renal Cell Carcinoma

352 | Oct 10 2023

The study developed a prognostic evaluation model for ccRCC patients using bioinformatics methods, identified 13 independent prognostic proteins, and demonstrated their strong predictive ability for patient survival, while also identifying potential drugs for targeted therapy. [Read the Full Post]

The protective effects of NE 52-QQ57 against interleukin-33-induced inflammatory response in activated synovial mast cells

595 | Oct 09 2023

The study suggests that inhibiting GPR4 signaling with the antagonist NE 52-QQ57 may have therapeutic benefits in rheumatoid arthritis by reducing inflammatory responses and oxidative stress in synovial mast cells. [Read the Full Post]

Tamoxifen resistance induction results in the upregulation of ABCG2 expression and mitoxantrone resistance in MCF-7 breast cancer cells

457 | Oct 07 2023

The study found that prolonged exposure of ER+ MCF-7 breast cancer cells to tamoxifen led to increased expression of the ABCG2 pump, associated with TAM resistance and potential cross-resistance to mitoxantrone. [Read the Full Post]

Anti-hepatocellular carcinoma activity of the cyclin-dependent kinase inhibitor AT7519

355 | Oct 07 2023

The research findings suggest that AT7519, a CDK inhibitor, shows potential as a monotherapy or in combination with drugs like gefitinib or cabozantinib, to improve the effectiveness of treatments for hepatocellular carcinoma. [Read the Full Post]

Preparation and Properties of Natural Polysaccharide-Based Drug Delivery Nanoparticles

310 | Oct 05 2023

The paper presents the development of RGD-(NPGP/CS)3NPGP nanoparticles through layer-by-layer assembly, which demonstrate high encapsulation efficiency, pH-sensitive release, and effective targeting to integrin receptor-expressing tumor cells, making them promising as novel anticancer drug carriers. [Read the Full Post]

Nr4a1 promotes renal interstitial fibrosis by regulating the p38 MAPK phosphorylation

254 | Oct 05 2023

Nr4a1 promotes renal fibrosis by activating p38 MAPK, as evidenced by its upregulation in a mouse model of renal interstitial fibrosis, its correlation with fibrotic protein levels, and the exacerbation of fibrosis by Nr4a1 activation and its inhibition by p38 MAPK blockade. [Read the Full Post]

Translation-dependent skin hyperplasia is promoted by type 1/17 inflammation in psoriasis

394 | Oct 05 2023

This study reveals that the molecule eukaryotic initiation factor 4E (eIF4E) plays a crucial role in the abnormal differentiation of keratinocytes driven by type 1/17 inflammation in psoriasis, suggesting its potential as a therapeutic target. [Read the Full Post]

APX-115, a pan-NADPH oxidase inhibitor, protects development of diabetic nephropathy in podocyte specific NOX5 transgenic mice

0 | Oct 02 2023

APX-115, a pan-NOX inhibitor, shows potential as a promising therapeutic agent for the treatment of diabetic nephropathy by improving pancreatic beta cell function, reducing lipid levels, restoring kidney damage markers, and exerting anti-inflammatory effects. [Read the Full Post]

KRASG12C mutation-induced TOPK overexpression contributes to tumour progression in non-small cell lung cancer

259 | Sep 30 2023

The study reveals that the KRAS-TOPK axis contributes to the progression of non-small cell lung cancer (NSCLC) with the KRASG12C mutation, and targeting this axis could enhance the anticancer effects of existing chemotherapeutics. [Read the Full Post]

RNF112-mediated FOXM1 ubiquitination suppresses the proliferation and invasion of gastric cancer

485 | Sep 27 2023

RNF112 suppresses gastric cancer progression by directly ubiquitinating FOXM1, making the RNF112/FOXM1 axis a potential prognostic biomarker and therapeutic target in gastric cancer. [Read the Full Post]

Pathway network of pyroptosis and its potential inhibitors in acute kidney injury

349 | Sep 23 2023

This article reviews the role of pyroptosis in acute kidney injury (AKI), focusing on the assembly and activation of the NLRP3 inflammasome and its downstream inflammatory cytokines as potential therapeutic targets for novel AKI therapies. [Read the Full Post]

Precious Gene: The Application of RET-Altered Inhibitors

409 | Sep 23 2023

The novel RET-specific inhibitors selpercatinib and pralsetinib, along with ongoing clinical trials of TPX-0046 and zetletinib, demonstrate promising efficacy and safety in the treatment of RET-altered cancers, addressing the limitations of previous multikinase inhibitors. [Read the Full Post]

Metformin protects against retinal ischemia/reperfusion injury through AMPK-mediated mitochondrial fusion

120 | Sep 22 2023

Metformin exhibits a protective effect against retinal ischemia/reperfusion (I/R) injury by promoting AMPK-mediated mitochondrial fusion and reducing mitochondrial reactive oxygen species (ROS) generation. [Read the Full Post]

Optimization of CAR-T Cell-Based Therapies Using Small-Molecule-Based Safety Switches

273 | Sep 21 2023

Cutting-edge investigations are underway to develop small-molecule-based safety switches for CAR-T cells, enabling pharmacological control over their activities and toxicities to improve the safety and efficacy of CAR-T cell therapy for leukemia. [Read the Full Post]

Genome editing HLA alleles for a pilot immunocompatible hESC line in a Chinese hESC bank for cell therapies

233 | Sep 21 2023

The study successfully customized an immunocompatible human embryonic stem cell (hESC) line based on Chinese HLA typing characteristics, providing a potential basis for establishing a universal HLA-AR bank of hESCs and expediting the clinical application of hESC-based therapies. [Read the Full Post]

Acetylation regulates the nucleocytoplasmic distribution and oncogenic function of karyopherin alpha 2 in lung adenocarcinoma

413 | Sep 18 2023

The acetylation of KPNA2 by CBP/p300 promotes cytosolic localization and suppresses its oncogenic activity in lung cancer cells. [Read the Full Post]

Targeting CDK9 with selective inhibitors or degraders in tumor therapy: an overview of recent developments

182 | Sep 14 2023

This review discusses the development of selective CDK9 inhibitors and PROTAC degraders for the treatment of cancer, highlighting their structures, inhibitory effects, and the need for further research to explore their efficacy in specific tumor genotypes and combination regimens. [Read the Full Post]

Unique osteogenic profile of bone marrow stem cells stimulated in perfusion bioreactor is Rho-ROCK-mediated contractility dependent

160 | Sep 14 2023

This study demonstrates that fluid shear stress in a 3D dynamic culture system induces increased actomyosin contractility, upregulation of mechanoreceptors and focal adhesions, and promotes a unique osteogenic profile in bone marrow mesenchymal stem/stromal cells (BMSC), highlighting the importance of mechanical cues in regulating BMSC behavior for potential clinical applications in bone regeneration. [Read the Full Post]

Increased NOX2 expression in astrocytes leads to eNOS uncoupling through dihydrofolate reductase in endothelial cells after subarachnoid hemorrhage

326 | Sep 13 2023

Increased NOX2 expression in astrocytes after subarachnoid hemorrhage leads to eNOS uncoupling, exacerbating acute vasoconstriction and cerebral ischemia. [Read the Full Post]

Detection of Ras nanoclustering-dependent homo-FRET using fluorescence anisotropy measurements

331 | Sep 12 2023

Fluorescence anisotropy-based homo-FRET measurements using Ras-derived constructs labeled with a single fluorescent protein provide a sensitive and advantageous approach to investigate Ras nanoclustering and assess modulators of functional Ras membrane organization. [Read the Full Post]

Degradation of MYC by the mutant p53 reactivator drug, COTI-2 in breast cancer cells

299 | Sep 08 2023

The study demonstrated that the mutant p53 reactivating drug COTI-2 effectively degraded MYC protein and showed synergistic growth inhibition when combined with an MYC inhibitor, suggesting its potential as a broad-spectrum anticancer therapy. [Read the Full Post]

Targeting of SOS1: from SOS1 Activators to Proteolysis Targeting Chimeras

0 | Sep 08 2023

Research has led to the development of targeted therapies, including KRAS G12C-directed drugs and SOS1 inhibitors, with potential for treating specific mutations in lung, pancreatic, and colon cancers. [Read the Full Post]

RUNX1 isoform disequilibrium promotes the development of trisomy 21-associated myeloid leukemia

224 | Sep 07 2023

The study proposes that an imbalance of RUNX1 isoforms, particularly elevated expression of RUNX1A, in combination with the Gata1s mutation, contributes to the development of myeloid leukemia associated with Down syndrome (ML-DS), and restoring the equilibrium between RUNX1A and RUNX1C holds potential for targeted therapies. [Read the Full Post]

Early changes in circulating cell free KRAS G12C predicts response to adagrasib in KRAS mutant non-small cell lung cancer patients

465 | Sep 06 2023

Early changes in circulating tumor DNA (ctDNA) levels of KRAS G12C, assessed approximately three weeks into treatment, can predict the likelihood of a favorable objective clinical response in patients with advanced, KRAS G12C mutant lung cancer. [Read the Full Post]

The Therapeutic Landscape for KRAS-Mutated Colorectal Cancers

289 | Sep 06 2023

The development of selective inhibitors targeting KRAS mutations, such as the FDA-approved Sotorasib and Adagrasib, has shown promise in treating colorectal cancer, but further research is needed to optimize their efficacy and overcome treatment resistance. [Read the Full Post]

Exosomes secreted from cardiomyocytes suppress the sensitivity of tumor ferroptosis in ischemic heart failure

211 | Sep 05 2023

Myocardial infarction-induced exosomes containing miR-22-3p derived from cardiomyocytes suppress ferroptosis and decrease the sensitivity of tumor cells to ferroptosis inducers, suggesting the potential of targeting exosome-mediated communication as a novel therapeutic strategy for antitumor therapy. [Read the Full Post]

Targeting cryptic-orthosteric site of PD-L1 for inhibitor identification using structure-guided approach

306 | Sep 03 2023

This study utilized structure-assisted virtual screening and molecular dynamics simulations to identify two novel small molecule compounds as potential therapeutic candidates for inhibiting the PD-L1 protein-protein interaction in cancer treatment. [Read the Full Post]

Targeting KRAS in pancreatic cancer: Emerging therapeutic strategies

299 | Aug 30 2023

This chapter provides an overview of KRAS biochemistry, signaling pathways, different mutations, emerging KRAS-targeted therapies, combination strategies, challenges in KRAS targeting, and future directions with a specific emphasis on pancreatic cancer. [Read the Full Post]

Clinical Characterization of Targetable Mutations (BRAF V600E and KRAS G12C) in Advanced Colorectal Cancer-A Nation-Wide Study

452 | Aug 30 2023

The retrospective analysis revealed that BRAF V600E mutation in metastatic colorectal cancer is associated with factors such as female sex, right colon primary location, and specific histological features, while KRAS G12C mutation is linked to left colon primary tumors and brain metastases, suggesting potential therapeutic targets and the need for further investigation. [Read the Full Post]

Evaluation of KRASG12C inhibitor responses in novel murine KRASG12C lung cancer cell line models

444 | Aug 30 2023

The generation of three novel murine KRASG12C-driven lung cancer cell lines provides valuable models for studying and improving therapeutic combination strategies with KRASG12C inhibitors. [Read the Full Post]

Design of rigid protein-protein interaction inhibitors enables targeting of undruggable Mcl-1

133 | Aug 30 2023

This work demonstrates the successful design of highly rigid inhibitors that induce a deepening of the protein binding pocket, providing valuable insights for targeting protein-protein interactions (PPIs) and potentially enabling the development of therapies for hematological cancers. [Read the Full Post]

Synergism of BCL-2 family inhibitors facilitates selective elimination of senescent cells

208 | Aug 30 2023

This study investigates the synergistic effects of combining BCL-2 family inhibitors, particularly BH3 mimetics, to eliminate senescent cells and overcome resistance within the population, potentially providing a more effective and less toxic approach to treating age-associated diseases. [Read the Full Post]

Therapeutic inhibition of Bmi-1 ablates chemoresistant cancer stem cells in adenoid cystic carcinoma

302 | Aug 29 2023

Targeting Adenoid Cystic Carcinoma (ACC) Cancer Stem Cells (CSCs) with Bmi-1 inhibitors, such as PTC596, demonstrates the potential to overcome chemoresistance and prevent tumor relapse in ACC. [Read the Full Post]

Targeting of SOS1: from SOS1 Activators to Proteolysis Targeting Chimeras

370 | Aug 29 2023

The development of KRAS G12C-directed drugs and SOS1 inhibitors represents promising approaches for targeting mutated oncogenes in lung, pancreatic, and colon cancers. [Read the Full Post]

Lysosomal lipid peroxidation mediates immunogenic cell death

186 | Aug 28 2023

The study by Bhardwaj et al. demonstrates that the lysosomal inhibitor DC661 induces lysosomal lipid peroxidation, leading to lysosomal membrane permeabilization, tumor cell death, and subsequent immune-mediated tumor cell clearance, suggesting the potential for combined immunotherapy and lysosomal inhibition in clinical trials. [Read the Full Post]

Angiotensin-(1-7) ameliorates intestinal barrier dysfunction by activating the Keap1/Nrf2/HO-1 signaling pathway in acute pancreatitis

465 | Aug 27 2023

Ang-(1-7) attenuates acute pancreatitis-induced intestinal inflammation and oxidative injuries by activating the Keap1/Nrf2/HO-1 pathway. [Read the Full Post]

Effect of erythrophagocytosis-induced ferroptosis during angiogenesis in atherosclerotic plaques

236 | Aug 27 2023

Intraplaque angiogenesis leads to the release of erythrocytes, their phagocytosis by macrophages, and subsequent erythrophagocytosis-induced ferroptosis, which contributes to plaque destabilization in advanced atherosclerosis and can be prevented by the ferroptosis inhibitor UAMC-3203. [Read the Full Post]

FDA Approval Summary: Selpercatinib for the Treatment of Advanced RET Fusion-Positive Solid Tumors

204 | Aug 26 2023

On September 21, 2022, the FDA granted accelerated approval to selpercatinib (Retevmo) for the treatment of adult patients with locally advanced or metastatic solid tumors with a rearranged during transfection (RET) gene fusion, making it the first tissue-agnostic targeted therapy for RET alterations. [Read the Full Post]

The BET PROTAC inhibitor dBET6 protects against retinal degeneration and inhibits the cGAS-STING in response to light damage

272 | Aug 25 2023

The study demonstrates that targeted degradation of BET proteins using dBET6 effectively inhibits the cGAS-STING pathway in reactive retinal macrophages/microglia, providing neuroprotective effects and suggesting a potential therapeutic approach for retinal degenerative diseases. [Read the Full Post]

Therapeutic inhibition of Mcl-1 blocks cell survival in estrogen receptor-positive breast cancers

214 | Aug 24 2023

The study revealed that inhibiting Bcl-2 or Bcl-xL in ERα+ breast cancer cells leads to rapid mTOR signaling, which triggers cap-dependent translation of Mcl-1 and contributes to resistance to Bcl-2/Bcl-xL inhibitors, but combined treatment with Mcl-1 or mTOR inhibitors enhances apoptosis and reduces tumor growth. [Read the Full Post]

Exposure-Response Analysis to Assess the Concentration-QTc Relationship of Iberdomide

241 | Aug 24 2023

The study suggests that iberdomide, at its maximum plasma concentration, does not have a clinically relevant effect on QT interval prolongation. [Read the Full Post]

A Phase 1, Multicenter, Open-Label Study to Evaluate the Pharmacokinetics of Iberdomide in Subjects with Mild, Moderate, or Severe Hepatic Impairment Compared with Healthy Subjects

252 | Aug 24 2023

The phase 1 study demonstrated that hepatic impairment had no clinically significant impact on the pharmacokinetics of iberdomide, supporting the conclusion that no dose adjustment is necessary for patients with hepatic impairment. [Read the Full Post]

Oxidative stress enhances the therapeutic action of a respiratory inhibitor in MYC-driven lymphoma

187 | Aug 23 2023

The combination of complex I inhibition and high-dose ascorbate demonstrates synergistic anticancer effects in MYC-driven cancers, such as high-grade lymphomas, by inducing oxidative stress and disrupting redox homeostasis. [Read the Full Post]

Precision Targeted Therapy with BLU-667 for RET-Driven Cancers

201 | Aug 22 2023

BLU-667, a highly potent and selective RET inhibitor, has demonstrated significant inhibition of RET signaling and induced durable clinical responses in patients with RET-altered NSCLC and MTC, validating its potential as a targeted therapy for these cancers. [Read the Full Post]

The CDK7 inhibitor CT7001 (Samuraciclib) targets proliferation pathways to inhibit advanced prostate cancer

246 | Aug 22 2023

The study demonstrates that the CDK7 inhibitor CT7001 shows promising antitumor efficacy in castration-resistant prostate cancer (CRPC), inhibiting cell proliferation, inducing apoptosis, and suppressing androgen receptor (AR) signaling, both as a monotherapy and in combination with the antiandrogen enzalutamide. [Read the Full Post]

Pulsatilla Saponins Inhibit Experimental Lung Metastasis of Melanoma via Targeting STAT6-Mediated M2 Macrophages Polarization

224 | Aug 21 2023

Pulsatilla saponins derived from Pulsatilla chinensis effectively suppress tumor progression by inhibiting the polarization of M2 macrophages through the STAT6 signaling pathway, revealing a novel mechanism for their anti-tumor activity. [Read the Full Post]

Molecular basis and targeted therapy in thyroid cancer: Progress and opportunities

276 | Aug 21 2023

Thyroid cancer management has advanced with the development of targeted therapies, such as multi-tyrosine kinase inhibitors and immune checkpoint inhibitors, offering potential options for controlling tumor progression and addressing resistance mechanisms. [Read the Full Post]

Transforming growth factor-β-activated kinase 1 (TAK1) mediates chronic pain and cytokine production in mouse models of inflammatory, neuropathic, and primary pain

236 | Aug 19 2023

The study demonstrated that inhibiting TAK1 with the small molecule inhibitor takinib alleviated pain and inflammation in various models of chronic pain, indicating its potential as a novel drug target for the treatment of different types of chronic pain syndromes. [Read the Full Post]

Development and Efficacy of an Orally Bioavailable Selective TAK1 Inhibitor for the Treatment of Inflammatory Arthritis

288 | Aug 19 2023

HS-276, a potent and selective orally bioavailable TAK1 inhibitor, shows promise in inhibiting TNF-mediated cytokine profiles and attenuating arthritic-like symptoms in a mouse model of inflammatory rheumatoid arthritis, suggesting it as a potential alternative to current biologic-based therapies. [Read the Full Post]

β-catenin ameliorates myocardial infarction by preventing YAP-associated apoptosis

352 | Aug 18 2023

The study demonstrated that upregulation of β-catenin in myocardial infarction (MI) reduces cardiac tissue damage and cardiomyocyte apoptosis, and this effect is mediated, at least in part, through the reactivation of Yes-Associated Protein (YAP). [Read the Full Post]

Necrostatin-1 attenuates delayed paraplegia after transient spinal cord ischemia in rabbits by inhibiting the upregulation of receptor-interacting protein kinase 1 and 3

237 | Aug 17 2023

Nec-1, a necroptosis inhibitor, effectively reduces delayed motor neuron death and mitigates delayed paraplegia following transient spinal cord ischemia in rabbits, primarily by selectively inhibiting necroptosis while minimally affecting apoptosis. [Read the Full Post]

Preclinical investigations of the efficacy of the glutaminase inhibitor CB-839 alone and in combinations in chronic lymphocytic leukemia

104 | Aug 17 2023

The study findings indicate that CB-839, a GLS-1 inhibitor, has limited efficacy as a standalone treatment for CLL and shows limited synergy when combined with commonly used CLL drugs. [Read the Full Post]

Dichloroacetic acid and rapamycin synergistically inhibit tumor progression

502 | Aug 15 2023

Rapamycin treatment leads to the inactivation of the pyruvate dehydrogenase complex (PDHc) through mTOR signaling inhibition, reducing cancer cells' response to rapamycin, while reactivating PDHc with dichloroacetic acid (DCA) enhances their susceptibility to rapamycin treatment. [Read the Full Post]

In Vitro/In Vivo Translation of Synergistic Combination of MDM2 and MEK Inhibitors in Melanoma Using PBPK/PD Modelling: Part III

282 | Aug 14 2023

The study utilized PBPK/PD modeling and virtual clinical trial simulations to evaluate the potential efficacy of the siremadlin and trametinib combination as a therapy for melanoma, based on in vitro studies and in vivo extrapolation. [Read the Full Post]

Co-Targeting of MDM2 and CDK4/6 with Siremadlin and Ribociclib for the Treatment of Patients with Well-Differentiated or Dedifferentiated Liposarcoma: Results from a Proof-of-Concept, Phase Ib Study

204 | Aug 14 2023

The combination of siremadlin and ribociclib showed manageable toxicity and early signs of antitumor activity in patients with advanced well-differentiated or dedifferentiated liposarcoma. [Read the Full Post]

Safety and efficacy of single insertion accelerated MR-image guided brachytherapy following chemo-radiation in locally advanced cervix cancer: modifying our EMBRACE during the COVID pandemic

102 | Aug 13 2023

The study showed that a modified image-guided adaptive brachytherapy protocol (mIGABT) was effective, cost-saving, and well-tolerated in treating locally advanced cervical cancer during the COVID-19 pandemic. [Read the Full Post]

CSF-1R inhibitor, pexidartinib, sensitizes esophageal adenocarcinoma to PD-1 immune checkpoint blockade in a rat model

0 | Aug 11 2023

This study demonstrates that pexidartinib, a CSF-1R inhibitor, alone or in combination with a PD-1 inhibitor, shows significant tumor shrinkage and enhanced antitumor immune responses in a rat model of esophageal adenocarcinoma, providing a promising combinatorial strategy for future clinical approaches. [Read the Full Post]

Downregulated XBP-1 Rescues Cerebral Ischemia/Reperfusion Injury-Induced Pyroptosis via the NLRP3/Caspase-1/GSDMD Axis

229 | Aug 08 2023

Downregulation of XBP-1 inhibits pyroptosis through the NLRP3/Caspase-1/GSDMD pathway, providing neuronal protection in the context of cerebral ischemia/reperfusion injury. [Read the Full Post]

A phase II trial of GSK2256098 and trametinib in patients with advanced pancreatic ductal adenocarcinoma

312 | Aug 08 2023

The combination of GSK2256098 and trametinib did not show significant clinical benefit in advanced pancreatic ductal adenocarcinoma (PDAC) patients, with short median progression-free survival and overall survival observed in the study. [Read the Full Post]

Cellular senescence in the response of HR+ breast cancer to radiotherapy and CDK4/6 inhibitors

403 | Aug 06 2023

The study findings suggest that the inferiority of CDK4/6 inhibition followed by radiation therapy (P→RT) compared to radiation therapy followed by CDK4/6 inhibition (RT→P) in preclinical models of HR+ breast cancer may be partially attributed to the differential accumulation of senescent cells in the tumor microenvironment. [Read the Full Post]

A PDX model combined with CD-DST assay to evaluate the antitumor properties of KRpep-2d and oxaliplatin in KRAS (G12D) mutant colorectal cancer

240 | Aug 06 2023

The combination of patient-derived xenograft (PDX) models and the collagen gel droplet embedded culture drug sensitivity test (CD-DST) offers a comprehensive and feasible approach for evaluating the antitumor properties of compounds, as demonstrated by the significant inhibitory effects of oxaliplatin but lack of effectiveness of KRpep-2d in both tests. [Read the Full Post]

Lyso-globotriaosylsphingosine induces endothelial dysfunction via autophagy-dependent regulation of necroptosis

115 | Aug 05 2023

Lyso-Gb3 induces necroptosis via autophagy and contributes to endothelial dysfunction in Fabry disease. [Read the Full Post]

BMP-1-induced GBA1 nuclear accumulation provokes CCN2 mRNA expression via importin-β-mediated nucleocytoplasmic pathway

155 | Aug 03 2023

The study demonstrated that bone morphogenetic protein-1 (BMP-1) promotes the nuclear accumulation of glucosylceramidase (GBA1) by reducing α2,6-sialylation, which subsequently affects the expression of cellular communication network factor 2 (CCN2) and provides insights into the role of the BMP-1-GBA1-CCN2 axis in dental and craniofacial diseases. [Read the Full Post]

Effects of Hypolipidemic Drugs on Psoriasis

340 | Aug 02 2023

The systematic review of 41 original articles assessed the effect of different hypolipidemic treatments on the course of psoriasis, highlighting the potential benefits of statins, fibrates, glitazones, and GLP-1 receptor agonists in improving lipid abnormalities associated with the disease. [Read the Full Post]

Bioinformatics screening of colorectal-cancer causing molecular signatures through gene expression profiles to discover therapeutic targets and candidate agents

348 | Aug 02 2023

This study utilized integrated statistics and bioinformatics approaches to identify key genes, transcriptional regulators, and candidate therapeutic agents for colorectal cancer (CRC), highlighting their potential diagnostic, prognostic, and therapeutic significance. [Read the Full Post]

Mivebresib alleviates systemic lupus erythematosus-associated diffuse alveolar hemorrhage via inhibiting infiltration of monocytes and M1 polarization of macrophages

98 | Aug 01 2023

Mivebresib, a BRD4 inhibitor, demonstrates potential as a therapeutic option for diffuse alveolar hemorrhage associated with systemic lupus erythematosus by inhibiting macrophage polarization and inflammatory cell infiltration. [Read the Full Post]

Loss of VOPP1 Contributes to BET Inhibitor Acquired Resistance in Non-Small Cell Lung Cancer Cells

184 | Aug 01 2023

This study demonstrates that the loss of VOPP1 leads to the gain of BCL-2, resulting in resistance to BET inhibitors in non-small cell lung cancer, and suggests that combination therapy with BET inhibitors and BCL-2 inhibitors may overcome this resistance. [Read the Full Post]

Successful Treatment and Retreatment With Erdafitinib for a Patient With FGFR3-TACC3 Fusion Squamous NSCLC: A Case Report

424 | Aug 01 2023

This case report demonstrates the potential efficacy of erdafitinib, an FGFR inhibitor, in achieving disease control and radiographic response in a patient with FGFR3-TACC3 fusion squamous NSCLC, suggesting the need for further investigation and expanding therapeutic options. [Read the Full Post]

Current scenario of pyrazole hybrids with in vivo therapeutic potential against cancers

388 | Aug 01 2023

This review provides a comprehensive overview of the potential of pyrazole hybrids as anticancer agents, summarizing their mechanisms of action, toxicity, and pharmacokinetics, with the aim of facilitating the rational exploitation and development of more effective candidates for cancer therapy. [Read the Full Post]

Phase 1 pilot study of RRx-001 + nivolumab in patients with advanced metastatic cancer (PRIMETIME)

146 | Aug 01 2023

The phase 1 pilot study demonstrated that the combination of RRx-001 and nivolumab was well-tolerated, showed preliminary anti-cancer activity, and further clinical trials with this combination are warranted. [Read the Full Post]

The effect of the ATM inhibitor AZD0156 on the radiosensitivity of human breast cancer and lung fibroblast cells

258 | Jul 31 2023

The combination of irradiation and AZD0156 showed enhanced efficacy in inducing cell cycle arrest and reducing clonogenic survival in breast cancer cells, while having minimal effect on fibroblast cells. [Read the Full Post]

UBA1 inhibition contributes radiosensitization of glioblastoma cells via blocking DNA damage repair

298 | Jul 29 2023

The study demonstrated that the UBA1 inhibitor TAK-243, in combination with ionizing radiation, effectively inhibited GBM cell proliferation, impaired DNA double-strand break repair, and increased apoptosis, providing a potential therapeutic approach to enhance the radiation sensitivity of GBM. [Read the Full Post]

Proteasomal pathway inhibition as a potential therapy for NF2-associated meningioma and schwannoma

242 | Jul 29 2023

This study highlights the potential of proteasome pathway inhibitors, specifically ixazomib and TAK-243, as novel and promising therapies for NF2-associated tumors, demonstrating efficacy in preclinical models and laying the groundwork for future clinical investigations. [Read the Full Post]

Thioredoxin-interacting protein deficiency protects against severe acute pancreatitis by suppressing apoptosis signal-regulating kinase 1

254 | Jul 28 2023

TXNIP, a protein involved in redox reactions and inflammatory responses, plays a significant role in acute pancreatitis by regulating the activation of JNK/p38 pathways and influencing oxidative stress, suggesting its potential as a therapeutic target for protecting against severe acute pancreatitis. [Read the Full Post]

Timely expression of PGAM5 and its cleavage control mitochondrial homeostasis during neurite re-growth after traumatic brain injury

251 | Jul 27 2023

The study reveals that phosphoglycerate mutase 5 (PGAM5) acts as a mitochondrial sensor in traumatic brain injury (TBI), promoting mitophagy and subsequent cleavage by PARL, leading to increased mitochondrial transcription factor A (TFAM) expression and functional recovery. [Read the Full Post]

pH-sensitive smart indicators based on cellulose and different natural pigments for tracing kimchi ripening stages

688 | Jul 27 2023

The study found that cellulose-based pH-sensitive indicators loaded with natural pigments showed more pronounced color changes in response to lactic acid and pH variations, with alkalized indicators being particularly effective for monitoring the fermentation process of acidic foods such as kimchi. [Read the Full Post]

The Combination of Sinusoidal Perfusion Enhancement and Apoptosis Inhibition by Riociguat Plus a Galactose-PEGylated Bilirubin Multiplexing Nanomedicine Ameliorates Liver Fibrosis Progression

207 | Jul 27 2023

The study describes a novel strategy for treating liver fibrosis by combining sinusoidal perfusion enhancement with apoptosis inhibition using riociguat and a hepatocyte-targeting galactose-PEGylated bilirubin nanomedicine (Sel@GBRNPs). [Read the Full Post]

MAPK-interacting kinases inhibition by eFT508 overcomes chemoresistance in preclinical model of osteosarcoma

636 | Jul 26 2023

The study highlights the therapeutic potential of eFT508, a selective inhibitor of MNK1/2, alone and in combination with paclitaxel, as a promising treatment for osteosarcoma by inhibiting tumor growth and demonstrating selectivity and synergistic effects. [Read the Full Post]

Treatment with eFT-508 increases chemosensitivity in breast cancer cells by modulating the tumor microenvironment

542 | Jul 26 2023

Tomivosertib (eFT-508) demonstrates promising efficacy both in vitro and in vivo, including synergistic effects with adriamycin, suggesting its potential as a more efficacious therapeutic option for patients with triple-negative breast cancer (TNBC). [Read the Full Post]

The mRNA-binding protein DDX3 mediates TGF-β1 upregulation of translation and promotes pulmonary fibrosis

214 | Jul 25 2023

Inhibiting the mRNA-binding protein DDX3, which mediates TGF-β1 upregulation of translation, shows promise in reducing pulmonary fibrosis and associated inflammation in experimental models. [Read the Full Post]

Targeting NRF2 uncovered an intrinsic susceptibility of acute myeloid leukemia cells to ferroptosis

93 | Jul 25 2023

Simultaneous inhibition of NRF2 and GPX4 shows promise as a synergistic combination therapy targeting ferroptosis and overcoming drug resistance in acute myeloid leukemia (AML). [Read the Full Post]

Combining ReACp53 with Carboplatin to Target High-Grade Serous Ovarian Cancers

123 | Jul 22 2023

The combination of ReACp53 and carboplatin has shown promising synergistic effects in targeting high-grade serous ovarian carcinomas, potentially offering a new therapeutic strategy for this aggressive subtype of ovarian cancer. [Read the Full Post]

Treating colorectal peritoneal metastases with an injectable cytostatic loaded supramolecular hydrogel in a rodent animal model

277 | Jul 21 2023

The experimental study demonstrated that treatment of peritoneal metastases with a supramolecular hydrogel loaded with mitomycin C (MMC) significantly improved overall survival compared to treatment with free MMC alone, suggesting the potential of this drug delivery system for enhancing therapeutic efficacy. [Read the Full Post]

Oncogenic KRAS G12C: Kinetic and redox characterization of covalent inhibition

212 | Jul 21 2023

The recent study reveals that the C12 thiol in KRASG12C exhibits a depressed pKa and susceptibility to chemical ligation, as well as oxidation, providing insights for drug discovery and indicating the occurrence of unknown biological consequences. [Read the Full Post]

Proof of concept for poor inhibitor binding and efficient formation of covalent adducts of KRASG12C and ARS compounds

288 | Jul 21 2023

This computational study provides a comprehensive understanding of the reaction mechanism and kinetic constants involved in the covalent binding of ARS-853 to the KRASG12C·GDP complex, offering insights into the design of selective covalent inhibitors for challenging RAS-like proteins. [Read the Full Post]

Extracellular Release of Citrullinated Vimentin Directly Acts on Osteoclasts to Promote Bone Resorption in a Mouse Model of Periodontitis

300 | Jul 20 2023

The release of citrullinated vimentin (CV) promotes osteoclastogenesis and bone resorption in periodontitis, suggesting a potential shared pathogenesis with rheumatoid arthritis. [Read the Full Post]

5-FU mediated depletion of myeloid suppressor cells enhances T-cell infiltration and anti-tumor response in immunotherapy-resistant lung tumor

488 | Jul 19 2023

Depletion of MDSCs using low-dose 5-fluorouracil (5-FU) chemotherapy showed significant anti-tumor effects by increasing the infiltration of CD8+ cytotoxic T-cells in a cold tumor model of Lewis Lung Carcinoma (LLC). [Read the Full Post]

Chemical screen identifies shikonin as a broad DNA damage response inhibitor that enhances chemotherapy through inhibiting ATM and ATR

204 | Jul 17 2023

Shikonin, a recently identified inhibitor of the DNA damage response (DDR), has been found to suppress DDR activation by targeting ATM and ATRIP, leading to enhanced anti-cancer effects of chemotherapy, making it a potential candidate for chemotherapy sensitization. [Read the Full Post]

Hexavalent chromium disrupts the skin barrier by targeting ROS-mediated mitochondrial pathway apoptosis in keratinocytes

212 | Jul 17 2023

This study demonstrates that hexavalent chromium (Cr(VI)) exposure leads to skin deterioration, hemorrhaging, collagen fiber layer thinning, impaired membrane integrity, and apoptosis primarily targeting keratinocytes, highlighting the importance of apoptosis and ROS-mediated mitochondrial pathway in Cr(VI)-induced skin barrier injury. [Read the Full Post]

A Point Mutation at C151 of Keap1 of Mice Abrogates NRF2 Signaling, Cytoprotection In Vitro and Hepatoprotection In Vivo by Bardoxolone Methyl (CDDO-Me)

423 | Jul 16 2023

The mutation of the KEAP1 cysteine 151 sensor in mouse models abrogates the induction of NRF2 signaling and the subsequent cytoprotective actions of bardoxolone methyl (CDDO-Me), emphasizing its crucial role in mediating the drug's therapeutic effects. [Read the Full Post]

Venetoclax Penetrates the Blood Brain Barrier: A Pharmacokinetic Analysis in Pediatric Leukemia Patients

267 | Jul 15 2023

The results of a Phase 1 study in pediatric patients with relapsed or refractory malignancies indicate that venetoclax can penetrate the central nervous system, with measurable concentrations in the cerebrospinal fluid, and its presence correlates with improved resolution of central nervous system involvement. [Read the Full Post]

A comparative analysis to determine the optimum histone deacetylase inhibitors and administration route for improving survival and organ injury in rats after hemorrhagic shock

0 | Jul 15 2023

The study found that intravenous administration of histone deacetylase inhibitors (HDACIs) was more effective than intraperitoneal administration, and both nonselective and isoform-specific HDACIs showed similar effects in improving survival and reducing histopathological damage, apoptosis, and inflammation in rats with hemorrhagic shock. [Read the Full Post]

Activity and safety of first-line treatments for advanced melanoma: A network meta-analysis

398 | Jul 14 2023

The systematic review and network meta-analysis revealed that relatlimab/nivolumab demonstrated similar progression-free survival and overall response rate to ipilimumab/nivolumab in the first-line treatment of advanced melanoma, with a potential advantage of a better safety profile. [Read the Full Post]

Nirogacestat, a γ-Secretase Inhibitor for Desmoid Tumors

214 | Jul 12 2023

The phase 3 clinical trial showed that nirogacestat, an oral γ-secretase inhibitor, significantly improved progression-free survival, objective response rates, and patient-reported outcomes while presenting common but mostly low-grade adverse events in adults with progressing desmoid tumors. [Read the Full Post]

Timed Notch Inhibition Drives Photoreceptor Fate Specification in Human Retinal Organoids

401 | Jul 12 2023

In this study, the researchers demonstrated that timing the inhibition of the Notch signaling pathway in human retinal organoids can enhance and synchronize the differentiation of photoreceptor cells, potentially leading to an enriched population of early cone or rod photoreceptors for transplantation therapies in vision loss disorders. [Read the Full Post]

A Phase I Study to Investigate the Safety, Tolerability and Pharmacokinetics of Napabucasin Combined with Sorafenib in Japanese Patients with Unresectable Hepatocellular Carcinoma

252 | Jul 10 2023

This phase I study in Japanese patients with unresectable hepatocellular carcinoma (HCC) demonstrated that the combination of napabucasin and sorafenib showed promising preliminary antitumor activity with manageable side effects. [Read the Full Post]

PIM Kinases in Multiple Myeloma

246 | Jul 10 2023

PIM kinase inhibitors show promise as a potential treatment for multiple myeloma, and their combination with other targeted agents, including immunomodulatory drugs, holds great potential for improving patient outcomes. [Read the Full Post]

PIM Kinase as an Executional Target in Cancer

385 | Jul 10 2023

PIM kinases, including PIM1, PIM2, and PIM3, are oncogenes that promote cell survival and cell cycle progression in various cancers, and the development of PIM kinase inhibitors shows promise in targeting these pathways for the treatment of human cancer. [Read the Full Post]

Apoptotic cell death in disease-Current understanding of the NCCD 2023

552 | Jul 09 2023

The Nomenclature Committee on Cell Death (NCCD) critically summarizes the extensive pre-clinical literature linking the core apoptotic apparatus to organismal homeostasis in various disease contexts, highlighting its role in both disease etiology and potential therapeutic interventions. [Read the Full Post]

Case Report: Identification of a novel NTRK3-AJUBA fusion co-existing with ETV6-NTRK3 fusion in papillary thyroid carcinoma

353 | Jul 08 2023

This study reports the identification of a novel NTRK3-AJUBA fusion co-existing with a known ETV6-NTRK3 fusion in thyroid cancer, expanding the spectrum of translocation partners and highlighting the importance of further investigation regarding the impact of dual NTRK3 fusion on TRK inhibitor therapy and prognosis. [Read the Full Post]

Larotrectinib versus historical standard of care in patients with infantile fibrosarcoma: protocol of EPI-VITRAKVI

355 | Jul 08 2023

The EPI VITRAKVI study is a retrospective study that compares the time to medical treatment failure between larotrectinib and chemotherapy in patients with infantile fibrosarcoma using external historical controls and adjusting for potential confounding using the Inverse Probability of Treatment Weighting method. [Read the Full Post]

A retrospective cohort study on the efficacy and safety for combination therapy of immunotherapy, targeted agent, and chemotherapy versus immunochemotherapy or chemotherapy alone in the first-line treatment of advanced biliary tract carcinoma

266 | Jul 05 2023

This retrospective study suggests that combining anti-PD-1/PD-L1 immunotherapy with anlotinib and gemcitabine shows promising efficacy and an acceptable safety profile in patients with advanced biliary tract carcinoma. [Read the Full Post]

Fangchinoline Exerts Anticancer Effects on Colorectal Cancer Cells by Evoking Cell Apoptosis via Endoplasmic Reticulum Stress

311 | Jul 04 2023

Fangchinoline (FAN) induces apoptosis in human colorectal cancer cells by activating endoplasmic reticulum stress through the upregulation of ER stress-related proteins and the involvement of the CHOP pathway. [Read the Full Post]

Targeting glutamine metabolism with photodynamic immunotherapy for metastatic tumor eradication

295 | Jul 04 2023

The study presents a novel photodynamic immunostimulant, BVC, that reprograms glutamine metabolism and combines immune checkpoint blockade therapy with photodynamic therapy to enhance immune recognition and prevent immune escape for the eradication of metastatic tumors. [Read the Full Post]

Design, synthesis, and evaluation of PD-1/PD-L1 small-molecule inhibitors bearing a rigid indane scaffold

304 | Jul 04 2023

Compound D3, a novel small-molecule inhibitor of the PD-1/PD-L1 interaction, demonstrates potent inhibitory activity and immune-enhancing effects, making it a promising candidate for further development in immunotherapy. [Read the Full Post]

Proof of concept nanotechnological approach to in vitro targeting of malignant melanoma for enhanced immune checkpoint inhibition

289 | Jul 04 2023

The study demonstrates that the delivery of a small molecule inhibitor of the PD-1/PD-L1 pathway using nanodiamond-based nanoparticles enhances immune cell stimulation and promotes stronger interactions between immune cells and melanoma cells, suggesting potential for improved melanoma therapy. [Read the Full Post]

Combined inhibition of XIAP and autophagy induces apoptosis and differentiation in acute myeloid leukaemia

217 | Jul 03 2023

In acute myeloid leukemia (AML), the inhibition of X-linked inhibitor of apoptosis (XIAP) induces autophagy, apoptosis, and differentiation, and combining XIAP inhibition with autophagy inhibition shows promise as a therapeutic strategy for AML. [Read the Full Post]

Prosaposin PS18 reduces dopaminergic neurodegeneration in a 6-hydroxydopamine rat model of Parkinson's disease

135 | Jul 03 2023

PS18, a peptide derived from prosaposin, exhibits neuroprotective effects by reducing dopaminergic neuronal loss, apoptosis, and endoplasmic reticulum stress in cellular and animal models of Parkinson's disease. [Read the Full Post]

AXL Inhibitor TP-0903 Reduces Metastasis and Therapy Resistance in Pancreatic Cancer

230 | Jul 02 2023

The study demonstrates that the AXL inhibitor TP-0903 exhibits anti-metastatic, antitumor effects, and sensitizes pancreatic ductal adenocarcinoma to therapy, potentially providing a new treatment strategy for pancreatic cancer. [Read the Full Post]

Repurposing Axl Kinase Inhibitors for the Treatment of Respiratory Syncytial Virus Infection

131 | Jul 02 2023

In this study, Axl kinase inhibitors demonstrated efficacy in reducing RSV infection, ameliorating pulmonary pathology, and promoting the expression of interferon-stimulated genes, suggesting their potential as broad-spectrum antiviral therapeutics. [Read the Full Post]

Runx3-overexpression cooperates with ex vivo AKT inhibition to generate receptor-engineered T cells with better persistence, tumor-residency, and antitumor ability

313 | Jun 28 2023

Combining Runx3 overexpression with ex vivo AKT inhibition generates CAR-T cells with both tissue-resident and central memory characteristics, enhancing their persistence, cytotoxic potential, and tumor-residency ability for the treatment of solid tumors. [Read the Full Post]

Celastrol inhibits necroptosis by attenuating the RIPK1/RIPK3/MLKL pathway and confers protection against acute pancreatitis in mice

0 | Jun 27 2023

Celastrol demonstrates potential as a therapeutic agent for inhibiting necroptosis and reducing the severity of necroptotic-related diseases such as pancreatitis [Read the Full Post]

Therapeutic Targets in Myelodysplastic Neoplasms: Beyond Hypomethylating Agents

273 | Jun 24 2023

This review discusses the current management strategies and promising novel targeted therapies under investigation for the treatment of high-risk myelodysplastic neoplasms (MDS), highlighting the need for alternative options due to the limitations of allogeneic hematopoietic stem cell transplantation and the challenges associated with hypomethylating agents (HMAs). [Read the Full Post]

Eprenetapopt combined with venetoclax and azacitidine in TP53-mutated acute myeloid leukaemia: a phase 1, dose-finding and expansion study

296 | Jun 24 2023

The combination of eprenetapopt and venetoclax with azacitidine showed promising activity and an acceptable safety profile in patients with TP53-mutated acute myeloid leukemia, supporting further evaluation of this combination as a frontline treatment option. [Read the Full Post]

JAK/BCL2 inhibition acts synergistically with LSD1 inhibitors to selectively target ETP-ALL

0 | Jun 22 2023

The combination of a LSD1 inhibitor with a JAK/STAT pathway inhibitor or a BCL2 inhibitor reverses resistance and efficiently inhibits the growth of ETP-ALL cells, suggesting a potential novel combination therapy for ETP-ALL patients. [Read the Full Post]

The role of small GTPases in bisphenol AF-induced multinucleation in comparison with dibutyl phthalate in the male germ cells

352 | Jun 22 2023

This study demonstrates that BPAF exposure leads to cytotoxicity, increased multinucleation in mouse spermatogonia cells, and highlights the involvement of small GTPase-signaling pathways in mediating these effects, providing insights into the genotoxic mechanisms of BPA analogs on male germ cells. [Read the Full Post]

Molecular Docking, Molecular Dynamics Simulations, and Free Energy Calculation Insights into the Binding Mechanism between VS-4718 and Focal Adhesion Kinase

405 | Jun 21 2023

This research work elucidates the binding mechanism between VS-4718 and focal adhesion kinase (FAK), providing valuable insights for optimizing the design of FAK inhibitors in cancer therapy. [Read the Full Post]

Effect of insulin-like growth factor system on luteinising angiogenesis

193 | Jun 21 2023

This study found that while exogenous IGF1 and IGF2 had limited effects on luteinizing follicular angiogenesis and progesterone production, inhibiting the IGF1 receptor signaling significantly reduced endothelial cell growth and progesterone concentration, indicating its crucial role in these processes. [Read the Full Post]

Three dimensional models of dedifferentiated liposarcoma cell lines: scaffold-based and scaffold-free approaches

357 | Jun 20 2023

This study aimed to establish 3D cell culture models of liposarcomas using different methods, observing distinct structural differences and demonstrating the potential of these models to provide new insights into efficacy and toxicity, serving as an important step in the pre-clinical phase prior to clinical trials. [Read the Full Post]

Exploring MicroRNA and Exosome Involvement in Malignant Pleural Mesothelioma Drug Response

285 | Jun 20 2023

The study revealed that transfection of specific microRNAs enhanced the sensitivity of malignant pleural mesothelioma cells to chemotherapy and a FAK inhibitor, while also demonstrating that YM155-resistant cells showed increased exosome secretion and upregulation of drug transporter genes ABCA6 and ABCA10, which correlated with poor sensitivity to YM155. [Read the Full Post]

Therapeutic potential of CDK11 in cancer

380 | Jun 19 2023

The discovery that CDK11 regulates pre-mRNA splicing and the identification of OTS964 as a CDK11 inhibitor with antiproliferative properties highlight the therapeutic potential of targeting CDK11 in cancer treatment. [Read the Full Post]

MI-773, a breaker of the MDM2/p53 axis, exhibits anticancer effects in neuroblastoma via downregulation of INSM1

264 | Jun 19 2023

MI-773, a specific antagonist of MDM2, disrupts the MDM2/p53 axis, leading to suppressed proliferation, induced apoptosis, and cell cycle arrest in neuroblastoma cells, suggesting its potential as a novel treatment strategy for this pediatric malignancy. [Read the Full Post]

Abrogation of Cellular Senescence Induced by Temozolomide in Glioblastoma Cells: Search for Senolytics

185 | Jun 17 2023

Targeting senescent cells with senolytic drugs, such as ABT-737, navitoclax, chloroquine, ATMi, ATRi, BV-6, PX-866, fisetin, and artesunate, may improve the outcome of glioblastoma therapy by preventing recurrences and reducing tumor inflammation. [Read the Full Post]

From preclinical efficacy to 2022 updated CROWN trial, lorlatinib is the preferred 1st-line treatment of advanced ALK+ NSCLC

358 | Jun 14 2023

The data from the CROWN trial, including the sustained and durable responses, favorable 3-year progression-free survival rates, and manageable CNS adverse events, strongly support lorlatinib as the preferred treatment for advanced ALK+ NSCLC. [Read the Full Post]

TLR4 is one of the receptors for Chikungunya virus envelope protein E2 and regulates virus induced pro-inflammatory responses in host macrophages

290 | Jun 11 2023

TLR4 inhibition using TAK-242 reduces CHIKV infection by decreasing viral copy number, CHIKV-E2 protein levels, and pro-inflammatory responses, highlighting TLR4 as a novel receptor involved in viral entry and modulation of infection-induced inflammation. [Read the Full Post]

Liver X Receptor Activation Attenuates Oxysterol-Induced Inflammatory Responses in Fetoplacental Endothelial Cells

253 | Jun 11 2023

The study suggests that 7-ketocholesterol and 7β-hydroxycholesterol induce placental inflammation in gestational diabetes mellitus by activating TLR-4 and that pharmacological activation of LXR can attenuate the pro-inflammatory effects of these oxysterols in fetoplacental endothelial cells. [Read the Full Post]

Systemic treatment in patients with Child-Pugh B liver dysfunction and advanced hepatocellular carcinoma

348 | Jun 07 2023

Hepatocellular carcinoma (HCC) is a major cause of death among patients with liver cirrhosis, and the limited efficacy of available therapies in patients with moderate liver dysfunction highlights the need for improved treatment algorithms and novel therapies specifically designed for this patient population. [Read the Full Post]

Anisomycin inhibits Coxsackievirus B replication by promoting the lysosomal degradation of eEF1A1

335 | Jun 07 2023

Anisomycin has been found to inhibit CVB type 3 infection and reduce viral replication by promoting lysosomal degradation of eEF1A1, which makes it a potential antiviral candidate for the treatment of CVB infection. [Read the Full Post]

Phytochemical characterization, antioxidant activity and antihypertensive evaluation of Ocimum basilicum L. in l-NAME induced hypertensive rats and its correlation analysis

322 | Jun 05 2023

The study found that Ocimum basilicum Linn. leaves extracts have potential as antihypertensive drugs due to their bioactive metabolites, with phenolic compounds playing a role in inhibiting l-Name induced hypertension and flavonoids contributing to antioxidant activities. [Read the Full Post]

A covalent inhibitor of K-Ras(G12C) induces MHC class I presentation of haptenated peptide neoepitopes targetable by immunotherapy

251 | Jun 04 2023

The study demonstrates that covalent drugs that alkylate mutated residues on oncoproteins can generate unique MHC-I-restricted neoantigens, which can be targeted with a bispecific T cell engager construct to elicit a cytotoxic T cell response against cancer cells, including those resistant to direct inhibition. [Read the Full Post]

Blockade of STAT3/IL-4 overcomes EGFR T790M-cis-L792F-induced resistance to osimertinib via suppressing M2 macrophages polarization

144 | Jun 04 2023

The study suggests that targeting the EGFR T790M-cis-L792F/STAT3 Tyr705/IL-4 pathway could be a potential strategy to suppress osimertinib resistance in NSCLC. [Read the Full Post]

Inhibitor of Apoptosis Proteins Antagonist Induces T-cell Proliferation after Cross-Presentation by Dendritic Cells

133 | Jun 04 2023

Researchers have identified AZD5582 as a compound that enhances dendritic cell cross-presentation of tumor antigens, leading to an increased frequency of systemic tumor antigen-specific CD8+ T cells, which could improve the clinical benefit of immune checkpoint blockade in patients who are unlikely to respond. [Read the Full Post]

KDELC2 Upregulates Glioblastoma Angiogenesis via Reactive Oxygen Species Activation and Tumor-Associated Macrophage Proliferation

331 | Jun 03 2023

This study demonstrates that KDELC2 promotes glioblastoma angiogenesis via the activation of multiple pathways, including NLRP3 inflammasome, autophagy, ER stress, and TAM polarization. [Read the Full Post]

NDUFS3 knockout cancer cells and molecular docking reveal specificity and mode of action of anti-cancer respiratory complex I inhibitors

398 | Jun 03 2023

This study highlights the need for cautious evaluation and dosage optimization of inhibitors targeting respiratory complex I in cancer treatment. [Read the Full Post]

Smad7 Is Highly Expressed in Human Degenerative Discs and Participates in IL-1 β-Induced Apoptosis of Rat AF Cells via the Mitochondria Pathway

136 | Jun 03 2023

Smad7 participates in IL-1β-induced apoptosis of rat annulus fibrosus cells via the mitochondria pathway and may be a potential target for the prevention and treatment of degenerative disc disease. [Read the Full Post]

Vaccines prevent reinduction of rheumatoid arthritis symptoms in collagen-induced arthritis mouse model

355 | Jun 02 2023

This study suggests that immune metabolic modulators such as paKG(PFK15 + bc2) microparticles may be a promising alternative or complementary treatment option for RA and paves the way for the development of flare-up mouse models and antigen-specific drug treatments. [Read the Full Post]

Loss of deubiquitylase USP2 triggers development of glioblastoma via TGF-β signaling

188 | Jun 01 2023

This study suggests that USP2 is a major regulator of the TGF-β signaling pathway in glioblastoma, and its loss leads to poor prognosis in patients, while DNMT3A inhibitor SGI-1027 could be a potential treatment by inducing USP2 expression and suppressing TGF-β signaling. [Read the Full Post]

Dieting reverses histone methylation and hypothalamic AgRP regulation in obese rats

216 | Jun 01 2023

The study suggests that KDM4D, a specific demethylase of residue H3K9, plays a key role in modulating the expression of AgRP, a key neuropeptide that regulates hunger response, and may offer a target to develop new treatments for obesity. [Read the Full Post]

Synergistic apoptotic effect of miR-183-5p and Polo-Like kinase 1 inhibitor NMS-P937 in breast cancer cells

103 | May 31 2023

This research study explores the role of miRNAs in breast cancer and their impact on breast cancer cells' response to PLK1 inhibition, with miR-183-5p targeting the PLK1 gene and enhancing the effectiveness of NMS-P937 in inducing apoptosis. [Read the Full Post]

Examining anti-inflammatory therapies in the prevention of cardiovascular events: protocol for a systematic review and network meta-analysis of randomised controlled trials

169 | May 30 2023

The proposed methodology for the systematic review appears appropriate for addressing the research question, with a comprehensive search strategy, independent review, network meta-analysis, and quality assessment tools. [Read the Full Post]

In vitro target validation and in vivo efficacy of p38 MAP kinase inhibition in established chronic collagen-induced arthritis model: a pre-clinical study

274 | May 30 2023

The study found that p38 MAPK inhibitors, GW856553X and GSK678361, effectively suppressed murine collagen-induced arthritis, indicating potential therapeutic value for the treatment of RA. [Read the Full Post]

Host-Erythrocytic Sphingosine-1-Phosphate Regulates Plasmodium Histone Deacetylase Activity and Exhibits Epigenetic Control over Cell Death and Differentiation

187 | May 28 2023

The study suggests that altering host S1P levels could dysregulate PfHDAC-1 activity and modulate the transcriptional patterns of genes associated with malaria parasite proliferation and virulence, offering a novel approach to combat malaria resistance to conventional antimalarial drugs. [Read the Full Post]

Protein kinase D1 promotes the survival of random-pattern skin flaps in rats

278 | May 28 2023

The study demonstrated that PKD1 improves skin flap survival by promoting angiogenesis, reducing oxidative stress, and inhibiting apoptosis and inflammation, suggesting it as a potential therapeutic target for flap failure treatment. [Read the Full Post]

Impact of setanaxib on quality of life outcomes in primary biliary cholangitis in a phase 2 randomized controlled trial

311 | May 27 2023

The study suggests that setanaxib may improve quality of life in patients with PBC, particularly for those with clinically significant fatigue. [Read the Full Post]

CD137 signaling aggravates myocardial ischemia-reperfusion injury by inhibiting mitophagy mediated NLRP3 inflammasome activation

215 | May 26 2023

CD137 signaling exacerbates myocardial ischemia-reperfusion injury by suppressing mitophagy and promoting NLRP3 inflammasome activation via increased mitochondrial ROS generation. [Read the Full Post]

Alteration of the tumor microenvironment by pharmacological inhibition of EZH2 in hepatocellular carcinoma

203 | May 26 2023

The study found that EZH2 inhibition with UNC1999 impaired HCC tumor growth but also altered the TME by decreasing interferon-γ+ CD8+ T cells and regulatory T cells and increasing myeloid-derived suppressor cells, and combination therapy with agents that reduce MDSCs may represent a potential novel therapeutic strategy for HCC. [Read the Full Post]

Long non-coding RNA HIF1A-As2 and MYC form a double-positive feedback loop to promote cell proliferation and metastasis in KRAS-driven non-small cell lung cancer

350 | May 25 2023

This passage describes a study on the role of lncRNA HIF1A-As2 in regulating the activation of KRAS in lung cancer and its potential as a therapeutic target. [Read the Full Post]

Apoptosis or Antiapoptosis? Interrupted Regulated Cell Death of Host Cells by Ascovirus Infection In Vitro

88 | May 21 2023

This study investigates the antiapoptotic capacity of ascovirus-infected insect cells and their biochemical characteristics during different stages of infection. [Read the Full Post]

Functional Assessment of Kinesin-7 CENP-E in Spermatocytes using In Vivo Inhibition, Immunofluorescence and Flow Cytometry

0 | May 21 2023

The article describes a practical and efficient in vivo inhibition method for kinesin-7 CENP-E in mouse spermatocytes via testicular injection, facilitating mechanistic studies of meiosis and potential clinical applications. [Read the Full Post]

Administration of an LXR agonist promotes atherosclerotic lesion remodelling in murine inflammatory arthritis

191 | May 20 2023

The study shows that the LXR agonist T0901317 improves cholesterol efflux and atherosclerotic lesion regression in murine arthritis, potentially offering therapeutic benefits for patients with rheumatoid arthritis and atherosclerotic cardiovascular disease. [Read the Full Post]

Kv1.3 blockade by ShK186 modulates CD4+ effector memory T-cell activity of patients with Granulomatosis with polyangiitis

321 | May 19 2023

The study suggests that Kv1.3 blockade using ShK-186 may be a potential treatment strategy for GPA by modulating the activity of CD4+TEM cells and reducing the production of pro-inflammatory cytokines, with less harmful side effects than current immunosuppressive regimens. [Read the Full Post]

Celastrol inhibits necroptosis by attenuating the RIPK1/RIPK3/MLKL pathway and confers protection against acute pancreatitis in mice

337 | May 18 2023

Celastrol has been found to inhibit necroptosis by attenuating the phosphorylation of RIPK1, RIPK3, and MLKL and mitochondrial dysfunction in in vitro models, and in a mouse model of acute pancreatitis, it significantly reduced the severity of the disease and decreased the phosphorylation of MLKL in pancreatic tissues. [Read the Full Post]

SMAC Mimetics Synergistically Cooperate with HDAC Inhibitors Enhancing TNF-α Autocrine Signaling

174 | May 18 2023

The combination of SMAC mimetics and HDAC inhibitors shows remarkable synergy in suppressing IAP proteins and restoring apoptotic pathways, providing a potential therapeutic strategy for recurrent ovarian cancer. [Read the Full Post]

PYCR1 promotes the malignant progression of lung cancer through the JAK-STAT3 signaling pathway via PRODH-dependent glutamine synthesize

247 | May 18 2023

PYCR1 has clinical significance in the diagnosis and prognosis of lung cancer, and its pro-tumorigenic role in lung cancer may be attributed to its regulation of the JAK-STAT3 signaling pathway and the metabolism link between proline and glutamine. [Read the Full Post]

Low gamma-butyrobetaine dioxygenase (BBOX1) expression as a prognostic biomarker in patients with clear cell renal cell carcinoma: a machine learning approach

186 | May 17 2023

This study found that low BBOX1 expression in clear cell renal cell carcinoma (RCC) patients is associated with poor prognosis, decreased CD8+ T cells, and increased neutrophils, and identified potential drugs, including midostaurin, that can inhibit RCC cells with low BBOX1 expression. [Read the Full Post]

Ocular adverse events associated with BRAF and MEK inhibitor combination therapy: a pharmacovigilance disproportionality analysis of the FDA adverse event reporting system

308 | May 17 2023

The authors conducted a retrospective study using FAERS data to investigate oAEs associated with three BRAF and MEK inhibitor combination therapies, identifying both previously reported and new oAEs and noting that oAE profiles varied across treatment regimens. [Read the Full Post]

ANCHOR CRC: Results From a Single-Arm, Phase II Study of Encorafenib Plus Binimetinib and Cetuximab in Previously Untreated BRAFV600E-Mutant Metastatic Colorectal Cancer

259 | May 17 2023

The ANCHOR CRC study showed that the first-line combination of encorafenib + binimetinib + cetuximab was effective and safe in treating BRAFV600E-mutated metastatic colorectal cancer patients with a locally assessed confirmed objective response rate of 47.4%. [Read the Full Post]

An Umpolung Approach to Acyclic 1,4-Dicarbonyl Amides via Photoredox-Generated Carbamoyl Radicals

427 | May 15 2023

This passage describes a method for the generation and reaction of carbamoyl radicals from oxamate salts followed by reaction with electron-poor olefins, which enables the mild and mass-efficient formation of 1,4-dicarbonyl products, supported by ab initio calculations, and designed to be environmentally friendly. [Read the Full Post]

Impact of SNPs, off-targets, and passive permeability on efficacy of BCL6 degrading drugs assigned by virtual screening and 3D-QSAR approach

103 | May 15 2023

The study utilized computational methods to identify potential BCL6 inhibitors from a library of approved drugs and highlighted the importance of considering off-target effects and membrane permeability in drug design and evaluation. [Read the Full Post]

Allosteric inhibition of HSP70 in collaboration with STUB1 augments enzalutamide efficacy in antiandrogen resistant prostate tumor and patient-derived models

190 | May 13 2023

The study suggests that targeting HSP70 using small-molecule inhibitors, in combination with ARSI drugs, could be a promising approach to overcome resistance to ARSI in advanced prostate cancer. [Read the Full Post]

Molecular Design of 68Ga- and 89Zr-Labeled Anticalin Radioligands for PET-Imaging of PSMA-Positive Tumors

362 | May 05 2023

The study demonstrates the potential of Anticalin proteins as radioligands for PET-imaging of xenograft tumors in mice, with the use of PASylation technology to tailor their plasma half-life and the cyclic radiochelator FsC being superior to Dfo for 89Zr-ImmunoPET-imaging. [Read the Full Post]

Apatinib combined with SOX regimen for conversion therapy in advanced gastric cancer patients: a retrospective cohort study

314 | May 02 2023

The study shows that conversion chemotherapy followed by surgery and apatinib-targeted therapy combined with SOX chemotherapy may be beneficial for patients with advanced gastric cancer. [Read the Full Post]

Fk506 Inhibit liver regeneration in HOC model Rat

388 | Apr 30 2023

The study found that FK506 inhibits HOC activation and proliferation, ultimately blocking liver regeneration and highlighting the importance of understanding the role of lymphocytes in liver regeneration and the clinical use of FK506 in liver transplantation. [Read the Full Post]

The Mystery of EVP4593: Perspectives of the Quinazoline-Derived Compound in the Treatment of Huntington's Disease and Other Human Pathologies

262 | Apr 29 2023

EVP4593, a quinazoline derivative, has shown potential as a therapeutic agent in various pathologies, including Huntington's disease, by modulating calcium signaling and reducing the levels of specific proteins. [Read the Full Post]

Maslinic Acid Ameliorates Myocardial Ischemia Reperfusion Injury-Induced Oxidative Stress via Activating Nrf2 and Inhibiting NF-[Formula: see text]B Pathways

125 | Apr 29 2023

The study found that maslinic acid has potent antioxidative properties and exerts its cardioprotective effect through activating the Nrf2/HO-1 pathway and inhibiting NF-κB activation, indicating its potential therapeutic use in the treatment of myocardial ischemia-reperfusion injury and other conditions associated with oxidative stress and inflammation. [Read the Full Post]

Glucose induced-AKT/mTOR activation accelerates glycolysis and promotes cell survival in acute myeloid leukemia

269 | Apr 28 2023

The study found that glucose-induced AKT/mTOR activation promotes AML growth and inhibition of glycolysis may be a potential therapy strategy for AML. [Read the Full Post]

4-octyl itaconate ameliorates alveolar macrophage pyroptosis against ARDS via rescuing mitochondrial dysfunction and suppressing the cGAS/STING pathway

335 | Apr 28 2023

This study suggests that 4-octyl itaconate has the potential to ameliorate acute respiratory distress syndrome by inhibiting NLRP3-mediated macrophage pyroptosis in a STING/IRF3-dependent manner and rescuing mitochondrial dysfunction. [Read the Full Post]

Positron Emission Tomography Imaging in Vasculitis

300 | Apr 27 2023

FDG-PET/CT is an important imaging tool in the diagnosis and therapeutic monitoring of vasculitides affecting large-sized and medium-sized vessels, and with advancements in newer generation scanners and development of novel tracers, it has shown significant potential in accurately assessing the full disease extent and detecting vascular infiltrates. [Read the Full Post]

The Multidrug Resistance Transporter P-glycoprotein Confers Resistance to Ferroptosis Inducers

262 | Apr 26 2023

The study investigates the interaction of small molecule ferroptosis inducers with ABC transporters, specifically P-glycoprotein and ABCG2, highlighting their potential role in limiting bioavailability and brain penetration of these inducers and predicting drug-drug interactions. [Read the Full Post]

Immune checkpoint inhibitors modulate the cytotoxic effect of chemotherapy in lung adenocarcinoma cells

385 | Apr 24 2023

The study found that immune checkpoint inhibitors can either potentiate or depotentiate the cytotoxic effects of chemotherapy in lung adenocarcinoma cell lines with different PD-L1 expression levels, and the specific effects vary depending on the ICIs and chemotherapy agents used. [Read the Full Post]

Insights into the mechanisms of triptolide nephrotoxicity through network pharmacology-based analysis and RNA-seq

508 | Apr 19 2023

The combination of network pharmacology and deep RNA-seq analysis provides valuable insights into the molecular mechanisms of TPL nephrotoxicity, identifying potential targets and signaling pathways for further investigation. [Read the Full Post]

Chlorogenic acid, rutin, and quercetin from Lysimachia christinae alleviate triptolide-induced multi-organ injury in vivo by modulating immunity and AKT/mTOR signal pathway to inhibit ferroptosis and apoptosis

528 | Apr 18 2023

The study showed that a combination of organ-protective ingredients from Lysimachia christinae could protect against triptolide-induced multi-organ injury in vivo by activating the AKT/mTOR pathway and reducing cell death including ferroptosis and apoptosis inhibition. [Read the Full Post]

Late gene expression-deficient cytomegalovirus vectors elicit conventional T cells that do not protect against SIV

219 | Apr 17 2023

The study found that Rh108-dependent late gene expression is required for the induction of MHC-E-restricted T cells and protection against SIV in rhesus macaques vaccinated with RhCMV/SIV vectors. [Read the Full Post]

Muscle-Specific Ablation of Glucose Transporter 1 (GLUT1) Does Not Impair Basal or Overload-Stimulated Skeletal Muscle Glucose Uptake

437 | Apr 15 2023

The study found that GLUT1 is not necessary for basal muscle glucose uptake and suggests a novel glucose transport mechanism mediates overload-stimulated glucose uptake. [Read the Full Post]

Investigation of the impact of rosuvastatin and telmisartan in doxorubicin-induced acute cardiotoxicity

387 | Apr 15 2023

The study found that pre-treatment with rosuvastatin and telmisartan, alone or in combination, showed significant cardio-protective effects against the acute cardiotoxicity induced by doxorubicin. [Read the Full Post]

Romidepsin-induced durable remission for relapsed nodal peripheral T-cell lymphoma with T follicular helper phenotype after allogeneic hematopoietic cell transplantation

284 | Apr 14 2023

This case report suggests that romidepsin may be a safe and effective treatment option for patients with relapsed or refractory PTCL-TFH after allogeneic HCT. [Read the Full Post]

Modulation of the endoplasmic reticulum stress and unfolded protein response mitigates the behavioral effects of early-life stress

434 | Apr 13 2023

The study suggests that modulation of ER stress and UPR processes may underlie susceptibility or resilience to early-life stress (ELS) in rats. [Read the Full Post]

Regulation of programmed death ligand 1 expression by interferon-γ and tumour necrosis factor-α in canine tumour cell lines

215 | Apr 12 2023

The study demonstrates that upregulation of PD-L1 expression in canine tumours is regulated by the JAK-STAT and NF-κB signaling pathways upon stimulation with IFN-γ and TNF-α, respectively. [Read the Full Post]

Targeting the Nerve Growth Factor Signaling Impairs the Proliferative and Migratory Phenotype of Triple-Negative Breast Cancer Cells

344 | Apr 11 2023

The study investigates the role of nerve growth factor and its receptor, tropomyosin receptor kinase A, in triple-negative breast cancer and suggests that targeting TrkA may be a potential therapeutic strategy for this disease. [Read the Full Post]

A Cell System-Assisted Strategy for Evaluating the Natural Antioxidant-Induced Double-Stranded DNA Break (DSB) Style

348 | Apr 11 2023

Researchers evaluated whether natural antioxidants induce DNA damage using gene-knockout cell lines and found that sulforaphane induces single-strand breaks or DNA strand crosslinks, quercetin induces double-strand breaks, while resveratrol exerts cytotoxic effects other than DNA damage, and the mechanisms through which kaempferol and genistein induce DNA damage remain unknown. [Read the Full Post]

The cytotoxic activity of carfilzomib together with nelfinavir is superior to the bortezomib/nelfinavir combination in non-small cell lung carcinoma

285 | Apr 09 2023

Combining carfilzomib with nelfinavir shows superior efficacy in inducing proteotoxicity and endoplasmic reticulum stress in non-small-cell-lung carcinoma (NSCLC) compared to the combination of bortezomib and nelfinavir, and may represent a future treatment option for NSCLC. [Read the Full Post]

The Current Role of Disease-modifying Osteoarthritis Drugs

320 | Apr 07 2023

The review explores the potential of disease-modifying osteoarthritis drugs (DMOADs) to induce repair and regeneration of articular tissues, but their clinical effectiveness has not yet been demonstrated for managing OA. [Read the Full Post]

Lonafarnib improves cardiovascular function and survival in a mouse model of Hutchinson-Gilford progeria syndrome

244 | Apr 06 2023

This study reports the positive effects of lonafarnib on cardiovascular structure, properties, and function in a mouse model of progeria, leading to 100% survival of treated mice and improved arterial structure and function, while rapamycin did not improve outcomes. [Read the Full Post]

The role of transforming growth factor-β2 in cigarette smoke-induced lung inflammation and injury

530 | Apr 06 2023

The study found that TGF-β2 attenuated CSE-induced IL-8 production in PBECs and alleviated lung inflammation/injury in CS-exposed mice through the Smad3 signaling pathway. [Read the Full Post]

Methyltransferase K-D-K-E motif influences the intercellular transmission of Newcastle disease virus

654 | Apr 05 2023

This research demonstrates that mutations in the K-D-K-E methyltransferase motif restrict the cell-to-cell spread of Newcastle disease virus via tunnelling nanotubes. [Read the Full Post]

Extracellularly Detectable Electrochemical Signals of Living Cells Originate from Metabolic Reactions

91 | Apr 05 2023

This study demonstrates that intracellular metabolic pathways generating ATP contribute to extracellularly detectable electrochemical signals in living cells, which can be amplified with metabolic activator cocktails and used to detect the effects of anticancer drugs and quantify senescence in mesenchymal stem cells. [Read the Full Post]

Pyruvate Dehydrogenase Inhibition Leads to Decreased Glycolysis, Increased Reliance on Gluconeogenesis and Alternative Sources of Acetyl-CoA in Acute Myeloid Leukemia

149 | Apr 05 2023

AML cells compensate for devimistat-mediated inhibition of PDH and glycolysis by activating alternative metabolic pathways such as gluconeogenesis, fatty acid oxidation, and non-glycolytic sources of acetyl-CoA, highlighting the need to explore strategies targeting these escape pathways to improve the efficacy of devimistat in AML. [Read the Full Post]

Patient-reported outcomes in capmatinib-treated patients with METex14-mutated advanced NSCLC: Results from the GEOMETRY mono-1 study

168 | Apr 05 2023

Capmatinib showed meaningful improvements in cough and preserved quality of life in patients with METex14-mutated advanced non-small cell lung cancer, as reported by patient-reported outcomes in the GEOMETRY mono-1 study. [Read the Full Post]

Real-world outcomes in non-small-cell lung cancer patients with MET Exon 14 skipping mutation and brain metastases treated with capmatinib

246 | Apr 05 2023

This retrospective medical record review study demonstrated that capmatinib is effective in treating non-small-cell lung cancer patients with MET exon 14 skipping mutation and brain metastases in a real-world setting, with high response rates and progression-free survival. [Read the Full Post]

Monitoring paxillin in astrocytes reveals the significance of the adhesion GPCR VLGR1/ADGRV1 for focal adhesion assembly

384 | Apr 04 2023

VLGR1 is a vital component of focal adhesions and regulates cell migration by controlling focal adhesion turnover during their assembly, and its dysfunctions may contribute to the pathogenesis of Usher syndrome, epilepsy, and other related diseases. [Read the Full Post]

Lipopolysaccharide sensitizes the therapeutic response of breast cancer to IAP antagonist

208 | Apr 03 2023

The study shows that LPS enhances the therapeutic response of IAP antagonists in treating triple-negative and ER+ breast cancer by inducing rapid apoptosis of cancer cells through TLR4- and MyD88-mediated production of TNFα, and suggests that antibiotics that can reduce microbiota-derived LPS should not be used together with an IAP antagonist for cancer therapy. [Read the Full Post]

CUDC907, a dual phosphoinositide-3 kinase/histone deacetylase inhibitor, promotes apoptosis of NF2 Schwannoma cells

295 | Apr 03 2023

CUDC907, a dual HDAC/PI3K inhibitor, selectively reduces the viability of human merlin deficient Schwann cells (MD-SCs), promotes cell cycle arrest and caspase-3/7 activation, decreases levels of pAKT and YAP, and shows potential as a therapeutic option for Neurofibromatosis Type 2 (NF2). [Read the Full Post]

Co-targeting of HDAC, PI3K, and Bcl-2 results in metabolic and transcriptional reprogramming and decreased mitochondrial function in acute myeloid leukemia

250 | Apr 03 2023

The study found that the combination of CUDC-907 and venetoclax induces metabolic and transcriptomic reprogramming and suppresses oxidative phosphorylation in AML cells, providing a promising therapeutic approach for AML. [Read the Full Post]

AZ-628 delays osteoarthritis progression via inhibiting the TNF-α-induced chondrocyte necroptosis and regulating osteoclast formation

226 | Apr 02 2023

AZ-628 has the potential to treat osteoarthritis by inhibiting chondrocyte inflammation and necroptosis, regulating osteoclast formation, and slowing down subchondral bone changes induced by dynamic bone remodeling. [Read the Full Post]

A Novel Quantum Dots-Based Fluorescent Sensor for Determination of the Anticancer Dacomitinib: Application to Dosage Forms

258 | Apr 01 2023

The study proposes a novel spectrofluorimetric method for determining the concentration of dacomitinib using newly synthesized nitrogen-doped carbon quantum dots as fluorescent probes, which exhibit native fluorescence and are selectively quenched by increasing concentrations of dacomitinib, offering a simple, efficient, and eco-friendly means of determining the concentration of dacomitinib. [Read the Full Post]

An evaluation of fedratinib for adult patients with newly diagnosed and previously treated myelofibrosis

391 | Apr 01 2023

Fedratinib is a selective JAK2 inhibitor that has been approved by the FDA for the treatment of intermediate-2 or high-risk primary or secondary MF, providing a second-line treatment option for patients who failed or discontinued ruxolitinib, but new combinations with other targeted therapies are needed to improve management of the disease. [Read the Full Post]

Pharmacotherapeutic advances for splenomegaly in myelofibrosis

446 | Apr 01 2023

Myelofibrosis is a hematologic malignancy characterized by splenomegaly in most patients, with JAK inhibitors being the primary pharmacologic treatment option, but alternative therapies and non-pharmacologic approaches may also be considered, and novel combination therapies are being explored. [Read the Full Post]

Transporter‑mediated drug‑drug interactions involving poly (ADP‑ribose) polymerase inhibitors (Review)

199 | Apr 01 2023

Transporter-mediated drug-drug interactions should be considered when co-administering PARP inhibitors with other therapeutic agents to avoid potential toxicity or suboptimal efficacy. [Read the Full Post]

New therapies in non-small cell lung cancer with EGFR exon 20 insertion mutations

275 | Mar 31 2023

The review identified promising therapies for NSCLC with EGFR exon 20 insertion mutations, but further comparative studies with larger sample sizes and better design are needed to confirm their efficacy. [Read the Full Post]

Bicarbonate transporter SLC4A7 promotes EMT and metastasis of HNSCC by activating the PI3K/AKT/mTOR signaling pathway

258 | Mar 29 2023

The study identifies SLC4A7 as a potential therapeutic target in HNSCC due to its promotion of EMT and metastasis through the PI3K/AKT/mTOR signaling pathway. [Read the Full Post]

Novel Dual PI3K/mTOR Inhibitor, Apitolisib (GDC-0980), Inhibits Growth and Induces Apoptosis in Human Glioblastoma Cells

227 | Mar 29 2023

The study found that the dual PI3K/mTOR inhibitor GDC-0980 induces cytotoxicity and apoptosis in GBM cells and may be a potential candidate for anti-GBM therapy. [Read the Full Post]

Identification of a novel circRNA-miRNA-mRNA regulatory axis in hepatocellular carcinoma based on bioinformatics analysis

228 | Mar 28 2023

This study explores the role of circRNAs in hepatocellular carcinoma and identifies potential diagnostic and therapeutic targets using various analytical methods. [Read the Full Post]

Effect of 11-Deoxycorticosterone in the Transcriptomic Response to Stress in Rainbow Trout Skeletal Muscle

214 | Mar 26 2023

The study demonstrates the role of 11-deoxycorticosterone (DOC) in modulating the stress response of skeletal muscles in rainbow trout and highlights its differential modulation by glucocorticoid receptor (GR) and mineralocorticoid receptor (MR), complementing the action of cortisol. [Read the Full Post]

Evaluation of Pain and Use of Analgesics during Medical Termination of Pregnancy in Real-Life Settings

338 | Mar 25 2023

This study evaluated pain related to medical termination of pregnancy (MToP) and its management in 23 centers in France, finding that higher doses of misoprostol were strongly associated with both pain and curative analgesic intake, while analgesic prophylaxis prescription was associated with a decreased risk of curative analgesic intake. [Read the Full Post]

Luteolin-7-O-rutinoside Protects RIN-5F Cells from High-Glucose-Induced Toxicity, Improves Glucose Homeostasis in L6 Myotubes, and Prevents Onset of Type 2 Diabetes

324 | Mar 24 2023

Lut-7-O-rutin has been found to have a protective effect on high-glucose-induced toxicity to RIN-5F cells and improve insulin secretion and glucose uptake through various molecular mechanisms. [Read the Full Post]

Neurotherapeutic Effects of Quercetin and Its Metabolite Compounds on Cognitive Impairment and Parkinson's Disease: An In Silico Study

507 | Mar 22 2023

This study identified the metabolomic profile and potential therapeutic effects of quercetin and its metabolites in cognitive impairment and Parkinson's disease, but further research is needed to confirm these findings in vivo and address potential adverse effects. [Read the Full Post]

Managing Vibration Training Safety by Using Knee Flexion Angle and Rating Perceived Exertion

438 | Mar 22 2023

This study found that a knee flexion angle of approximately 110 degrees is most effective in reducing vibration transmissibility during whole-body vibration exercise, while also observing a positive correlation between the rating of perceived exertion and the platform-to-head transmissibility. [Read the Full Post]

Dihydroartemisinin-ursodeoxycholic acid conjugate is a potential treatment agent for inflammatory bowel disease

163 | Mar 21 2023

Compound 4, a dihydroartemisinin-ursodeoxycholic acid conjugate, exhibits strong immunosuppressive activity and has the potential to be developed into an anti-inflammatory bowel disease drug. [Read the Full Post]

WP1130 relieves septic shock in mice by inhibiting NLRP3 inflammasome activation

278 | Mar 20 2023

WP1130 specifically inhibits NLRP3 inflammasome activation and alleviates septic shock in mice. [Read the Full Post]

USP9x promotes CD8 + T-cell dysfunction in association with autophagy inhibition in septic liver injury

279 | Mar 20 2023

This study suggests that USP9x inhibition could be a potential therapeutic target for septic liver injury by promoting CD8+ T-cell function via autophagy regulation. [Read the Full Post]

Defining the role of mTOR pathway in the regulation of stem cells of glioblastoma

190 | Mar 19 2023

Inhibition of the mTOR pathway, particularly with the small molecule inhibitor Torin2, shows potential as a strategy for targeting the cancer stem cells of glioblastoma, a deadly brain tumor characterized by resistance to conventional therapies. [Read the Full Post]

Targeting Echinococcus multilocularis PIM kinase for improving anti-parasitic chemotherapy

454 | Mar 18 2023

The study identified PIM kinase as a potential target for the development of novel treatments for alveolar echinococcosis, and demonstrated the utility of high-throughput in silico approaches to design small molecule compounds of higher specificity for parasite cells. [Read the Full Post]

Targeting peripheral immune organs with self-assembling prodrug nanoparticles ameliorates allogeneic heart transplant rejection

182 | Mar 18 2023

The passage describes the development of a self-assembling nanoparticle, DHA-PP242 nanoparticle (DPNP), which targets immune organs to regulate T cell function and has shown promise in reducing inflammatory response and extending the survival of grafts in an experimental model of heart transplantation. [Read the Full Post]

Significance of Basal Membrane Permeability of Epithelial Cells in Predicting Intestinal Drug Absorption

176 | Mar 15 2023

The study showed that assessing the permeability of A and B membranes separately and accounting for the intracellular drug concentration can improve the accuracy of predicting drug absorption in the gastrointestinal tract and understanding the role of transporters and enzymes. [Read the Full Post]

HDAC8-Selective Inhibition by PCI-34051 Enhances the Anticancer Effects of ACY-241 in Ovarian Cancer Cells

272 | Mar 13 2023

The study suggests that co-inhibition of HDAC6 and HDAC8 through selective inhibitors could be a novel therapeutic approach for ovarian cancer patients with wild-type p53. [Read the Full Post]

Effects of supplementing organic- and inorganic-based selenium with vitamin E on intestinal histomorphology, caecal bacterial proliferation, and short-chain fatty acid profile in layer hens

371 | Mar 12 2023

Organic selenium supplementation, particularly bacterial organic selenium, enhances intestinal histomorphology, increases beneficial caecal bacterial proliferation, and increases butyric acid content in layer chickens. [Read the Full Post]

Emerging drug targets for sickle cell disease: shedding light on new knowledge and advances at the molecular level

376 | Mar 10 2023

Understanding early events in sickle cell disease pathogenesis associated with the presence of hemoglobin S is crucial for identifying new targets for treatment, including reducing HbS levels, reducing the impact of HbS polymers, and targeting membrane events, and exploiting the unique permeability of sickle cells for developing targeted therapies. [Read the Full Post]

DTIC (nsc-45388) and combination therapy for melanoma. I. Studies with DTIC, BCNU (NSC-409962), CCNU (NSC-79037), vincristine (NSC-67574), and hydroxyurea (NSC-32065)

261 | Mar 10 2023

The study found that combination chemotherapy regimens can improve response rates and survival times in patients with metastatic malignant melanoma, but careful monitoring of toxicity is necessary and treatment decisions should be individualized based on the patient's clinical profile. [Read the Full Post]

Effect of hybrid compounds of stilbene and pentadienone on inhibition of tubulin polymerization

551 | Mar 09 2023

The study designed and synthesized hybrid compounds with excellent anticancer properties that inhibit tubulin polymerization and induce cell cycle arrest in MDA-MB-231 human breast cancer cells. [Read the Full Post]

Hypoxia-induced YAP activation and focal adhesion turnover to promote cell migration in mesenchymal TNBC cells

390 | Mar 08 2023

The study suggests that hypoxia-induced YAP activation is positively associated with mesenchymal TNBC cell migration and may be a novel factor responsible for promoting the aggressive behavior of TNBC cells under hypoxic conditions. [Read the Full Post]

Impacts of Statin Therapy Strategies on Incidence of Ischemic Cerebrovascular Events in Patients With Aneurysmal Subarachnoid Hemorrhage: A Systematic Review and Bayesian Network Meta-Analysis

171 | Mar 08 2023

The Bayesian network meta-analysis and systematic review suggest that statins can significantly improve functional prognosis and reduce the incidence of ischemic cerebrovascular events in patients with aSAH, with pravastatin (40 mg/d) being the most effective type of statin. [Read the Full Post]

Assessment of the regenerative potential of macro-porous chitosan-calcium simvastatin scaffolds on bone cells

321 | Mar 08 2023

The study evaluated the bioactive potential of a macro-porous chitosan scaffold incorporated with calcium hydroxide and functionalized with bioactive doses of simvastatin for bone tissue regeneration, demonstrating increased bioactivity and promising potential. [Read the Full Post]

Chemotherapeutic Activity of Pitavastatin in Vincristine Resistant B-Cell Acute Lymphoblastic Leukemia

247 | Mar 07 2023

The study suggests that pitavastatin may have potential as a repurposed chemotherapeutic agent for vincristine-resistant B-cell acute lymphoblastic leukemia. [Read the Full Post]

Association between the choice of the conditioning regimen and outcomes of allogeneic hematopoietic cell transplantation for myelofibrosis

141 | Mar 04 2023

The study found that Fludarabine/busulfan is the optimal conditioning regimen for allogeneic hematopoietic cell transplantation in myelofibrosis based on lower mortality and graft versus host disease rates. [Read the Full Post]

Effect of maca (Lepidium meyenii) extract on non-obstructive azoospermia in male mice

223 | Mar 04 2023

The study found that maca can improve azoospermia by promoting testicular recovery and increasing testosterone levels, with the polysaccharide fraction identified as the active component. [Read the Full Post]

Effect of Disulfiram on the Reproductive Capacity of Female Mice

313 | Mar 03 2023

Disulfiram (DSF) has been found to increase ovulation rate, enhance antioxidant capacity of oocytes, and promote successful pregnancy in mice by regulating gene expression related to angiogenesis, follicular development, ovulation, and antioxidants, however, more research is needed to determine if these results can be translated to humans and the safety of using DSF during pregnancy. [Read the Full Post]

Medications for the Treatment of Alcohol Dependence-Current State of Knowledge and Future Perspectives from a Public Health Perspective

369 | Mar 03 2023

The treatment of alcohol dependence requires a multi-disciplinary approach, combining psychotherapy with medications, and more research is needed to find new and effective treatments for this complex condition. [Read the Full Post]

Evaluation of the knowledge of hematologists about the management of infectious complications in hematologic patients

187 | Mar 02 2023

The study results highlight the need for continuous education for hematologists in Brazil to improve their knowledge and understanding of infectious complications in patients with hematologic malignancies and hematopoietic cell transplant recipients. [Read the Full Post]

Effect of MXRA7 on the Biological Functions of Acute B Lymphoblastic Leukemia Cell Line REH

219 | Mar 02 2023

The study found a positive correlation between the expression of MXRA7 and acute B-ALL and suggests that knockdown of MXRA7 may be a potential target for the treatment of B-ALL by reducing cell proliferation and increasing sensitivity to cytarabine, but further research is needed to confirm its usefulness. [Read the Full Post]

Excess copper catalyzes protein disulfide bond formation in the bacterial periplasm but not in the cytoplasm

237 | Feb 28 2023

Copper toxicity was found to impact proteins by generating disulfide bonds in the periplasm and inactivating enzymes with solvent-exposed [4Fe-4S] clusters, but it was too inefficient at creating disulfide stress in the cytoplasm due to a slow rate of oxygen regeneration. [Read the Full Post]

High Glucose-Induced Kidney Injury via Activation of Necroptosis in Diabetic Kidney Disease

313 | Feb 28 2023

The study found that inhibiting the RIPK1/RIPK3/MLKL pathway through the use of necrostatin-1 or N-acetylcysteine can effectively protect the kidney against high glucose-induced damage in diabetic mice and could be a therapeutic target for diabetic kidney disease. [Read the Full Post]

Clinical efficacy of retreatment of daratumumab-based therapy (D2) in daratumumab-refractory multiple myeloma

208 | Feb 26 2023

In a study of 43 patients with daratumumab-refractory multiple myeloma, a combination of daratumumab-based retreatment with different classes of anti-myeloma drugs showed a 49% response rate, with a median progression-free survival of 7.97 months and a median overall survival of 32.6 months. [Read the Full Post]

Nanodroplet-enhanced sonodynamic therapy potentiates immune checkpoint blockade for systemic suppression of triple-negative breast cancer

428 | Feb 25 2023

The combination of STING activation, hypoxia relief, and sonodynamic therapy with anti-PD-L1 therapy using an O2-filled nanodroplet shows strong efficacy in suppressing triple-negative breast cancer growth and improving therapeutic outcome by promoting mature DCs, inducing immunogenic cell death, and enhancing tumor infiltration of CTLs. [Read the Full Post]

Association between Quality of Life and Visual Acuity in a Randomized Clinical Trial of Patients with Uveitis Taking Antimetabolites

130 | Feb 23 2023

The study evaluated the association between changes in visual acuity and quality of life among patients with non-infectious uveitis taking antimetabolites, and found that changes in visual acuity were significantly correlated with changes in quality of life, and the treatment group was not significantly associated with any quality of life measure. [Read the Full Post]

Influence of SLCO1B1 Polymorphisms on the Pharmacokinetics of Mycophenolic Acid in Renal Transplant Recipients

169 | Feb 23 2023

This study found a correlation between 4 single nucleotide polymorphisms (SNPs) and the pharmacokinetics of mycophenolic acid (MPA) in renal transplant recipients, with the most relevant SNP being rs4149036 located in SLCO1B1, which had a stronger influence on older, male, or high-albumin recipients. [Read the Full Post]

Role of STAT3 in the initiation, progression, proliferation and metastasis of breast cancer and strategies to deliver JAK and STAT3 inhibitors

255 | Feb 23 2023

This review article focuses on the role of STAT3 in the development and progression of breast cancer, and the potential of phytochemicals, synthetic molecules, and biologicals to inhibit JAK-STAT and STAT3, as a promising approach in the development of better therapeutics against breast cancer. [Read the Full Post]

The novel histone deacetylase inhibitor pracinostat suppresses the malignant phenotype in human glioma

189 | Feb 23 2023

Pracinostat is a promising novel therapy for human glioma, as it inhibited proliferation, induced apoptosis, and reduced migration and invasion, while also affecting the PI3K/Akt and STAT3 pathways. [Read the Full Post]

Fludarabine or cyclophosphamide in combination with total body irradiation as myeloablative conditioning prior to allogeneic hematopoietic cell transplantation for acute lymphoblastic leukemia: an analysis by the Acute Leukemia Working Party of the EBMT

263 | Feb 22 2023

In this study, results showed that TBI/Cy conditioning was associated with reduced risk of relapse and increased risk of grade 2-4 acute GVHD, while a matched-pair analysis revealed a reduced rate of relapse and no significant effect on other transplantation outcomes when compared to TBI/Flu, leading to the conclusion that TBI/Cy should be considered a preferable regimen for allo-HCT in adult patients with ALL in complete remission. [Read the Full Post]

Drug resistance dependent on allostery: A P-loop rigor Eg5 mutant exhibits resistance to allosteric inhibition by STLC

202 | Feb 20 2023

Resistance to Eg5 inhibitors, a potential target for cancer chemotherapy, was explored using the HCT116 cell line and found to arise from a dominant point mutation in the P-loop of the ATP binding domain of Eg5, Eg5(T107N), causing strong non-exchangeable binding to microtubules and resistance to loop-L5 binding inhibitors, but potentially overcome by inhibitors that bind to sites other than the loop-L5 binding site. [Read the Full Post]

Single-cell transcriptomics reveals the role of Macrophage-Naïve CD4 + T cell interaction in the immunosuppressive microenvironment of primary liver carcinoma

182 | Feb 20 2023

The study investigates the important interactions between immune cells and their targeting drugs in liver carcinoma using single-cell and bulk transcriptomic data, revealing the crucial role of macrophage-naive CD4 + T cell interaction in the immunosuppressive microenvironment of liver carcinoma and identifying five predictive drugs that may help improve the immunosuppressive microenvironment and prevent immune evasion. [Read the Full Post]

Current therapeutic modalities and chemopreventive role of natural products in liver cancer: Progress and promise

910 | Feb 19 2023

Liver cancer treatment options depend on the progression stage of the disease and may include surgery, ablation and radiotherapy, first-line drugs and immunotherapy, and second-line chemotherapeutic drugs, while natural compounds like resveratrol, curcumin and diallyl sulfide are emerging as promising anticancer agents to manage liver cancer. [Read the Full Post]

Another Brick to Confirm the Efficacy of Rigosertib as Anticancer Agent

349 | Feb 18 2023

Rigosertib, a dual PLK1 and PI3K inhibitor, showed dose- and time-dependent efficacy against 5 human tumor cell lines in vitro, with A549 cells being the most sensitive and U87-MG cells the most resistant, with p53 levels affecting the efficacy, making Rigosertib a potential antineoplastic agent against lung cancer in humans. [Read the Full Post]

PLK1-ELAVL1/HuR-miR-122 signaling facilitates hepatitis C virus proliferation

241 | Feb 18 2023

Rigosertib, an anticancer agent under clinical trials, targets PLK1 and modulates ELAVL1/HuR-miR-122 signaling to effectively inhibit the proliferation of wild-type and sofosbuvir resistance-associated HCVs, suggesting it could be useful for treating HCV and HCV-associated diseases. [Read the Full Post]

Transferrin receptor 2 deficiency promotes macrophage polarization and inflammatory arthritis

369 | Feb 18 2023

Tfr2 deletion results in increased joint swelling and bone erosion in a K/BxN serum-transfer arthritis model, which may be due to Tfr2's role in suppressing pro-inflammatory M1-like polarization in macrophages. [Read the Full Post]

Predicting the systemic exposure and lung concentration of nafamostat using physiologically-based pharmacokinetic modeling

194 | Feb 18 2023

This study used a physiologically based pharmacokinetic (PBPK) approach and global sensitivity analysis to predict and evaluate the pharmacokinetic profiles of nafamostat in a virtual healthy population under various dosing regimens and found that the approach is valuable in predicting the PK profile and designing an appropriate dosage regimen for the treatment of COVID-19. [Read the Full Post]

Change in Cutibacterium acnes phylotype abundance and improvement of clinical parameters using a new dermocosmetic product containing Myrtus communis and Celastrol enriched plant cell culture extracts in patients with acne vulgaris

361 | Feb 15 2023

The new dermocosmetic product containing Myrtus communis and Celastrol-enriched plant cell culture extracts improved acne severity by decreasing pro-pathogen phylotype IC and increasing non-pathogen phylotype IB of Cutibacterium acnes and decreasing acne lesion count and improving the Global Evaluation Acne score. [Read the Full Post]

Alpha-kinase1 promotes tubular injury and interstitial inflammation in diabetic nephropathy by canonical pyroptosis pathway

230 | Feb 15 2023

The study shows that ALPK1 activation in diabetic nephropathy causes renal injury and fibrosis through the activation of the canonical caspase-1-GSDMD pyroptosis pathway, which is regulated by the ALPK1/NF-κB pathway. [Read the Full Post]

Synthesis and mechanical properties of highly structure-controlled Zr-based metallic glasses by thermal rejuvenation technique

313 | Feb 15 2023

A new thermal rejuvenation process was developed for Zr-based bulk metallic glass to improve ductility by re-introducing free volume through rapid heating and indirect liquid nitrogen quenching, which was confirmed to reduce STZ volume and enhance homogeneous deformation by molecular dynamics simulations. [Read the Full Post]

Early identification of a 12-bp tandem duplication in TNFRSF11A encoding receptor activator of nuclear factor-kappa B (RANK): Clinical characterization and response to bisphosphonate therapy

220 | Feb 15 2023

A young girl with early-onset deafness, progressive external tooth root resorption, and increased bone turnover due to a 12-bp duplication within exon 1 of TNFRSF11A was successfully treated with bisphosphonates, preventing further skeletal disease. [Read the Full Post]

The effects of neoadjuvant zoledronic acid in breast cancer patients: A meta-analysis of randomized controlled trials

291 | Feb 15 2023

Our study showed that adding Zoledronic acid (ZA) to neoadjuvant therapy for breast cancer did not improve the pathological complete response rate and resulted in worse mortality compared to the control group, but subgroup analysis revealed a potential benefit for postmenopausal women and patients with triple-negative BC, warranting further investigation. [Read the Full Post]

Camptothecin analogs in malignant gliomas: comparative analysis and characterization

294 | Feb 14 2023

The authors compared and characterized several new classes of camptothecin analogs and found that 10,11-methylenedioxy class consistently demonstrated the greatest cytotoxicity and hold promise for more effective local antitumor treatments against malignant intracranial brain tumors. [Read the Full Post]

Population pharmacokinetic analysis of TQ-B3203 following intravenous administration of TQ-B3203 liposome injection in Chinese patients with advanced solid tumors

468 | Feb 14 2023

A population pharmacokinetic model was successfully developed for TQ-B3203, a novel topoisomerase I inhibitor, in Chinese patients with advanced solid tumors and showed that body mass index, lean body weight, and direct bilirubin were significant covariates that affected TQ-B3203 pharmacokinetics. [Read the Full Post]

Celastrol suppresses colorectal cancer via covalent targeting peroxiredoxin 1

224 | Feb 14 2023

A text-mining-based web-server tool was used to identify peroxiredoxin 1 (PRDX1) as the ROS-manipulating target of Celastrol, a natural product isolated from the plant Thunder God Vine, and the anti-tumor efficacy of Celastrol was reduced in colorectal cancer cells by inhibiting PRDX1, and a new derivative compound 19-048 with improved potency against PRDX1 was synthesized. [Read the Full Post]

Effect of Gubenyiliu formula II and its disassembled prescriptions on cell autophagy in breast cancer through PI3K/AKT/mTOR pathway

556 | Feb 12 2023

This study confirmed that GYII can effectively treat breast cancer by inhibiting the PI3K/AKT/mTOR signaling pathway-mediated autophagy, while QX and FZ have different effects on tumor growth and metastasis. [Read the Full Post]

Specific gene module pair-based target identification and drug discovery

778 | Feb 12 2023

A novel method called "gene module pair-based target identification (GMPTI)" was developed to predict the targets of new compounds using consensus gene modules extracted from transcriptional profiles induced by perturbagens of known targets, resulting in the discovery of novel inhibitors for three PI3K pathway proteins. [Read the Full Post]

Successful Treatment of Patient With Ewing Sarcoma in the Setting of Inherited Cholestatic Liver Disease

234 | Feb 12 2023

Treatment of Ewing sarcoma in a patient with PFIC1 presents a challenge due to the reliance of standard chemotherapy on intact hepatic metabolism, which results in prolonged lymphopenia and severe infectious complications in this patient. [Read the Full Post]

Effect of hyperthermia alone and in combination with anticancer drugs on the viability of P388 leukemic cells

242 | Feb 12 2023

Local tumor hyperthermia (42°C) for 1 hour with antineoplastic drugs Adriamycin, Vincristine, or 5-Fluorouracil showed synergistic cell killing action against P388 murine lymphocytic leukemia cells in vitro, while Cyclophosphamide and Cytosine Arabinoside did not show enhanced therapeutic effects. [Read the Full Post]

Zearalenone and its metabolite exposure directs oestrogen metabolism towards potentially carcinogenic metabolites in human breast cancer MCF-7 cells

294 | Feb 11 2023

Mycoestrogens increase the production of CYP1B1-mediated oestrogen catechol metabolites, directing the biotransformation of E2 towards 4-OHE2, a crucial factor in oestrogen-induced tumour initiation. [Read the Full Post]

Survival in a consecutive series of 467 glioblastoma patients: Association with prognostic factors and treatment at recurrence at two independent institutions

165 | Feb 11 2023

A study of 467 recurrent glioblastoma patients in Norway found that age, promoter methylation of MGMT, tumour location, and extent of resection at primary diagnosis were independent prognostic factors, while 60 Gray radiotherapy with concomitant and adjuvant temozolomide at primary diagnosis, gamma knife/stereotactic radiosurgery at first recurrence, and combination chemotherapy with or without bevacizumab at second recurrence were treatments associated with superior survival. [Read the Full Post]

Does PARP Inhibition Sensitize Chondrosarcoma Cell Lines to Chemotherapy or Radiotherapy? Results From a Three-dimensional Spheroid Cell Model

312 | Feb 11 2023

This study shows that long-term talazoparib treatment, a PARP inhibitor, effectively reduced the viability of three representative chondrosarcoma cell lines grown as spheroids, and the combination of talazoparib and temozolomide had a higher chance of success than combination with radiotherapy. [Read the Full Post]

A Camptothetin Analog, Topotecan, Promotes HIV Latency via Interference with HIV Transcription and RNA Splicing

146 | Feb 10 2023

The camptothecin analog topotecan reduces residual activity of HIV in an in vitro primary T cell model of HIV latency, with a reduction in HIV transcriptional activity and downregulation of HIV RNA that cannot be reversed by latency reversing agents; other camptothecin analogs, less toxic than topotecan, should be investigated as potential "block and lock" agents to further silence the HIV provirus and suppress residual inflammation. [Read the Full Post]

Targeting RNA G-quadruplex with repurposed drugs blocks SARS-CoV-2 entry

160 | Feb 10 2023

Topotecan (TPT) and Berbamine (BBM), two clinical approved drugs, have been found to have potential as broad-spectrum antivirals against SARS-CoV-2 by stabilizing RNA G-quadruplexes in several host factors and reducing SARS-CoV-2 pseudovirus entry into target cells in vitro and murine tissues in vivo. [Read the Full Post]

Synthesis and antiproliferative activity evaluation of B-norcholesterol-6-amide compounds

273 | Feb 10 2023

The study found that introducing chloroalkyl acyl groups into the 6-position of 6-amino-B-norcholesterol greatly enhanced the cytotoxicity of the resulting B-norcholesterol-6-amide compounds, with compound 20 having an IC50 value of 3.9 μM on HeLa cells. [Read the Full Post]

Identifying CDC7 as a synergistic target of chemotherapy in resistant small-cell lung cancer via CRISPR/Cas9 screening

180 | Feb 09 2023

CRISPR/Cas9 screening in a chemo-resistant SCLC cell line identified serine/threonine kinase CDC7 as a target and the CDC7 inhibitor XL413 was found to synergize with chemotherapy, increasing apoptosis and inducing G1/S phase arrest and DNA damage in chemo-resistant SCLC cells and improving efficacy in vitro and in vivo with patient-derived xenografts. [Read the Full Post]

Long-Term Complete Remission of a Patient With Double-Hit Diffuse Large B-Cell Lymphoma Treated by Chemoimmunotherapy and Chinese Herbal Medicine

308 | Feb 09 2023

A 73-year-old male diagnosed with double-hit diffuse large B-cell lymphoma underwent a successful treatment combining R-CHOP-14 and dose-adjusted DA-EPOCH-R chemotherapy with Chinese herbal medicine (Sijunzi Decoction and Prunella vulgaris) with no adverse events, resulting in no evidence of recurrence and a good quality of life for over 8 years. [Read the Full Post]

Final analysis of the phase 3 randomized clinical trial comparing HD201 vs. referent trastuzumab in patients with ERBB2-positive breast cancer treated in the neoadjuvant setting

143 | Feb 08 2023

The final analysis of the TROIKA trial confirmed that HD201 and trastuzumab were equally effective in terms of event-free and overall survival, and both treatments were safe with no serious adverse events related to the study treatment. [Read the Full Post]

DROEG: a method for cancer drug response prediction based on omics and essential genes integration

275 | Feb 08 2023

The study developed a novel method called DROEG for predicting drug response in cancer patients by integrating genomic, transcriptomic, methylomic and CRISPR essential gene information and found it to be a more accurate approach compared to existing algorithms. [Read the Full Post]

Comparative study between two different morphological structures based on polylactic acid, nanocellulose and magnetite for co-delivery of flurouracil and curcumin

321 | Feb 07 2023

The magnetic copolymeric micelles M-PLA-co-NC/5-FU/CUR showed superior antibacterial and antitumor efficacy, slower release and higher loading % of CUR compared to the blended formulation PLA/M-NC/5-FU/CUR, making them a promising nanomedicine against bacteria and multiple cell lines. [Read the Full Post]

Extracellular vesicles derived from dental mesenchymal stem/stromal cells with gemcitabine as cargo have an inhibitory effect on the growth of pancreatic carcinoma cell lines in vitro

323 | Feb 07 2023

DP-MSC-EVs have therapeutic potential as a drug delivery tool for cancer therapy by absorbing and secreting gemcitabine and expressing a suicide gene to convert non-toxic prodrug 5-FC to cytotoxic drug 5-FU, resulting in significant inhibition of cancer cell growth. [Read the Full Post]

Melatonin activates mitochondrial unfolded protein response to preserve osteogenic potential of senescent BMSCs via upregulating PDI-6

325 | Feb 06 2023

PDI-6, a regulator of mitochondrial homeostasis, is a target for melatonin in the treatment of age-related osteoporosis due to its ability to enhance osteogenic differentiation in senescent BMSCs, which has decreased function, by rescuing mitochondrial function and being a downstream effector of the Wnt/β-catenin pathway. [Read the Full Post]

Insights into the antioxidative mechanisms of melatonin in ameliorating chromium-induced oxidative stress-mediated hepatic and renal tissue injuries in male Wistar rats

354 | Feb 06 2023

Melatonin has been shown to protect against chromium-induced oxidative damage in liver and kidney tissues by preserving organ weight, intracellular antioxidant enzymes, and reducing tissue chromium content, oxidative stress biomarkers, and pro-oxidant enzyme activities through its antioxidant and metal-chelating activity. [Read the Full Post]

[Single-center study of different treatment for advanced or unresectable angiosarcoma patients]

407 | Feb 06 2023

This study found that doxorubicin-based and paclitaxel-based chemotherapy are the most common treatments for advanced angiosarcoma, and combined targeted therapy with anti-PD-1 immunotherapy showed potential efficacy in some patients with long duration of response and moderate adverse events. [Read the Full Post]

Novel carboxymethyl cellulose-halloysite-polyethylene glycol nanocomposite for improved 5-FU delivery

399 | Feb 06 2023

This study synthesized a pH-responsive nanocomposite based on halloysite nanotube (HNT) coated with carboxymethyl cellulose (CMC)/polyethylene glycol (PEG) hydrogel for controlled delivery of 5-Fluorouracil (5-FU), a hydrophobic chemotherapy drug, using the W/O/W technique, achieving high drug entrapment and loading and showing improved and sustained 5-FU delivery in acid environment and considerable cytotoxicity on MCF-7 breast cancer cells. [Read the Full Post]

Decitabine enhances the tumoricidal potential of TRAIL via the epigenetic regulation of death receptor 4 in gastric cancer

272 | Feb 05 2023

Decitabine enhances the anti-tumor effect of TRAIL by upregulating DR4 expression through epigenetic modification, acting as a sensitizing agent, and providing a novel idea for gastric cancer treatment when used in combination. [Read the Full Post]

Mechanisms of response and resistance to combined decitabine and ipilimumab for advanced myeloid disease

306 | Feb 05 2023

The study of combining decitabine and ipilimumab for AML/MDS showed that the clinical response to the combination therapy is primarily driven by decitabine-induced cytoreduction, but evidence of immune activation was only observed after ipilimumab exposure, and long-lasting responses require elimination of leukemic progenitor cells. [Read the Full Post]

Addressing adherence to guidelines on prevention of acute chemotherapy-induced nausea and vomiting in pediatric patients

350 | Feb 04 2023

Guideline adherence for prevention of chemotherapy-induced nausea and vomiting improved significantly, particularly in the high emetogenic chemotherapy group, with education, addition of anti-emetics to formulary, and implementation of a standardized guideline tool, but further improvement is needed in the moderately emetogenic chemotherapy group. [Read the Full Post]

Antiemetic use and chemotherapy induced nausea and vomiting related hospitalization costs after highly or moderately emetogenic chemotherapy

337 | Feb 04 2023

PrecisionQ's database analysis found lower CINV related hospitalization costs among patients receiving netupitant/fosnetupitant with palonosetron (NEPA) compared to aprepitant/fosaprepitant with ondansetron (APON) or aprepitant/fosaprepitant with palonosetron (APPA) during highly emetogenic chemotherapy or moderately emetogenic chemotherapy. [Read the Full Post]

On-treatment derived neutrophil-to-lymphocyte ratio and survival with palbociclib and endocrine treatment: analysis of a multicenter retrospective cohort and the PALOMA-2/3 study with immune correlates

118 | Feb 04 2023

On-treatment derived neutrophil-to-lymphocyte ratio (dNLR) is a significant predictor of progression-free survival (PFS) in postmenopausal women with HR-positive, HER2-negative advanced breast cancer (ABC) receiving palbociclib and endocrine treatment, with reduction in dNLR after treatment predictive of a survival benefit and evidence of systemic immune responses elicited by palbociclib. [Read the Full Post]

Analysis of Circulating DNA to Assess Prognoses for Metastatic Colorectal Cancer Patients Treated with Regorafenib Dose-Escalation Therapy: A Retrospective, Exploratory Analysis of the RECC Trial

249 | Feb 03 2023

A study of 45 patients with metastatic colorectal cancer treated with regorafenib found that KRAS mutations in tissue or plasma did not impact its efficacy, but higher levels of circulating cell-free DNA were associated with poorer prognoses. [Read the Full Post]

Effectiveness of different treatment regimens on patients with COVID-19, hospitalized in Sanandaj hospitals: a retrospective cohort study

167 | Feb 03 2023

The study found that the drug regimen 2 (Interferons (ReciGen/Ziphron) or Interferon Vectra (lopinavir/ritonavir)) increased the days of hospitalization and hospitalization in ICU, while other drug regimens had no significant effect on mortality, use of a ventilator, or reducing mortality compared to the others. [Read the Full Post]

Awareness on current status of usage of ritonavir in the management of covid among dental students

265 | Feb 03 2023

A survey of 100 dental students in Chennai showed that postgraduate students had greater knowledge of the current use of Ritonavir in the management of COVID-19, but the study highlights the need for regular education and training programs for all healthcare workers on COVID-19 infection control procedures. [Read the Full Post]

A combination of telomerase inhibition and NK cell therapy increased breast cancer cell line apoptosis

172 | Feb 03 2023

Inhibiting telomerase with BIBR1532 increased the cytotoxicity of natural killer cells against breast cancer and synergistically enhanced cell death by suppressing hTERT and upregulating apoptotic-related genes, making breast cancer cells more sensitive to NK cell therapy and potentially useful in the treatment of breast cancer. [Read the Full Post]

Immunotherapy in hepatocellular carcinoma: how will it reshape treatment sequencing?

147 | Feb 02 2023

The treatment landscape for advanced hepatocellular carcinoma (HCC) has become complex with the introduction of immune checkpoint inhibitors (ICIs), and a number of second-line therapies, with rechallenge with ICIs being an attractive alternative, but requires careful evaluation and the identification of predictive biomarkers is an urgent matter to address in HCC research. [Read the Full Post]

Evaluating the role of polysaccharide extracted from Pleurotus columbinus on cisplatin-induced oxidative renal injury

264 | Feb 02 2023

The polysaccharide PsPc-3 from Pleurotus columbinus showed antioxidant activity and reduced oxidative renal injury induced by cisplatin in rats, indicating it may be a potential treatment for cisplatin-induced nephrotoxicity. [Read the Full Post]

Microglial P2Y12 Signaling Contributes to Cisplatin-induced Pain Hypersensitivity via IL-18-mediated Central Sensitization in the Spinal Cord

306 | Feb 02 2023

Microglia P2Y12-Src family kinase-p38 signaling contributes to cisplatin-induced pain hypersensitivity via IL-18-mediated central sensitization in the spinal cord, with P2Y12 being a potential target for preventing chemotherapy-induced pain hypersensitivity. [Read the Full Post]

STAT3 promotes differentiation of monocytes to MDSCs via CD39/CD73-adenosine signal pathway in oral squamous cell carcinoma

143 | Feb 01 2023

The study found that STAT3 blockade reduced the expression of CD39/CD73 and the synthesis of adenosine, inhibiting monocytes to MDSCs differentiation, leading to prominent anti-tumor efficacy in OSCC mouse model and suggesting STAT3 blockade as a promising therapeutic strategy for oral squamous cell carcinoma. [Read the Full Post]

Efficacy and safety of treatments for advanced thymic carcinoma after failure of first-line platinum-based chemotherapy: A systematic literature review and meta-analysis

266 | Feb 01 2023

This study conducted a systematic literature review of 19 clinical trials to assess the clinical outcomes of various regimens in patients with thymic carcinoma (TC) who failed first-line chemotherapy, finding limited treatment options with response rates ranging from 9% to 38% and prolonged duration of response with pembrolizumab, but a need for further well-powered clinical trials to better inform on optimal treatments. [Read the Full Post]

SNS-023 sensitizes hepatocellular carcinoma to sorafenib by inducing degradation of cancer drivers SIX1 and RPS16

92 | Jan 29 2023

Yuan Liu et al. identified that both SIX1 and RPS16 were crucial substrates for the EGFR-AKT-USP1 axis-driven growth of HCC, suggesting a potential anti-HCC strategy from a novel perspective. [Read the Full Post]

SNS-032 attenuates liver fibrosis by anti-active hepatic stellate cells via inhibition of cyclin dependent kinase 9

82 | Jan 28 2023

Xiao-Li He et al. found that SNS-032 was a potential drug and CDK9 might be a new prospective target for the treatment of liver fibrosis. [Read the Full Post]

Impact of Results of TTF-1 Immunostaining on Efficacy of Platinum-Doublet Chemotherapy in Japanese Patients with Nonsquamous Non-Small-Cell Lung Cancer

452 | Jan 26 2023

Akira Nakao et al. thought that the positivity of TTF-1 immunostaining in tumors could be a predominant prognostic marker for patients who had advanced nonsq NSCLC. [Read the Full Post]

Exonuclease 1 genetic variant is associated with clinical outcomes of pemetrexed chemotherapy in lung adenocarcinoma

462 | Jan 26 2023

Mi Jeong Hong et al. thought that two SNPs in miRNA binding sites, especially EXO1 rs1047840G>A, were associated with the chemotherapy response and survival outcome in lung adenocarcinoma patients treated with pemetrexed. [Read the Full Post]

Remarkable Synergy When Combining EZH2 Inhibitors with YM155 Is H3K27me3-Independent

143 | Jan 25 2023

Jun Yang et al. identified a 27-gene module that was highly expressed in solid tumors, encoding actionable targets including EZH2 and BIRC5. [Read the Full Post]

Drug Repositioning Identifies Six Drug Candidates for Systemic Autoimmune Diseases by Integrative Analyses of Transcriptomes from Scleroderma, Systemic Lupus Erythematosus, and Sjogren's Syndrome

330 | Jan 25 2023

Elif Kubat Oktem et al. provided new insights and opens up new possibilities on both pathogenesis and treatment of systemic ADs through drug repositioning. [Read the Full Post]

Anticancer effects of putative and validated BH3-mimetic drugs in head and neck squamous cell carcinomas: An overview of current knowledge

62 | Jan 24 2023

Gilberto Melo et al. thought that although clinical data were still insufficient to evaluate the anticancer effects of BH3-mimetics in head and neck squamous cell carcinomas, promising results in preclinical settings were observed concerning induction of cell death and inhibition of tumour growth. [Read the Full Post]

VEGFR-TKI treatment for radiation-induced brain injury after gamma knife radiosurgery for brain metastases from renal cell carcinomas

183 | Jan 23 2023

Ryuichi Noda et al. demonstrated the therapeutic effects of vascular endothelial growth factor receptor tyrosine kinase inhibitors on radiation-induced brain injury in patients with brain metastases from renal cell carcinoma treated via gamma knife radiosurgery. [Read the Full Post]

Inhibition of androgen receptor enhanced the anticancer effects of everolimus through targeting glucose transporter 12

263 | Jan 23 2023

Bo Cao et al. thought that interference with AR/GLUT12 pathway might serve as a promising approach to promoting the translational application of everolimus in GC therapy. [Read the Full Post]

Treatment and Implications of Vascular Endothelial Growth Factor Inhibitor-Induced Blood Pressure Rise: A Clinical Cohort Study

318 | Jan 22 2023

Daan C H van Dorst et al. thought that both calcium channel blockers and renin-angiotensin system inhibitors were effective antihypertensive treatments. [Read the Full Post]

Interactive webtool for analyzing drug sensitivity and resistance associated with genetic signatures of cancer cell lines

525 | Jan 19 2023

Myriam Boeschen et al. found support for the described sensitivity of H1047 mutants to GSK690693 targeting the AKT pathway. [Read the Full Post]

Assessment of alterations in histone modification function and guidance for death risk prediction in cervical cancer patients

316 | Jan 17 2023

Tingting Zhao et al.revealed histone modification-associated prognostic genes to construct the HMAG signature, aiming to provide a new insight into prognosis prediction and precise clinical treatment. [Read the Full Post]

Integrative analysis reveals clinically relevant molecular fingerprints in pancreatic cancer

307 | Jan 17 2023

Libin Song et al. found that PCCLs with mutations in CDKN2A, TP53, and SMAD4 were more sensitive to certain anti-cancer drugs. [Read the Full Post]

Systems Drug Design for Muscle Invasive Bladder Cancer and Advanced Bladder Cancer by Genome-Wide Microarray Data and Deep Learning Method with Drug Design Specifications

112 | Jan 09 2023

Po-Wei Su et al. investigated the oncogenic mechanisms of MIBC and ABC, and provided promising therapeutic options for MIBC and ABC, respectively. [Read the Full Post]

Identification of potent inhibitors of SARS-CoV-2 infection by combined pharmacological evaluation and cellular network prioritization

113 | Jan 09 2023

J J Patten et al. establishesd a rigorous approach for future pharmacological and computational identification of host factor dependencies and treatments for viral diseases. [Read the Full Post]

A Novel Cuproptosis-Related Prognostic Model and the Hub Gene FDX1 Predict the Prognosis and Correlate with Immune Infiltration in Clear Cell Renal Cell Carcinoma

250 | Jan 07 2023

Kenan Zhang et al. constructed a CRGs prognostic model and revealed that FDX1 could serve as a prognostic biomarker and predict therapeutic response in ccRCC. [Read the Full Post]

Identification of cuproptosis-related long non-coding ribonucleic acid signature as a novel prognosis model for colon cancer

245 | Jan 07 2023

Rong Xu et al. found that inhibition of AL512306.3 and ZEB1-AS1 significantly suppressed the cell proliferation in colon cancer cells. [Read the Full Post]

Ferroptosis-related differentially expressed genes serve as new biomarkers in ischemic stroke and identification of therapeutic drugs

373 | Jan 05 2023

Yinjiang Zhang et al. found that ferroptosis played a critical role in the diversity and complexity of the IS immune microenvironment. [Read the Full Post]

ZD6474 Attenuates Fibrosis and Inhibits Neovascularization in Human Pterygium by Suppressing AKT-mTOR Signaling Pathway

403 | Jan 05 2023

Wenting Liu et al. found that ZD6474 was more effective than MMC in reducing fibrosis and EMT in HPFs. [Read the Full Post]

Utilizing inner filter effect in resonance Rayleigh scattering technique: a case study with silver nanocubes as RRS probe and several analytes as absorbers

230 | Jan 04 2023

Rasoul Gheitaran et al. found that the newly developed IFE mechanism could be employed as an attractive and highly efficient analytical technique for measuring different analytes. [Read the Full Post]

Complexity in radiological morphology predicts worse prognosis and is associated with an increase in proteasome component levels in clear cell renal cell carcinoma

270 | Jan 04 2023

Kohei Kobatake et al. thought that investigating RM on pre-treatment CT scans could effectively predict worse prognosis. [Read the Full Post]

PIK-24 Inhibits RSV-Induced Syncytium Formation via Direct Interaction with the p85α Subunit of PI3K

203 | Jan 03 2023

Li-Feng Chen et al. showed that a novel PI3K inhibitor inhibited RSV-induced PI3K signaling activation and actin cytoskeleton reorganization by targeting the p85α protein. [Read the Full Post]

Optimizing the value of lenalidomide maintenance by genetic profiling - an analysis of 556 Myeloma XI trial patients

325 | Dec 30 2022

Aikaterini Panopoulou et al. found that extended genetic profiling identified patients deriving exceptional benefit from Len maintenance. [Read the Full Post]

Desensitization Protocol to Lenalidomide: An Effective and Safe Treatment Modality for Delayed Hypersensitivity-induced Rash in Patients with Multiple Myeloma

435 | Dec 29 2022

Oded Shamriz et al. thought that desensitization to lenalidomide was safe and effective. [Read the Full Post]

Combined use of dasatinib and quercetin alleviates overtraining-induced deficits in learning and memory through eliminating senescent cells and reducing apoptotic cells in rat hippocampus

254 | Dec 28 2022

Chenkang Wang found that D+Q alleviated overtraining-induced deficits in learning and memory through elimination of senescent cells and reduction of apoptotic cell number. [Read the Full Post]

Comprehensive Analysis of Circular RNA Expression Profiles in Gefitinib-Resistant Lung Adenocarcinoma Patients

284 | Dec 28 2022

Junyong Zou et al. validated that upregulations of hsa_circ_0030591 and hsa_circ_0040348 might play key roles in EGFR-TKI resistance and thus serving as candidates for biomarker. [Read the Full Post]

GPR120-ERK1-Srebp1c signaling pathway regulates long-chain polyunsaturated fatty acids biosynthesis in marine teleost Siganus canaliculatus

195 | Dec 27 2022

Yewei Dong et al. found that the GPR120-ERK1-Srebp1c signaling pathway regulated rabbitfish LC-PUFA biosynthesis, representing a novel regulatory mechanism in vertebrates. [Read the Full Post]

Clinical impact of minimal residual disease and genetic subtypes on the prognosis of childhood acute lymphoblastic leukemia

373 | Dec 27 2022

Chih-Hsiang Yu et al. found that MRD-directed therapy improved the outcomes for pediatric ALL, especially standard-risk patients. [Read the Full Post]

Sulforaphane attenuates cancer cell-induced atrophy of C2C12 myotubes

216 | Dec 26 2022

Wenlan Li et al. suggested the chemoprotective and antioxidative function of SFN in myotubes, highlighting its therapeutic potential for cancer-related muscle wasting. [Read the Full Post]

A mitophagy-related gene signature associated with prognosis and immune microenvironment in colorectal cancer

549 | Dec 24 2022

Cong Zhang et al. developed a novel mitophagy-related gene signature that could be utilized not only as an independent predictive biomarker but also as a tool for tailoring personalizing treatment for CRC patients. [Read the Full Post]

Safety and tolerability of bosutinib in patients with amyotrophic lateral sclerosis (iDReAM study): A multicentre, open-label, dose-escalation phase 1 trial

401 | Dec 23 2022

Keiko Imamura et al. found that the treatment-responsive patients could be distinguished by lower levels of plasma NFL. [Read the Full Post]

Comparison of efficacy of roxadustat and erythropoietin for the treatment of renal anemia in patients with chronic kidney disease: a retrospective study

174 | Dec 21 2022

Chen Jin et al. thought that orally administered roxadustat improved hemoglobin levels more than rhEPO in patients with CKD and anemia. [Read the Full Post]

A Pan-Cancer Analysis Reveals CLEC5A as a Biomarker for Cancer Immunity and Prognosis

237 | Dec 20 2022

Rui Chen et al. thought that CLEC5A was a potential prognostic biomarker of diverse cancers and a target for anti-tumor therapy. [Read the Full Post]

Epigenomic and transcriptomic landscaping unraveled candidate repositioned therapeutics for non-functioning pituitary neuroendocrine tumors

190 | Dec 19 2022

B Aydin et al. found that molecular docking simulations, palbociclib, linifanib, trametinib, eplerenone, niguldipine, and zuclopenthixol showed higher binding affinities with hub genes compared to their inhibitors. [Read the Full Post]

Factors contributing to the utilization of robotic colorectal surgery: a systematic review and meta-analysis

140 | Dec 17 2022

Dana M Hayden et al. identifies nonclinical disparities in access to robotics that should be addressed to provide more equitable access to innovations in colorectal surgery. [Read the Full Post]

3-deazaadenosine (3DA) alleviates senescence to promote cellular fitness and cell therapy efficiency in mice

122 | Dec 16 2022

Ana Guerrero et al. identified 3DA as a promising drug enhancing the efficiency of cellular therapies by restraining senescence. [Read the Full Post]

APX-115, a pan-NADPH oxidase inhibitor, protects development of diabetic nephropathy in podocyte specific NOX5 transgenic mice

370 | Dec 15 2022

Eun Soo Lee et al. suggested that APX-115 might be a promising therapeutic agent for the treatment of DN because of its pan-NOX inhibitory activity, including its NOX5 inhibitory activity, and also owing to its anti-inflammatory effect. [Read the Full Post]

Fifty Shades of Scandium: Comparative Study of PET Capabilities Using Sc-43 and Sc-44 with Respect to Conventional Clinical Radionuclides

202 | Dec 11 2022

Thiago V M Lima et al. thought that accurate quantitative scandium-43/44 PET/CT was achievable in commercial devices. [Read the Full Post]

Epoxomicin, a Selective Proteasome Inhibitor, Activates AIM2 Inflammasome in Human Retinal Pigment Epithelium Cells

143 | Dec 07 2022

Iswariyaraja Sridevi Gurubaran et al. thought that a selective proteasome inhibitor was a potent inflammasome activator in human RPE cells. [Read the Full Post]

Prolonged activation of NMDA receptors induces dedifferentiation of islet β cells in mice

152 | Dec 07 2022

Xiaoting Huang et al. found that prolonged activation of NMDA receptors induced islet β-cell dedifferentiation via regulating the NF-κB pathway. [Read the Full Post]

The inhibition of MDM2 slows cell proliferation and activates apoptosis in ADPKD cell lines

216 | Dec 05 2022

Simone Patergnani et al. found that the targeting of MDM2 by RG7112 might represent a new therapeutic option for the treatment of ADPKD. [Read the Full Post]

DOT1L regulates MTDH-mediated angiogenesis in triple-negative breast cancer: intermediacy of NF-κB-HIF1α axis

179 | Dec 01 2022

Praveen Kumar Neeli et al. thought that the therapeutic disruption of the DOT1L-MTDH-NF-κB-HIF1α axis might have usefulness in the management of TNBC. [Read the Full Post]

Endothelial NOX4 aggravates eNOS uncoupling by decreasing dihydrofolate reductase after subarachnoid hemorrhage

297 | Dec 01 2022

Sheng-Qing Gao et al. suggested that endothelial DHFR decreased significantly because of the elevated level of endothelial NOX4 leading to decreased cortical perfusion and worse neurological outcome. [Read the Full Post]

Notch signaling-induced cyclin d1 in diabetes ameliorating effects of the isolated polysaccharide from Rosa canina: In vitro and in vivo studies

409 | Nov 30 2022

Soraya Sajadimajd et al. thought that upregulation of Notch signaling-induced cyclin d1 could be proposed as the underlying diabetes-reducing effects of the isolated polysaccharide derivative. [Read the Full Post]

Development of resistance to FGFR inhibition in urothelial carcinoma via multiple pathways in vitro

313 | Nov 29 2022

Geoffrey A Pettitt et al. indicated a benefit from treatment interruptions or re-treatment following disease relapse in some patients. [Read the Full Post]

Renal tubular epithelial cell necroptosis promotes tubulointerstitial fibrosis in patients with chronic kidney disease

167 | Nov 29 2022

Ziyan Lin et al. showed that necroptosis of renal tubular epithelial cells in CKD patients occured, and the peak of necroptosis was in stages 2 and 3a CKD. [Read the Full Post]

Predictors of anemia response to momelotinib therapy in myelofibrosis and impact on survival

395 | Nov 27 2022

Naseema Gangat et al. suggested a short-term survival benefit associated with anemia response in momelotinib-treated patients with MF. [Read the Full Post]

MPN-379 Matching-Adjusted Indirect Comparison (MAIC) of Pelabresib (CPI-0610) in Combination With Ruxolitinib vs. JAK Inhibitor Monotherapy in Patients With Intermediate or High-Risk Myelofibrosis

409 | Nov 27 2022

Vikas Gupta et al. suggested that MAIC-adjusted improvements observed in SVR35 and TSS50 at Week 24 with pelabresib and ruxolitinib vs. ruxolitinib, fedratinib, or momelotinib monotherapy were consistent with unadjusted comparisons. [Read the Full Post]

Hypoxia inducible factor 1α inhibitor induces cell death via suppression of BCR-ABL1 and Met expression in BCR-ABL1 tyrosine kinase inhibitor sensitive and resistant chronic myeloid leukemia cells

150 | Nov 22 2022

Masanobu Tsubaki et al. indicated that HIF-1α regulated BCR-ABL and Met expression and was involved in cell survival in CML cells. [Read the Full Post]

Effect of concomitant use of pitavastatin with neoadjuvant chemotherapy protocols in breast cancer patients: A randomized controlled clinical trial

352 | Nov 21 2022

Samar A Dewidar et al. thought that concomitant use of pitavastatin with standard neoadjuvant chemotherapy protocols might improve neoadjuvant chemotherapy responses in patients with breast cancer. [Read the Full Post]

Immune infiltration landscape on prognosis and therapeutic response and relevant epigenetic and transcriptomic mechanisms in lung adenocarcinoma

108 | Nov 18 2022

Liangming Zhang et al. found that EXO1 facilitated PD-L1 and sPD-L1 expression in LUAD cells. [Read the Full Post]

Multifunctional Polydopamine-Based Nanoparticles for Dual-Mode Imaging Guided Targeted Therapy of Lupus Nephritis

284 | Nov 16 2022

Mifang Li et al. found that Nec-1/PDA@Pt-Fe3O4 nanocarrier exhibited good biocompatibility. [Read the Full Post]

Ricolinostat suppresses proliferation, promotes apoptosis, and enhances the antiproliferative activity of topoisomerase inhibitors in cervical cancer cells

218 | Nov 14 2022

Sumeet Kaur et al. found that ricolinostat suppressed proliferation by inducing G2/M phase arrest and promoted apoptosis in cervical cancer cells, indicating that ricolinostat might be a promising antitumor agent in cervical cancer. [Read the Full Post]

Antithrombotic Effects of Fostamatinib in Combination with Conventional Antiplatelet Drugs

163 | Nov 11 2022

Maan H Harbi et al. found that the Syk inhibitor R406 provided mild inhibition of platelet responses induced by atherosclerotic plaque and that this was mildly amplified by aspirin and ticagrelor. [Read the Full Post]

Hedgehog Signaling as a Therapeutic Target for Airway Remodeling and Inflammation in Allergic Asthma

215 | Nov 10 2022

Anthony Tam et al. found that TGFβ1-induced airway remodeling was partially mediated through the hedgehog signaling pathway via the PTCH1-SMO-GLI axis. [Read the Full Post]

Chk1 and the Host Cell DNA Damage Response as a Potential Antiviral Target in BK Polyomavirus Infection

0 | Nov 07 2022

Lydia E Hainley et al. thought that Chk1 inhibitors that were found to be safe and effective in clinical trials for cancer should be evaluated for antiviral activity against BKPyV. [Read the Full Post]

Enterovirus A71 utilizes host cell lipid β-oxidation to promote its replication

141 | Nov 06 2022

Xiuwen Yang et al. found that it was the β-oxidation of lipid that plays a core role, not ER stress, which was only a concomitant change without restrictive effect, on virus replication. [Read the Full Post]

Ganetespib selectively sensitizes cancer cells for proximal and distal spread-out Bragg peak proton irradiation

371 | Oct 30 2022

Simon Deycmar et al. provided additional experimental data on cellular response and a rational for future combinatorial approaches with proton radiotherapy. [Read the Full Post]

Hsp90 Inhibitor STA9090 induced VPS35 related extracellular vesicle release and metastasis in hepatocellular carcinoma

222 | Oct 29 2022

Wenchong Tan et al. found that therapeutic strategy to inhibit the metastasis of HCC caused by N-terminal Hsp90 inhibitor induced extracellular vesicles. [Read the Full Post]

Poziotinib for EGFR exon 20-mutant NSCLC: Clinical efficacy, resistance mechanisms, and impact of insertion location on drug sensitivity

136 | Oct 27 2022

Yasir Y Elamin et al. found that poziotinib was active in EGFR exon 20-mutant NSCLC, although this activity was influenced by insertion location. [Read the Full Post]

A Protein Kinase D Inhibitor Suppresses AKT on T cells and Antagonizes Cancer Immunotherapy by Anti-PD-1

188 | Oct 26 2022

Kazuhide Miyamoto et al. thought that PKD was fundamentally required for T-cell reactivation by anti-PD-1, therefore inhibition of PKD was not appropriate for combination therapy with anti-PD-1. [Read the Full Post]

HER2 in Non-Small Cell Lung Cancer: A Review of Emerging Therapies

186 | Oct 26 2022

Natalie F Uy et al. summarized recent progress in novel HER2-targeted agents, and projected next steps in advancing treatment for the thousands of patients with HER2 altered NSCLC. [Read the Full Post]

Expression patterns and therapeutic implications of histone deacetylase-1 across carcinomas: a comprehensive molecular docking and MD simulation study

284 | Oct 24 2022

Bader Alshehri signified that targeting HDAC1 was a promising therapeutic strategy, and exploring novel therapeutic agents through basic, translational design might lead to their ultimate use in cancer prevention. [Read the Full Post]

Clinical and immune correlate results from a phase 1b study of the histone deacetylase inhibitor mocetinostat with ipilimumab and nivolumab in unresectable stage III/IV melanoma

242 | Oct 24 2022

Jeffrey S Weber et al. found that combining CPI and mocetinostat had favorable response rates but with high levels of toxicity. [Read the Full Post]

Delta-short consensus repeat 4-decay accelerating factor (DAF: CD55) inhibits complement-mediated cytolysis but not NK cell-mediated cytolysis

0 | Oct 21 2022

Shuji Miyagawa et al. thought that SCR2-4 was required but no relation to its complement regulatory function exists. [Read the Full Post]

Preclinical Test of Dacomitinib, an Irreversible EGFR Inhibitor, Confirms Its Effectiveness for Glioblastoma

0 | Oct 20 2022

Cristina Zahonero et al. found that dacomitinib clearly affected receptor signaling in vivo and that its strong antitumoral effect was independent of the presence of mutant receptor isoforms although it could be affected by the PTEN status [Read the Full Post]

Brain pharmacokinetics and metabolism of the AMP-activated protein kinase selective inhibitor SBI-0206965, an investigational agent for the treatment of glioblastoma

127 | Oct 16 2022

Janki M Desai et al. found that SBI-0206965 had adequate brain permeability but low relative oral bioavailability which might be due to rapid hepatic metabolism. [Read the Full Post]

Treatment-related adverse events of PD-1/PD-L1 inhibitors combined with CTLA-4 inhibitors in clinical trials: a meta-analysis

91 | Oct 16 2022

Ze Mi et al. thought that PD-L1 inhibitors plus CTLA-4 inhibitors showed better safety in treatment-related adverse events than PD-1 inhibitors plus CTLA-4 inhibitors. [Read the Full Post]

Vascular Disruptive Hydrogel Platform for Enhanced Chemotherapy and Anti-Angiogenesis through Alleviation of Immune Surveillance

110 | Oct 13 2022

Fasheng Li et al. provided a new treatment strategy through the mediation of the tumor immune microenvironment by vascular disruption to fulfill enhanced chemotherapy and immunotherapy. [Read the Full Post]

Aberrant cholesterol metabolic signaling impairs antitumor immunosurveillance through natural killer T cell dysfunction in obese liver

125 | Oct 13 2022

Wenshu Tang et al. found mTORC1/SREBP2/cholesterol-mediated NKT dysfunction in the tumor-promoting NAFLD liver microenvironment, providing intervention strategies that invigorating NKT cells to control HCC in the obesity epidemic. [Read the Full Post]

The Efficacy of Fosbretabulin Disodium Combined with Radiofrequency Ablation in Lung Cancer

133 | Oct 12 2022

Jieli Kou et al. found that FBTD promoted the antitumor effects of RFA in lung tumor-bearing mice in the study. [Read the Full Post]

Design, synthesis and biological evaluation of conformationnally-restricted analogues of E7010 as inhibitors of tubulin assembly (ITA) and vascular disrupting agents (VDA)

160 | Oct 12 2022

Vassili Prudhomme et al. found that indole 4j exhibited good potency against HUVEC and HIG-82 cell lines, as well as a good ability to inhibit tubulin assembly. [Read the Full Post]

Int J Oncol . 2022 Oct;61(4):114. doi: 10.3892/ijo.2022.5404. Epub 2022 Aug 3. Targeting PIM2 by JP11646 results in significant antitumor effects in solid tumors

440 | Oct 04 2022

Eriko Katsuta et al. found that JP11646 may thus be a possible treatment strategy for multiple types of solid cancers. [Read the Full Post]

BCL-XL inhibition induces an FGFR4-mediated rescue response in colorectal cancer

165 | Oct 03 2022

Prashanthi Ramesh et al. found a cell transferable induction of a FGF2/FGFR4 rescue response in CRC that was induced upon BCL-XL inhibition and lead to MCL-1 upregulation. [Read the Full Post]

RIPK3 inhibitor-AZD5423 alleviates acute kidney injury by inhibiting necroptosis and inflammation

124 | Oct 01 2022

Chuan-Hui Xu et al. found that AZD5423 may serve as a potent inhibitor of RIPK3 kinase and a promising clinical candidate for AKI treatment. [Read the Full Post]

Co-targeting of BAX and BCL-XL proteins broadly overcomes resistance to apoptosis in cancer

64 | Oct 01 2022

Andrea Lopez et al. advanced the understanding of apoptosis resistance mechanisms and demonstrate a novel therapeutic strategy for cancer treatment. [Read the Full Post]

Temsirolimus Enhances Anti-Cancer Immunity by Inducing Autophagy-Mediated Degradation of the Secretion of Small Extracellular Vesicle PD-L1

277 | Sep 29 2022

Seong-Sik Park et al. suggested that TEM, previously known as a targeted anti-cancer drug, could overcome the low reactivity of ICBT by inhibiting sEV PD-L1 and cellular PD-L1 levels. [Read the Full Post]

FACT subunit SUPT16H associates with BRD4 and contributes to silencing of interferon signaling

145 | Sep 28 2022

Dawei Zhou et al. demonstrated that depletion or inhibition of SUPT16H caused the remarkable activation of IFN signaling in NK cells, which promoted the NK-mediated killing of virus-infected cells in a co-culture system using human primary NK cells. [Read the Full Post]

In silico drug repurposing and lipid bilayer molecular dynamics puzzled out potential breast cancer resistance protein (BCRP/ABCG2) inhibitors

193 | Sep 28 2022

Nahlah Makki Almansour et al. identified zotarolimus, temsirolimus and glecaprevir as auspicious anti-MDR drug leads that warrant further experimental assays. [Read the Full Post]

Subtype and site specific-induced metabolic vulnerabilities in prostate cancer

176 | Sep 27 2022

Federica Mossa et al. thought that castration-resistant ARPC and AVPC exhibited different metabolic dependencies, which could further undergo metabolic reprogramming in bone. [Read the Full Post]

Arylamine N-acetyltransferase 1 deficiency inhibits drug-induced cell death in breast cancer cells: switch from cytochrome C-dependent apoptosis to necroptosis

106 | Sep 18 2022

Courtney E McAleese et al. found NAT1 deficiency could switch cell death from apoptosis to necroptosis resulting in decreased response to cytotoxic drugs. [Read the Full Post]

[Correlation between low expression of Hsp90 protein in keratinocytes and the number of small extracellular vesicles and its potential clinical significance]

368 | Sep 17 2022

Jun Chen et al. found that the secretion of sEVs in HaCaT cells. sEVs may be involved in the transfer of molecules between epithelial cells and immune cells. [Read the Full Post]

Identification of potential immunotherapy biomarkers for breast cancer by bioinformatics analysis

366 | Sep 16 2022

Yao Song et al. found that CD24, MMP1, SDC1, and SPP1 were potentially associated with five immune cell types infiltration (CD8+ T cells, CD4+ T cells, neutrophils, macrophages,and dendritic cells) by TIMER. [Read the Full Post]

Randomized, Double-Blind, Placebo-Controlled Phase III Study of Paclitaxel ± Napabucasin in Pretreated Advanced Gastric or Gastroesophageal Junction Adenocarcinoma

136 | Sep 14 2022

Manish A Shah et al. showed that adding napabucasin to paclitaxel did not improve survival in patients with pretreated advanced gastric or GEJ adenocarcinoma. [Read the Full Post]

p53 positively regulates the proliferation of hepatic progenitor cells promoted by laminin-521

148 | Sep 13 2022

Mingyang Ma et al. identified LN-521 as an ideal candidate substrate for HPC culture and uncovered an unexpected positive role for p53 in regulating proliferation of HPCs, which made it a potential target for HPC-based regenerative medicine. [Read the Full Post]

First-in-Class Hydrazide-Based HDAC6 Selective Inhibitor with Potent Oral Anti-Inflammatory Activity by Attenuating NLRP3 Inflammasome Activation

150 | Sep 13 2022

Kairui Yue et al. indicated that 35m could be a potential orally active therapeutic agent for the treatment of NLRP3-related diseases. [Read the Full Post]

Pharmacokinetic/pharmacodynamic modeling of roxadustat's effect on LDL cholesterol in patients in Japan with dialysis-dependent chronic kidney disease and anemia

137 | Sep 12 2022

Akitsugu Takada found that roxadustat could decrease LDL-C independent of statins and sevelamer. [Read the Full Post]

Histone methyltransferase MLL1 drives renal tubular cell apoptosis by p53-dependent repression of E-cadherin during cisplatin-induced acute kidney injury

114 | Sep 12 2022

Chunyun Zhang et al. identified MLL1 as a novel DDR regulator that drived cisplatin-induced RPTC apoptosis and AKI by modulating the MLL1/WDR5-/ATR/ATM-Chk-p53-E-cadherin axis. [Read the Full Post]

Target of rapamycin (TOR) regulates the response to low nitrogen stress via autophagy and hormone pathways in Malus hupehensis

142 | Sep 11 2022

Danyang Li et al. found that appropriate inhibition of TOR activated autophagy and jasmonic acid signaling in M. hupehensis, which allowed plants to cope with low N stress. [Read the Full Post]

CRNDE acts as an epigenetic modulator of the p300/YY1 complex to promote HCC progression and therapeutic resistance

281 | Sep 11 2022

Yu-Chin Liu et al. supported the potential of targeting the CRNDE/p300/YY1 axis as a novel therapeutic strategy to overcome sorafenib resistance of HCC. [Read the Full Post]

Liproxstatin‑1 induces cell cycle arrest, apoptosis, and caspase‑3/GSDME‑dependent secondary pyroptosis in K562 cells

31 | Sep 07 2022

Hai-Qun Dong et al. found that liproxstatin‑1 induced cell cycle arrest, apoptosis, and caspase‑3/GSDME‑dependent secondary pyroptosis in K562 leukemia cells, which provided new hope for the treatment of leukemia. [Read the Full Post]

Repeated treatments of Capan-1 cells with PARP1 and Chk1 inhibitors promote drug resistance, migration and invasion

165 | Sep 06 2022

Ne Guo et al. found that activating CXCL3-ERK1/2 signaling might contribute to the enhanced migratory capabilities rather than the acquired drug resistance. [Read the Full Post]

Non-small cell lung cancer with EGFR exon 20 insertion mutation: a systematic literature review and meta-analysis of patient outcomes

312 | Sep 05 2022

Christina Soeun Kwon et al. found EGFR exon 20 insertion mutations as the availability of new targeted treatments might offer additional therapeutic options to these patients. [Read the Full Post]

A Low Membrane Hsp70 Expression in Tumor Cells With Impaired Lactate Metabolism Mediates Radiosensitization by NVP-AUY922

290 | Sep 05 2022

Melissa Schwab et al. found that the membrane Hsp70 density, but not cytosolic HSP levels determined the radiosensitizing effect of the Hsp90 inhibitor NVP-AUY922 in LDH-/- cells. [Read the Full Post]

Drug Repurposing Based on Protozoan Proteome: In Vitro Evaluation of In Silico Screened Compounds against Toxoplasma gondii

137 | Aug 27 2022

Débora Chaves Cajazeiro et al. found that interactions with the Na+/K+ ATPase transporter for Homo sapiens and Mus musculus, indicating a possible mechanism of action of this compound. [Read the Full Post]

MiR-630 suppresses non-small cell lung cancer by targeting vimentin

169 | Aug 26 2022

Bin Wang et al. thought that MiR-630 constrained the progression of NSCLC by inhibiting JAK2/STAT3 pathway and downregulating VIM expression. [Read the Full Post]

Alpha1B-adreneroceptor is involved in norepinephrine-induced pulmonary artery smooth muscle cell proliferation via p38 signaling

153 | Aug 22 2022

Xiaolin Xiao et al. suggested that α1B-AR was involved in NE-induced PASMCs proliferation via p38 signaling pathway, which might be downstream of α1B-AR. [Read the Full Post]

Atezolizumab, vemurafenib, and cobimetinib in patients with melanoma with CNS metastases (TRICOTEL): a multicentre, open-label, single-arm, phase 2 study

262 | Aug 17 2022

Reinhard Dummer et al. evaluated atezolizumab in combination with cobimetinib or vemurafenib plus cobimetinib in patients with melanoma with CNS metastases. [Read the Full Post]

Small Molecule Inhibitors of MERTK and FLT3 Induce Cell Cycle Arrest in Human CD8 + T Cells

167 | Aug 15 2022

Richard M Powell et al. found that caution was needed when using potent RTKIs in the context of antitumor immune responses. [Read the Full Post]

A truncated derivative of FGFR1 kinase cooperates with FLT3 and KIT to transform hematopoietic stem cells in syndromic and de novo AML

171 | Aug 14 2022

Baohuan Cai et al. demonstrated a novel model for transformation of hematopoietic stem cells by chimeric FGFR1 kinases with the combined effects of direct protein activation by the full-length kinases and transcriptional regulation by the truncated nuclear tnFGFR1 derivative. [Read the Full Post]

The CBP/β-Catenin Antagonist, ICG-001, Inhibits Tumor Metastasis via Blocking of the miR-134/ITGB1 Axis-Mediated Cell Adhesion in Nasopharyngeal Carcinoma

170 | Aug 11 2022

Luo Chen et al. showed that ICG-001 transient overexpression of miR-134 or stable overexpression of miR-134 could significantly reduce the lung metastasis of NPC cells. [Read the Full Post]

Effect of ALA-PDT on inhibition of oral precancerous cell growth and its related mechanisms

193 | Aug 09 2022

Jian-Qiu Jin et al. indicated that ALA-PDT could be a promising alternative treatment against oral precancerous lesions. [Read the Full Post]

Casein Kinase 2 Signaling in White Matter Stroke

415 | Aug 04 2022

Hung Nguyen et al. thought that miRNA regulation might be one of the protective actions of CX-4945 against WM ischemic injury. [Read the Full Post]

Anti-adipogenic and Pro-lipolytic Effects on 3T3-L1 Preadipocytes by CX-4945, an Inhibitor of Casein Kinase 2

399 | Aug 04 2022

Anil Kumar Yadav et al. found that CX-4945 had strong anti-adipogenic and pro-lipolytic effects on differentiating and differentiated 3T3-L1 cells, mediated by control of the expression and phosphorylation levels of CK2, C/EBP-α, PPAR-γ, FAS, ACC, perilipin A, AMPK, LKB-1, ERK-1/2, and HSL. [Read the Full Post]

A Novel Defined Pyroptosis-Related Gene Signature for Predicting Prognosis and Treatment of Glioma

125 | Aug 03 2022

Zhihao Yang et al. thought that pyroptosis-related genes were of great significance for performing prognostic stratification and developing treatment strategies for glioma. [Read the Full Post]

Nanodevices for the Efficient Codelivery of CRISPR-Cas9 Editing Machinery and an Entrapped Cargo: A Proposal for Dual Anti-Inflammatory Therapy

117 | Aug 03 2022

Alba García-Fernández et al. found the potential of MSNs as a versatile platform by allowing multiple combinations for gene editing and drug therapy to prepare advanced nanodevices to meet possible biomedical needs. [Read the Full Post]

Comprehensive genome profiling in patients with metastatic non-small cell lung cancer: the precision medicine phase 2 randomized SAFIR02-Lung trial

159 | Aug 01 2022

Fabrice Barlesi et al. thought that molecular profiling could feasibly be implemented to guide treatment choice for the maintenance strategy in EGFR/ALK wt NSCLC. [Read the Full Post]

Murine Double Minute 2 Antagonist Nutlin-3 Enhanced Chemosensitivity in Esophageal Squamous Cell Carcinoma

200 | Jul 31 2022

Ken Ito et al. found that the combination of nutlin-3 with chemotherapeutic agents might become a novel therapeutic strategy in esophageal cancer over-expressing MDM2. [Read the Full Post]

Hesperidin Protects Human HaCaT Keratinocytes from Particulate Matter 2.5-Induced Apoptosis via the Inhibition of Oxidative Stress and Autophagy

509 | Jul 30 2022

Pincha Devage Sameera Madushan Fernando et al. found that hesperidin showed therapeutic potential against PM2.5-induced skin damage by mitigating excessive ROS accumulation, autophagy, and apoptosis. [Read the Full Post]

Amplification of CDK4 and MDM2: a detailed study of a high-risk neuroblastoma subgroup

189 | Jul 29 2022

Angela Martinez-Monleon et al. presented detailed biological data of an aggressive neuroblastoma subgroup hallmarked by 12q amplification and atypical clinical presentation for which in vitro studies indicated that CDK4 and/or MDM2 inhibition also could be beneficial. [Read the Full Post]

BKM120 alters the migration of doublecortin-positive cells in the dentate gyrus of mice

119 | Jul 28 2022

Yeonggwang Hwang et al. suggested that the altered migration of adult-born neurons in the dentate gyrus played a role in mood disturbances. [Read the Full Post]

RB loss determines selective resistance and novel vulnerabilities in ER-positive breast cancer models

193 | Jul 27 2022

Vishnu Kumarasamy et al. demonstrated the highly selective use of birinapant based combinations for the treatment of RB-deficient tumors. [Read the Full Post]

Patient-derived models of brain metastases recapitulate human disseminated disease

97 | Jul 27 2022

Claudia C Faria et al. thought that models of BMs recapitulated the biology of human metastatic disease and could be valuable translational platforms for precision medicine. [Read the Full Post]

Inhibiting PI3K-AKT-mTOR Signaling in Multiple Myeloma-Associated Mesenchymal Stem Cells Impedes the Proliferation of Multiple Myeloma Cells

227 | Jul 25 2022

Luca Heinemann et al. found that targeting PI3K-AKT-mTOR signaling in MSCs might represent an additional therapeutic pathway in the treatment of MM patients. [Read the Full Post]

GDC-0941 activates integrin linked kinase (ILK) expression to cause resistance to GDC-0941 in breast cancer by the tumor necrosis factor (TNF)-α signaling pathway

160 | Jul 25 2022

Haifeng Chen et al. thought that GDC-0941 increased ILK level by upregulating TNF-α, thus affecting AKT expression and the sensitivity of breast cancer cells to GDC-0941. [Read the Full Post]

Clostridioides difficile toxin B alone and with pro-inflammatory cytokines induces apoptosis in enteric glial cells by activating three different signalling pathways mediated by caspases, calpains and cathepsin B

187 | Jul 24 2022

Katia Fettucciari et al. demonstrated that TcdB induced caspase-dependent, mitochondria-independent enteric glial cell (EGC) apoptosis that was enhanced by the pro-inflammatory cytokines TNF-α and IFN-γ (CKs) by increasing caspase-3/7/9 and PARP activation. [Read the Full Post]

Construction of m6A-Related lncRNA Prognostic Signature Model and Immunomodulatory Effect in Glioblastoma Multiforme

340 | Jul 22 2022

Pan Xie et al. constructed an m6A-associated lncRNA risk model to predict the prognosis of GBM patients and provided new ideas for the treatment of GBM. [Read the Full Post]

Genome-wide CRISPR/Cas9 screening for therapeutic targets in NSCLC carrying wild-type TP53 and receptor tyrosine kinase genes

190 | Jul 22 2022

Qianqian Wang et al. identified MDM2 as an essential gene and a potential therapeutic target in wtTP53-RTK NSCLC via a genome-wide CRISPR/Cas9 screening. [Read the Full Post]

Compassionate Use of Ripretinib for Patients With Metastatic Gastrointestinal Stromal Tumors: Taiwan and Hong Kong Experience

443 | Jul 20 2022

Li-Ching Lin et al. thought that ripretinib was generally tolerable, with loss of hair being the most common AE. [Read the Full Post]

Simulating Colorectal Cancer Trials Using Real-World Data

350 | Jul 18 2022

Zhaoyi Chen et al. simulated five CRC trials, and tested two simulation scenarios with several different configurations demonstrated that our simulations couldrobustly generated effectiveness and safety outcomes comparable with the original trials using real-world data. [Read the Full Post]

Multicenter phase II, double-blind placebo-controlled trial of maintenance ixazomib after allogeneic transplantation for high-risk multiple myeloma: Results of the BMT CTN 1302 Trial

358 | Jul 17 2022

Qaiser Bashir et al. found the safety and durable disease control with allo-HCT in high-risk myeloma patients. [Read the Full Post]

Machine Learning Screens Potential Drugs Targeting a Prognostic Gene Signature Associated With Proliferation in Hepatocellular Carcinoma

240 | Jul 16 2022

Jun Liu et al. found that the five-gene signature associated with proliferation can be used for survival prediction and risk stratification for HCC patients. Potential drugs targeting this gene signature deserve further attention in the treatment of HCC. [Read the Full Post]

Parp Inhibition and Beyond in Brca- Associated Breast Cancer in Women: A State- Of- The- Art Summary of (Pre) - Clinical Research into Risk Reduction and Clinical Benefits

129 | Jul 15 2022

Ernest K J Pauwels et al. described the various causes of PARP inhibitor resistance as well as the research that indicated how to overcome phenomenon. [Read the Full Post]

STAT3-mediated ferroptosis is involved in ulcerative colitis

203 | Jul 11 2022

Fangfang Huang et al. suggested that ferroptosis was closely associated with the development of colitis and ferroptosis-related gene STAT3 could serve as a potential biomarker for diagnosis and treatment of ulcerative colitis. [Read the Full Post]

Novel Iron Oxide Nanoparticles Induce Ferroptosis in a Panel of Cancer Cell Lines

100 | Jul 10 2022

Roberto Fernández-Acosta et al. reported on novel ferroptosis-inducing iron encapsulated nanoparticles with potent anti-cancer properties, which had promising potential for further in vivo validation. [Read the Full Post]

Shedding light on the binding mechanism of kinase inhibitors BI-2536, Volasetib and Ro-3280 with their pharmacological target PLK1

193 | Jul 08 2022

Jesús Fernández-Sainz et al. thought that the higher affinity of the inhibitors to PLK1 compared to ATP was mainly attributed to stronger van der Waals interactions. [Read the Full Post]

Predictive role of CD36 expression in HER2-positive breast cancer patients receiving neoadjuvant trastuzumab

301 | Jul 08 2022

Francesca Ligorio et al. thought that high CD36 expression predicted worse clinical outcomes in early-stage HER2+ BC treated with trastuzumab-based neoadjuvant therapy. [Read the Full Post]

PLK inhibitors identified by high content phenotypic screening promote maturation of human PSC-derived cardiomyocytes

194 | Jul 07 2022

Mengying Feng et al. found that PLK inhibitors could promote maturation of hPSC-CMs through suppressing AKT signaling pathway. [Read the Full Post]

Carfilzomib plus dexamethasone in patients with relapsed and refractory multiple myeloma: a retro-prospective observational study

283 | Jul 04 2022

Maria Livia Del Giudice et al. thought that Kd56 was an effective and well tolerated regimen in highly pretreated and elderly patients with a good safety profile. [Read the Full Post]

The impact of emricasan on chronic liver diseases: current data

209 | Jul 03 2022

Vasileios Lekakis et al. showed that as emricasan treatment appeared safe and well-tolerated, irrespective the severity of liver disease, more studies were required to clarify better these subgroups of patients who might benefit most from this drug. [Read the Full Post]

Single-Molecule Sensing of an Anticancer Therapeutic Protein-Protein Interaction Using the Chemically Modified OmpG Nanopore

139 | Jul 02 2022

Hye-Jin Hwang et al. found that the chemically modified OmpG nanopore can serve as a valuable sensor platform for ultrasensitive, rapid, and single-molecule-based drug screening against protein-protein interactions, which are therapeutic targets for various diseases. [Read the Full Post]

Class Ⅰ histone deacetylase inhibitor regulate of Mycobacteria-Driven guanylate-binding protein 1 gene expression

339 | Jul 01 2022

Meili Wei et al. showed that the CpG site of the GBP1 promoter was hypermethylated, and the methylation status of the GBP1 promoter did not change significantly upon Mtb infection. [Read the Full Post]

Caspase-3-induced activation of SREBP2 drives drug resistance via promotion of cholesterol biosynthesis in hepatocellular carcinoma

272 | Jul 01 2022

Etienne H Mok et al. demonstrated that CSC populations in HCC expanded via CASP3-dependent, SREBP2-mediated cholesterol biosynthesis in response to tyrosine kinase inhibitor therapy and that targeting cholesterol biosynthesis could overcome acquired drug resistance. [Read the Full Post]

Tumor-targeted interleukin-12 synergizes with entinostat to overcome PD-1/PD-L1 blockade-resistant tumors harboring MHC-I and APM deficiencies

383 | Jun 30 2022

Christine M Minnar et al. demonstrated that the combination of entinostat and NHS-IL12 therapy elicited potent antitumor activity. [Read the Full Post]

Immunogenic Cell Death and Immunomodulatory Effects of Cabozantinib

357 | Jun 27 2022

Fabio Scirocchi et al. reported that Cabozantinib might exert an immunostimulatory role by inducing immunogenic stress of prostate cancer cells and directly modulating dendritic cells (DCs). [Read the Full Post]

Repression of HIV-1 reactivation mediated by CRISPR/dCas9-KRAB in lymphoid and myeloid cell models

460 | Jun 26 2022

Lendel Correia da Costa et al. demonstrated that KRAB repressor protein was crucial to reactivation resistance phenotype. [Read the Full Post]

Histone Deacetylase Inhibitors Counteract CGRP Signaling and Pronociceptive Sensitization in a Rat Model of Medication Overuse Headache

382 | Jun 26 2022

Matteo Urru et al. provided evidence for a key role of HDACs and epigenetics in MOH pathogenesis, highlighting the therapeutic potential of HDAC inhibition in the prevention of migraine chronification. [Read the Full Post]

Survival benefit of using pemetrexed for EGFR mutation-positive advanced non-small-cell lung cancer in a randomized phase III study comparing gefitinib to cisplatin plus docetaxel (WJTOG3405)

286 | Jun 23 2022

Naoki Haratake et al. thought that pemetrexed should be administered without fail as a sequential treatment to improve the prognosis of EGFR-mutated NSCLC as well as like EGFR-tyrosine kinase inhibitors. [Read the Full Post]

Discovery of novel targets and mechanisms of MEK inhibitor Selumetinib for LGG treatment based on molecular docking and molecular dynamics simulation

212 | Jun 22 2022

Dongdong Zhang et al. thought that CDK2 might be a new direction of Selumetinib in the clinical treatment of LGG. [Read the Full Post]

The efficacy and safety of selumetinib as secondary therapy for late-stage and metastatic non-small cell lung cancer: results from a systematic review and meta-analysis

324 | Jun 21 2022

Wei-Wei Wang et al.showed that the efficacy of selumetinib was not superior compared to combined therapy for treating NSCLC but did have a better safety profile. [Read the Full Post]

BAK plays a key role in A-1331852-induced apoptosis in senescent chondrocytes

122 | Jun 20 2022

Guihao Wu et al. found that A-1331852 selectively promoted apoptosis in senescent chondrocytes by interfering with the interaction between Bcl-xL and BAK. [Read the Full Post]

Tenofovir alafenamide prophylaxis post-liver transplantation: a real-world study in patients with chronic kidney disease

408 | Jun 19 2022

E Sinakos et al. found that conversion to TAF in post-LT patients who develop CKD did not lead to improvement of kidney function after a period of one year. [Read the Full Post]

Aurora kinase a inhibitor MLN8237 suppresses pancreatic cancer growth

288 | Jun 15 2022

Yuebo Zhang et al. provided the molecular basis for a novel chemotherapy strategy for PDAC patients. [Read the Full Post]

Phase II study of alisertib as a single agent for treating recurrent or progressive atypical teratoid/rhabdoid tumor

277 | Jun 14 2022

Santhosh A Upadhyaya et al. discovered that single agent alisertib was well tolerated by children with recurrent AT/RT, and SD or PR was observed in approximately a third of the patients. [Read the Full Post]

Systematic Evaluation for the Influences of the SOX17/Notch Receptor Family Members on Reversing Enzalutamide Resistance in Castration-Resistant Prostate Cancer Cells

438 | Jun 12 2022

Zhongbo Du et al. thought that the Notch1 and Notch4 inhibitors GSI-IX and RO4929097 were promising therapeutic agents for the treatment of CRPC. [Read the Full Post]

Antithrombotic Therapy in Elderly Patients with Acute Coronary Syndromes

480 | Jun 11 2022

Clara Bonanad et al. it is imperative to deepen our knowledge regarding the management of these challenging patients through real-world data and specifically designed geriatric studies to help resolve the questions remaining in their disease management. [Read the Full Post]

Exposure to escalating olaparib does not induce acquired resistance to PARPi and to other chemotherapeutic compounds in ovarian cancer cell lines

325 | Jun 10 2022

André Fedier et al. found that olaparib exposure was unlikely to produce an acquired resistance phenotype and that PARPi‑sensitive ovarian cancer cells were also cross‑sensitive to non‑platinum and even to compounds not directly interacting with the DNA. [Read the Full Post]

ARHGAP9 inhibits colorectal cancer cell proliferation, invasion and EMT via targeting PI3K/AKT/mTOR signaling pathway

746 | Jun 10 2022

Jufeng Sun et al. thought that ARHGAP9 inhibited the malignant phenotypes of CRC cells via interdicting PI3K/AKT/mTOR signaling pathway. [Read the Full Post]

Disclosing Potential Key Genes, Therapeutic Targets and Agents for Non-Small Cell Lung Cancer: Evidence from Integrative Bioinformatics Analysis

383 | Jun 09 2022

Md Parvez Mosharaf et al. validated six FDA-approved launched drugs (Dinaciclib, Afatinib, Icotinib, Bosutinib, Dasatinib, and TWS-119) by molecular docking interaction analysis with the respective target proteins for the treatment against NSCLC. [Read the Full Post]

Inhibitory Response to CK II Inhibitor Silmitasertib and CDKs Inhibitor Dinaciclib Is Related to Genetic Differences in Pancreatic Ductal Adenocarcinoma Cell Lines

232 | Jun 09 2022

Yixuan Ma et al. thought that specific aberrations in TP53 and KRAS affected the efficacy of both inhibitors. [Read the Full Post]

Lonafarnib Inhibits Farnesyltransferase via Suppressing ERK Signaling Pathway to Prevent Osteoclastogenesis in Titanium Particle-Induced Osteolysis

240 | Jun 07 2022

Linke Huang et al. found that Lon was a promising treatment option for osteoclast-related osteolysis diseases including periprosthetic osteolysis by targeted inhibition of FTase through suppressing ERK signaling. [Read the Full Post]

Acid-Responsive Micelles Releasing Cinnamaldehyde Enhance RSL3-Induced Ferroptosis in Tumor Cells

243 | Jun 06 2022

Ziliang Yan et al. confirmed that RSL3@PCA has excellent inhibition of tumor growth without significant toxicity to normal cells and tissues and still has a good therapeutic effect on tumor cells that are resistant to conventional chemotherapy drugs. [Read the Full Post]

Congenital sideroblastic anemia model due to ALAS2 mutation is susceptible to ferroptosis

225 | Jun 05 2022

Koya Ono et al. found that defective heme biosynthesis in XLSA clones could confer enhanced BACH1 expression, leading to increased susceptibility to ferroptosis. [Read the Full Post]

Dihydroquercetin Attenuates Silica-Induced Pulmonary Fibrosis by Inhibiting Ferroptosis Signaling Pathway

344 | Jun 02 2022

Leyong Yuan et al. found that inhibition of ferritinophagy-mediated HBE cells ferroptosis was responsible for DHQ to ameliorate SiO2-induced lung fibrosis, which provided a preliminary theoretical basis for the clinical application of DHQ in the treatment of silicosis. [Read the Full Post]

LAMP2-regulates-autophagy-in-the-thymic-epithelium-and-thymic-stroma-dependent-CD4-T-cell-development

331 | May 31 2022

Pedro M Rodrigues et al. suggested that LAMP2 interconnected the autophagy-lysosomal axis and the processing of selecting self-peptides:MHC II complexes in cTECs, underling its implications for the generation of a broad CD4 TCR repertoire. [Read the Full Post]

The role of autophagy in cadmium-induced acute toxicity in glomerular mesangial cells and tracking polyubiquitination of cytoplasmic p53 as a biomarker

306 | May 30 2022

Ki-Tae Jung et al. indicated that cytoplasmic polyUb-p53 was a potential biomarker for Cd-induced acute toxicity in mesangial cells. [Read the Full Post]

Evaluation of mitochondrial oxidative toxicity in mammalian cardiomyocytes by determining the highly reproducible and reliable increase in mitochondrial superoxides after exposure to therapeutic drugs

636 | May 27 2022

Dohee Ahn et al. found that a screening system using MitoSOX™ had the potential to be applied as a reliable biomarker for determining mitochondrial oxidative toxicity in new drug development. [Read the Full Post]

Vasorelaxant effect of curcubisabolanin A isolated from Curcuma longa through the PI3K/Akt/eNOS signaling pathway

336 | May 25 2022

Jin-Feng Chen et al. demonstrated that the vasorelaxant effect of curcubisabolanin A was partially endothelium-dependent. [Read the Full Post]

Rutaecarpine Attenuates Oxidative Stress-Induced Traumatic Brain Injury and Reduces Secondary Injury via the PGK1/KEAP1/NRF2 Signaling Pathway

264 | May 24 2022

Min Xu et al. showed that rutaecarpine might be a promising therapeutic agent for the treatment of TBI-related neuro-oxidative damage. [Read the Full Post]

Enhancing Radioiodine Incorporation Into Radio Iodine Refractory Thyroid Cancer With MAPK Inhibition (ERRITI): A Single-Center Prospective Two-Arm Study

315 | May 22 2022

Manuel Weber et al. found that genotype-guided MAPK inhibition was safe and resulted in successful redifferentiation in about one third of patients in each arm. [Read the Full Post]

Blue Light Induces RPE Cell Necroptosis, Which Can Be Inhibited by Minocycline

181 | May 22 2022

Weilin Song et al. provided new ideas for the pathogenesis and treatment of retinal degeneration. [Read the Full Post]

Abrocitinib: A New FDA-Approved Drug for Moderate-to-Severe Atopic Dermatitis

670 | May 20 2022

Patrick O Perche et al. thought that abrocitinib was an efficacious oral JAK 1 inhibitor recently FDA-approved for patients ≥ 18 years old with moderate-to-severe AD who had not responded to systemic medications or when contraindicated otherwise. [Read the Full Post]

CSF-1R inhibitor, pexidartinib, sensitizes esophageal adenocarcinoma to PD-1 immune checkpoint blockade in a rat model

716 | May 19 2022

Ashten N Omstead et al. showed limited toxicity with significant tumor shrinkage in pexidartinib treated animals compared to controls, single agent and in combination with a PD-1 inhibitor, AUNP-12. [Read the Full Post]

Targeting Apoptosis in ALL

281 | May 17 2022

Wesley M Smith et al. showed that ALL depended on the BCL-2 family of proteins for cell survival and proliferation. [Read the Full Post]

Addition of navitoclax to ongoing ruxolitinib treatment in patients with myelofibrosis (REFINE): a post-hoc analysis of molecular biomarkers in a phase 2 study

147 | May 17 2022

Naveen Pemmaraju et al. revealed clinically meaningful splenic responses independent of high molecular risk mutation status in patients treated with navitoclax plus ruxolitinib who were not benefiting from ruxolitinib monotherapy. [Read the Full Post]

Targeting PI3K/AKT/mTOR pathway to enhance the anti-leukemia efficacy of venetoclax

240 | May 15 2022

Hongcai Liu et al. found that the combination of BEZ235 and ABT199 exhibited a synergistic anti-tumor effect in AML by down-regulating MCL-1 protein. [Read the Full Post]

Inside the cracked kernel: establishing the molecular basis of AMG510 and MRTX849 in destabilising KRASG12C mutant switch I and II in cancer treatment

361 | May 14 2022

Abdul Rashid Issahaku et al. found that these insights present useful atomistic perspectives into the success of AMG510 and MRTX849 which could guide the design of more selective and potent KRAS inhibitors.Communicated by Ramaswamy H. Sarma. [Read the Full Post]

Non-cytomembrane PD-L1: An atypical target for cancer

406 | May 12 2022

Honggang Ying et at. highlighted that non-cytomembrane PD-L1s were of significant cancer diagnostic value and were promising therapeutic targets to treat cancer. [Read the Full Post]

Effects of Elexacaftor/Tezacaftor/Ivacaftor Therapy on Lung Clearance Index and Magnetic Resonance Imaging in Patients with Cystic Fibrosis and One or Two F508del Alleles

380 | May 12 2022

Simon Y Graeber et al. found that improvement of CFTR function by ELX/TEZ/IVA improved lung ventilation and abnormalities in lung morphology including airway mucus plugging and wall thickening in adolescent. [Read the Full Post]

Inhibitory Effect of a Glutamine Antagonist on Proliferation and Migration of VSMCs via Simultaneous Attenuation of Glycolysis and Oxidative Phosphorylation

0 | May 11 2022

Hyeon Young Park et al. suggested that treatment with a glutamine antagonist was a promising approach to prevent progression of atherosclerosis and restenosis. [Read the Full Post]

Proton pump inhibitors may reduce the efficacy of ribociclib and palbociclib in metastatic breast cancer patients based on an observational study

411 | May 09 2022

Kadir Eser et al. found that concomitant usage of PPIs was associated with shorter PFS in mBC treated with both ribociclib and especially palbociclib. [Read the Full Post]

Design, Synthesis, and Antitumor Activity of Erlotinib Derivatives

634 | May 08 2022

Long-Fei Mao et al. suggested that compound 3d suppressed cancer cell proliferation through the EGFR-TK pathway. [Read the Full Post]

Regorafenib induces the apoptosis of gastrointestinal cancer-associated fibroblasts by inhibiting AKT phosphorylation

353 | May 07 2022

Mingjia Zhang et al. found that regorafenib inhibited the proliferation of CAFs and induced the apoptosis of CAFs in vitro. [Read the Full Post]

Tumor acidity/redox hierarchical-activable nanoparticles for precise combination of X-ray-induced photodynamic therapy and hypoxia-activated chemotherapy

459 | May 07 2022

Beibei Zhang et al. developed a combined therapeutic modality based on an intelligent nanosized platform (DATAT-NPVT) with tumor acidity-activated TAT presenting. [Read the Full Post]

[Ocular toxicity of targeted therapies with MEK inhibitors and BRAF inhibitors in the treatment of metastatic cutaneous melanoma]

435 | May 06 2022

E Fauviaux et al. found that a multidisciplinary approach including ophthalmologists, dermatologists and oncologists was essential in order to adapt treatment in the advent of the ocular complications. [Read the Full Post]

How Immunotherapy Modified the Therapeutic Scenario of Endometrial Cancer: A Systematic Review

472 | May 06 2022

Brigida Anna Maiorano et al. found that ICIs represented an effective option for pretreated advanced EC patients with a tolerable profile. [Read the Full Post]

Longitudinal monitoring of STAT3 phosphorylation and histologic outcome of tofacitinib therapy in patients with ulcerative colitis

417 | May 01 2022

Bram Verstockt et al. showed that Longitudinal monitoring of nuclear pSTAT3 in mucosal tissue compartments reflected distinctive on-target effects, independently of long-term treatment outcomes. [Read the Full Post]

Utilizing Three-Dimensional Culture Methods to Improve High-Throughput Drug Screening in Anaplastic Thyroid Carcinoma

347 | Apr 29 2022

Kensey Bergdorf et al. utilized three-dimensional culture methods, as they had been shown to more accurately recapitulate tumor responses in vivo. [Read the Full Post]

Long-Term Outcomes of Targeted Therapy after First-Line Immunotherapy in BRAF-Mutated Advanced Cutaneous Melanoma Patients-Real-World Evidence

243 | Apr 28 2022

Paweł Rogala et al. found that BRAFi/MEKi therapy was effective in the second-line in advanced and metastatic melanoma patients. [Read the Full Post]

Unique Presentation of Bortezomib-Associated Thrombotic Microangiopathy Responsive to Therapeutic Plasma Exchange and Eculizumab Therapy

406 | Apr 27 2022

Robert C Sterner et al. demonstrated the possible utility of TPE with plasma replacement. [Read the Full Post]

Long non-coding RNA ATXN8OS Promotes Ferroptosis and Inhibits the Temozolomide-resistance of Gliomas Through the ADAR/GLS2 Pathway

392 | Apr 26 2022

Jin Luo et al. found that ATXN8OS mediated ferroptosis and regulated the TMZ-resistance of glioma via ADAR/GLS2 pathway. [Read the Full Post]

Treatment of a Double Cancer Patient With Primary Inferior Vena Cava Sarcoma and Lung Adenocarcinoma: A Case Report and Literature Review

334 | Apr 26 2022

Xiaohu Guo et al. found that surgery was still an effective treatment for patients with a primary IVC leiomyosarcoma and lung adenocarcinoma at present. [Read the Full Post]

Proangiogenesis effects of compound danshen dripping pills in zebrafish

285 | Apr 24 2022

Yang-Xi Hu et al. found that CDDP had a proangiogenic effect, the mechanism of which involved the VEGF/VEGFR and PI3K/AKT signaling pathways. [Read the Full Post]

Theratyping of the Rare CFTR Variants E193K and R334W in Rectal Organoid-Derived Epithelial Monolayers

476 | Apr 24 2022

Fabiana Ciciriello et al. proposed that the functional CFTR assay might guide personalized medicine in patients with CF-like clinical manifestations as well as in those carrying rare CFTR mutations. [Read the Full Post]

Individualization in the first-line treatment of advanced ovarian cancer based on the mechanism of action of molecularly targeted drugs

617 | Apr 23 2022

Hidekatsu Nakai et al, found that the importance of achieving complete surgery and aiming for cure in the treatment of ovarian cancer and how the use of bevacizumab, olaparib, and niraparib should be individualized. [Read the Full Post]

A CT-based radiomics model to predict subsequent brain metastasis in patients with ALK-rearranged non-small cell lung cancer undergoing crizotinib treatment

559 | Apr 21 2022

Yongluo Jiang et al. developed a CT-based radiomics model to predict subsequent BM in patients with non-brain metastatic NSCLC undergoing crizotinib treatment. [Read the Full Post]

Diet impacts triple-negative breast cancer growth, metastatic potential, chemotherapy responsiveness, and doxorubicin-mediated cardiac dysfunction

427 | Apr 20 2022

Manuel U Ramirez et al. found that the Mediterranean diet might reduce lung metastatic lesions formation and prevent the development of cardiac toxicities. [Read the Full Post]

Clinically relevant CHK1 inhibitors abrogate wild-type and Y537S mutant ERα expression and proliferation in luminal primary and metastatic breast cancer cells

835 | Apr 20 2022

Sara Pescatori et al. thought that CHK1 could be considered as an appealing novel pharmacological target for the treatment of luminal primary and MBCs. [Read the Full Post]

Nuclear translocation of p85β promotes tumorigenesis of PIK3CA helical domain mutant cancer

793 | Apr 19 2022

Yujun Hao et al. found that the drug combination could be an effective therapeutic approach for PIK3CA helical domain mutant tumors. [Read the Full Post]

Janus Kinase Inhibitors in the Treatment of Type I Interferonopathies: A Case Series From a Single Center in China

466 | Apr 18 2022

Wendao Li et al. found that the JAK inhibitors baricitinib and tofacitinib were promising therapeutic agents for patients with SAVI, AGS, and SPENCD, especially for the improvement of cutaneous lesions and febrile attacks. [Read the Full Post]

Improved Survival With Enzalutamide in Patients With Metastatic Hormone-Sensitive Prostate Cancer

262 | Apr 16 2022

Andrew J Armstrong et al.found that enzalutamide plus ADT significantly prolongs survival versus placebo plus ADT in patients with mHSPC. [Read the Full Post]

Erythrocyte-cancer Hybrid Membrane-camouflaged Mesoporous Silica Nanoparticles Loaded with Gboxin for Glioma-targeting Therapy

710 | Apr 15 2022

Xiuxiu Jiao et al. found that the (MSNs/Gboxin)@[RBC-U] exhibited significant anti-cancer effected in vitro and the specific self-recognition to GBM cells. [Read the Full Post]

An effective AKT inhibitor-PARP inhibitor combination therapy for recurrent ovarian cancer

500 | Apr 15 2022

Jing Xu et al. suggested that the combination of AKT inhibitor and PARP inhibitor could be a viable approach for clinical testing in recurrent ovarian cancer patients. [Read the Full Post]

Update on International Medical Taxonomies of Biomarkers and Their Applications in Management of Thyroid Cancers

264 | Apr 14 2022

Maria Trovato thought that BM taxonomies should have common standards internationally recognized. [Read the Full Post]

Cotargeting of Bcl-2 and Mcl-1 shows promising antileukemic activity against AML cells including those with acquired cytarabine resistance

247 | Apr 12 2022

Fangbing Liu et al. revealed that the combined inhibition of Mcl-1 and Bcl-2 showed promise against AML cells, including relapse/refractory AML. [Read the Full Post]

Unmasking BCL-2 Addiction in Synovial Sarcoma by Overcoming Low NOXA

173 | Apr 11 2022

Carter K Fairchild Jr et al. found remarkably depressed levels of the endogenous MCL-1 inhibitor, NOXA, in SS compared to other sarcomas. [Read the Full Post]

GRP78 blockade overcomes intrinsic resistance to UBA1 inhibitor TAK-243 in glioblastoma

389 | Apr 10 2022

Xu Zhang et al. provided a new strategy for improving the sensitivity of GBM to TAK-243 treatment and experimental basis for further clinical trials to evaluate this combination therapy. [Read the Full Post]

Neddylation is essential for β-catenin degradation in Wnt signaling pathway

520 | Apr 10 2022

Bojun Wang et al. highlighted the importance of reassessing previously identified ubiquitylation substrates. [Read the Full Post]

Transplantation of autologous bone marrow pre-loaded ex vivo with oncolytic myxoma virus is efficacious against drug-resistant Vk*MYC mouse myeloma

241 | Apr 05 2022

Nancy Y Villa et al. found the utility of autologous BM grafts armed ex vivo with oncolytic MYXV alone or in combination with chemotherapy/immunotherapy to treat drug-resistant MM in vivo. [Read the Full Post]

Inhibition of the PINK1-Parkin Pathway Enhances the Lethality of Sorafenib and Regorafenib in Hepatocellular Carcinoma

500 | Apr 05 2022

Shun Zhang et al. found that PINK1-Parkin-mediated mitophagy alleviates sorafenib and regorafenib antitumor effected in vitro and in vivo. [Read the Full Post]

JIB-04 Has Broad-Spectrum Antiviral Activity and Inhibits SARS-CoV-2 Replication and Coronavirus Pathogenesis

466 | Apr 03 2022

Juhee Son et al. found that a limited but still promising utility of JIB-04 as an antiviral agent in the combat against COVID-19 and potentially other viral diseases. [Read the Full Post]

In Vitro Evaluation of Rigosertib Antitumoral and Radiosensitizing Effects against Human Cholangiocarcinoma Cells

724 | Apr 01 2022

Alessio Malacrida et al. thought that rigosertib could be a potential therapeutic option, alone or in combination with radiations, for nonresectable patients with cholangiocarcinoma. [Read the Full Post]

Rigosertib and Cholangiocarcinoma: A Cell Cycle Affair

490 | Mar 31 2022

Alessio Malacrida et al. hypothesized the mechanism of the action of Rigosertib against cholangiocarcinoma EGI-1 cells, highlighting the importance of proteins involved in the regulation of cell cycles. [Read the Full Post]

DNA repair protein DNA-PK protects PC12 cells from oxidative stress-induced apoptosis involving AKT phosphorylation

387 | Mar 30 2022

Alessio Cardinale et al. found that DNA-PK could protect cells from oxidative stress induced-apoptosis independently from its function of DSB repair enzyme. [Read the Full Post]

Cyclin-dependent kinase 7/9 inhibitor SNS-032 induces apoptosis in diffuse large B-cell lymphoma cells

269 | Mar 29 2022

Liling Jiang et al. provided pre-clinical evidence for application of targeting the CDK7/9 in DLBCL. [Read the Full Post]

Hdac8 Inhibitor Alleviates Transverse Aortic Constriction-Induced Heart Failure in Mice by Downregulating Ace1

490 | Mar 25 2022

Tingwei Zhao et al. suggested that HDAC8 was a potential novel therapeutic target for heart failure accompanied by pathological lung diseases. [Read the Full Post]

Luminescent Human iPSC-Derived Neurospheroids Enable Modeling of Neurotoxicity After Oxygen-glucose Deprivation

398 | Mar 24 2022

Elise Van Breedam et al. found that treatment of oxygen- and glucose-deprived neurospheroids with the pan-caspase inhibitor Z-VAD-FMK did not increase overall neural survival, despite its successful attenuation of apoptosis, in a human-based 3D environment. [Read the Full Post]

Hypoxia represses early responses of prostate and renal cancer cells to YM155 independent of HIF-1α and HIF-2α

347 | Mar 23 2022

David Danielpour et al. hypothesized that a hypothetical hypoxia-inducer factor (HIF-X) repressed early signaling responses to YM155. [Read the Full Post]

miRNA‑218 targets multiple oncogenes and is a therapeutic target for osteosarcoma

551 | Mar 22 2022

Kentaro Sato et al. found that miR‑218 showed a wider range of therapeutic efficacy compared with YM155, suggesting that miR‑218 should be evaluated as a treatment target. [Read the Full Post]

Activation of Age-Related Nuclear Factor-κB Signaling Pathway Leads to Chronic Inflammation and Pituitary Fibrosis

267 | Mar 21 2022

Jian Mao et al. investigated the mechanism of pituitary fibrosis in elderly people. [Read the Full Post]

What's new in myeloproliferative neoplasia

873 | Mar 19 2022

Stefan Schmidt et al. revealed components of the alarmin complex (S100A8 und S100A9) drove this local sterile inflammation process, which also represented a potential therapeutic target, as the S100A8 and A9 inhibitor Tasquinimod reduced fibrosis in a pre-clinical animal model. [Read the Full Post]

Defining Endocytic Pathways of Fucoidan-Coated PIBCA Nanoparticles from the Design of their Surface Architecture

925 | Mar 19 2022

M C B Lira-Nogueira et al. found that internalization pathways of PIBCA nanoparticles by J774A.1 macrophages could be determined by nanoparticle fucoidan surface composition and architecture. [Read the Full Post]

The beneficial effect of salubrinal on neuroinflammation and neuronal loss in intranigral LPS-induced hemi-Parkinson disease model in rats

804 | Mar 18 2022

Fatma Nihan Cankara et al. found that salubrinal was attenuating several inflammatory mediators and thereby decreased the inflammatory effects of LPS in the neurons of the SN. [Read the Full Post]

The role of the atypical chemokine receptor CCRL2 in myelodysplastic syndrome and secondary acute myeloid leukemia

762 | Mar 18 2022

Theodoros Karantanos et al. implicated CCRL2 as an MDS/sAML cell growth mediator, partially through JAK2/STAT signaling. [Read the Full Post]

Tumorigenic circulating tumor cells from xenograft mouse models of non-metastatic NSCLC patients reveal distinct single cell heterogeneity and drug responses

389 | Mar 15 2022

Kanve N Suvilesh et al. showed that CDX models deserved further development and studied to discover personalized strategies against micrometastases in non-metastatic NSCLC patients. [Read the Full Post]

Construction of an Immune-Autophagy Prognostic Model Based on ssGSEA Immune Scoring Algorithm Analysis and Prognostic Value Exploration of the Immune-Autophagy Gene in Endometrial Carcinoma (EC) Based on Bioinformatics

480 | Mar 13 2022

Xiaomin Xu et al. constructed the immuno-autophagy prognosis model of endometrial cancer and identified three high-risk immunoautophagy genes, including VEGFA, CCL2, and Ifng. [Read the Full Post]

Tubastatin A suppresses the proliferation of fibroblasts in epidural fibrosis through phosphatidylinositol-3-kinase/protein kinase B/mammalian target of rapamycin (PI3K/AKT/mTOR) signalling pathway

639 | Mar 12 2022

Yang Liu et al.discovered that Tub A could prevent epidural fibrosis formation by inhibiting fibroblast proliferation through mediating PI3K/AKT/mTOR pathway. [Read the Full Post]

The effect of danusertib, an Aurora kinase inhibitor, onto the cytotoxicity, cell cycle and apoptosis in pancreatic ductal adenocarcinoma cells

1014 | Mar 11 2022

Ismail Ayberk Kirbiyik et al. thought that Aurora kinase inhibitor danusertib might be a potential alternative to the treatment of pancreatic cancers. [Read the Full Post]

Combined Inhibition of Polo-Like Kinase-1 and Wee1 as a New Therapeutic Strategy to Induce Apoptotic Cell Death in Neoplastic Mast Cells

1039 | Mar 10 2022

Manuela Mancini et al. showed that repurposing Plk1 or AKA ± Wee1 inhibitors in advanced clinical development for other indications was a therapeutic strategy worthy of being explored, in order to improve the outcome of patients with advanced SM. [Read the Full Post]

Dual Targeting of PI3K and HDAC by CUDC-907 Inhibits Pediatric Neuroblastoma Growth

679 | Mar 07 2022

Rameswari Chilamakuri et al. found that the dual inhibition of PI3K and HDAC by CUDC-907 was an effective therapeutic strategy for NB and other MYC-dependent cancers. [Read the Full Post]

A FAK Inhibitor Boosts Anti-PD1 Immunotherapy in a Hepatocellular Carcinoma Mouse Model

567 | Mar 05 2022

Yuhua Wei et al. suggested that combination of the FAK inhibitor VS4718 and anti-PD1 could be a potential therapy for HCC by improving the immune environment, reducing liver fibrosis and simultaneously preventing PD1 from binding to the increased PD-L1 induced by FAK inhibitor VS4718. [Read the Full Post]

The underlying molecular mechanism and drugs for treatment in adrenal cortical carcinoma

329 | Mar 04 2022

Chengquan Ma et al. thought that the hub-genes expression was significant useful in adrenal cortical carcinoma, provide new diagnostic, prognosis and therapeutic approaches for adrenal cortical carcinoma. [Read the Full Post]

The Role of E-Cadherin and microRNA on FAK Inhibitor Response in Malignant Pleural Mesothelioma (MPM)

442 | Mar 04 2022

Man Lee Yuen et al. showed that MPM cells with high CDH1 mRNA levels exhibited resistance to the FAK inhibitor PND-1186. [Read the Full Post]

Inhibition MNK-eIF4E-β-catenin preferentially sensitizes gastric cancer to chemotherapy

950 | Feb 25 2022

Xiaolin Yang et al. provided preclinical evidence to initialize clinical trials for gastric cancer using tomivosertib in combination with chemotherapy. [Read the Full Post]

Functional Assessment of Kinesin-7 CENP-E in Spermatocytes using In Vivo Inhibition, Immunofluorescence and Flow Cytometry

439 | Feb 24 2022

Meng-Fei Xu et al. found that CENP-E inhibition resulted in chromosome misalignment and metaphase arrest in primary spermatocytes during meiosis I. [Read the Full Post]

Medical Therapy for Craniopharyngiomas

487 | Feb 24 2022

Krystallenia I Alexandraki et al. conducted a systematic review to identify case series or case reports with patients currently treated with systemic medical therapy. [Read the Full Post]

Fin56-induced ferroptosis is supported by autophagy-mediated GPX4 degradation and functions synergistically with mTOR inhibition to kill bladder cancer cells

630 | Feb 21 2022

Yadong Sun et al. thought that the combined application of ferroptosis inducers and mTOR inhibitors was a promising approach to improve therapeutic options in the treatment of bladder cancer. [Read the Full Post]

Sensitizing TRAIL response via differential modulation of anti- and pro-apoptotic factors by AZD5582 combined with ER nanosomal TRAIL in neuroblastoma

134 | Feb 19 2022

Chaohong Huang et al. identified that the concomitant regulation of both antiapoptotic and proapoptotic factors and DR5 is an essential molecular mechanism for overcoming TRAIL resistance in SH-SY5Y and the combination of ERN-T and AZD5582 potentially constitutes a novel therapeutic strategy, which is highly effective and safe for neuroblastoma. [Read the Full Post]

ATRX loss in glioma results in dysregulation of cell-cycle phase transition and ATM inhibitor radio-sensitization

550 | Feb 18 2022

Tingting Qin et al. found that ATRX-deficient high-grade gliomas (HGGs) displayed Chk1-mediated dysregulation of cell-cycle phase transitions. [Read the Full Post]

Cervical Alignment of Patients with Basilar Invagination: A Radiological Study

269 | Feb 17 2022

Jun-Yu Lin et al. showed that the negative correlation between upper and lower cervical curvatures was more obvious in BI patients. [Read the Full Post]

The heat shock response, determined by QuantiGene multiplex, is impaired in HD mouse models and not caused by HSF1 reduction

587 | Feb 14 2022

Casandra Gomez-Paredes et al. found that following pharmacological activation in vivo,the heat shock response impairment in tibialis anterior, brain hemispheres and striatum was comparable between zQ175 and R6/2 mice. [Read the Full Post]

Osthole Exerts Inhibitory Effects on Hypoxic Colon Cancer Cells via EIF2[Formula: see text] Phosphorylation-mediated Apoptosis and Regulation of HIF-1[Formula: see text]

426 | Feb 13 2022

Kui-Yuan Peng et al. thought that osthole might be a potential agent in the treatment of colon cancer. [Read the Full Post]

Drug-repurposing against COVID-19 by targeting a key signaling pathway: An in silico study

463 | Feb 13 2022

Ki Kwang Oh et al. provided three key elements to alleviate COVID-19 symptoms might be anti-inflammatory effects on SARs-CoV-2-infected lung cells. [Read the Full Post]

Bidirectional Responses of Eight Neuroinflammation-Related Transcriptional Factors to 64 Flavonoids in Astrocytes with Transposable Insulated Signaling Pathway Reporters

429 | Feb 12 2022

Valeri V Mossine et al. conclude that transposable insulated reporters of transcriptional activation represent a convenient neurochemistry tool in screening for activators/inhibitors of signaling pathways. [Read the Full Post]

Performance of noninvasive tests of fibrosis among Asians, Hispanic and non-Hispanic Whites in the STELLAR trials

533 | Feb 11 2022

Vincent Wai-Sun Wong et al. found that the diagnostic performance of routinely available noninvasive tests for the detection of advanced fibrosis due to NASH was acceptable and similar between White and Asian patients. [Read the Full Post]

Lumican silencing alleviates tumor necrosis factor-α-induced nucleus pulposus cell inflammation and senescence by inhibiting apoptosis signal regulating kinase 1/p38 signaling pathway via inactivating Fas ligand expression

590 | Feb 11 2022

Zhenqiang Li et al. found that interference with LUM effectively mitigated TNF-α-induced inflammatory response, cell cycle arrest, and cell senescence. [Read the Full Post]

Paracrine production of IL-6 promotes a hypercoagulable state in pancreatic cancer

611 | Feb 09 2022

Silu Wang et al. found the key role of the Jagged/Notch/IL-6/STAT3 feedback loop in the development of a hypercoagulable state in pancreatic cance. [Read the Full Post]

γ-Secretase inhibitors for breast cancer and hepatocellular carcinoma: From mechanism to treatment

618 | Feb 09 2022

Hui Jia et al. thought that the γ-secretase complex was very important for activation of the Notch receptor and regulation of target-gene transcription. [Read the Full Post]

Role of KSP inhibitors as anti-cancer therapeutics: an update

625 | Feb 06 2022

Rinkal Chamariya et al. thought that KSP inhibitors had exhibited promising results and continued exploration was greatly required to establish the clinical potential of KSP inhibitors. [Read the Full Post]

Efficacy and Synergy of Small Molecule Inhibitors Targeting FLT3-ITD + Acute Myeloid Leukemia

602 | Feb 06 2022

Javier Bregante et al. suggested WS6, ispinesib, ponatinib and cabozantinib as novel options for targeting FLT3-ITD+ AML. [Read the Full Post]

Potential effects and application prospect of angiotensin receptor-neprilysin inhibitor in diabetic kidney disease

558 | Feb 05 2022

Xingjian Zhang found that ARNI has application potential in DKD, but there still need clinical studies that focus on DKD patients to determine its effectiveness, safety and underlying mechanism. [Read the Full Post]

Anti-Leukemic Properties of Aplysinopsin Derivative EE-84 Alone and Combined to BH3 Mimetic A-1210477

205 | Feb 05 2022

Sungmi Song et al. demonstrated the synergistic cytotoxic effect of EE-84 with a BH3 mimetic, the Mcl-1 inhibitor A-1210477, against imatinib-sensitive and resistant K562 cells, highlighting the inhibition of antiapoptotic Bcl-2 proteins as a promising novel senolytic approach against chronic myeloid leukemia. [Read the Full Post]

Traditional Chinese medicine Lingguizhugan decoction ameliorate HFD-induced hepatic-lipid deposition in mice by inhibiting STING-mediated inflammation in macrophages

215 | Feb 04 2022

Lin Cao et al. demonstrated that LGZG can ameliorate HFD-induced hepatic-lipid deposition through inhibiting STING-TBK1-NF-κB pathway in liver macrophages, which provides novel insight for elucidating the molecular mechanism of LGZG alleviating HFD induced hepatic steatosis. [Read the Full Post]

Effects of Combinatorial Ubiquitinated Protein-Based Nanovaccine and STING Agonist in Mice With Drug-Resistant and Metastatic Breast Cancer

253 | Feb 03 2022

iFang Huang et al. indicated that this novel combinatorial immunotherapy with UPs-4T1/EPB vaccine and STING agonist is effective in mice with drug-resistant and metastatic breast cancer. [Read the Full Post]

Ascorbate Inhibits Proliferation and Promotes Myeloid Differentiation in TP53-Mutant Leukemia

294 | Feb 02 2022

Carlos C Smith-Díaz et al. suggested that ascorbate could exert a beneficial anti-proliferative effect on AML cells harboring both TET2 and TP53 mutations whilst not interfering with targeted cytotoxic therapies such as Prima-1Met. [Read the Full Post]

Restoring p53 Function in Head and Neck Squamous Cell Carcinoma to Improve Treatments

313 | Feb 01 2022

Tycho de Bakker et al. described and discussed p53 regulation and its targeting in combination with existing therapies for HNSCC through a new classification of such cancers based on p53 mutation status and HPV infection. [Read the Full Post]

The Effect of STAT3 Signal Pathway Activation on Retinopathy of Prematurity

354 | Jan 29 2022

Jianbing Ren et al. provided potential novel therapeutic approach to the prevention and treatment of ROP. [Read the Full Post]

Inhibitor GSK690693 extends Drosophila lifespan via reduce AKT signaling pathway

1382 | Jan 27 2022

Xingyi Cheng et al. indicated that GSK690693 might become an effective compound for anti-aging intervention. [Read the Full Post]

Rifampin and ritonavir increase oral availability and elacridar enhances overall exposure and brain accumulation of the NTRK inhibitor larotrectinib

355 | Jan 26 2022

Yaogeng Wang et al.found that elacridar enhanced both larotrectinib plasma and tissue exposure and especially relative brain penetration, which might be therapeutically relevant. [Read the Full Post]

Neutrophil Extracellular Traps Are Increased in Chronic Myeloid Leukemia and Are Differentially Affected by Tyrosine Kinase Inhibitors

699 | Jan 24 2022

Alona Telerman et al. thought that CML was associated with increased NET formation, which was augmented by ponatinib, suggesting a possible role for NETs in promoting vascular toxicity in CML. [Read the Full Post]

Targeted Treatment of Non-Small Cell Lung Cancer: Focus on Capmatinib with Companion Diagnostics

514 | Jan 19 2022

Matthew Z Guo et al.discussed limitations of capmatinib, and highlighted ongoing trials of capmatinib in combinatorial approaches. [Read the Full Post]

Regulation of the mammalian maternal-to-embryonic transition by eukaryotic translation initiation factor 4E

797 | Jan 18 2022

Yan Li et al. thought that eIF4E activity was regulated at key embryonic transitions in the mammalian embryo and was essential for the successful transition from maternal to embryonic control of development. [Read the Full Post]

Novel function of THEMIS2 in the enhancement of cancer stemness and chemoresistance by releasing PTP1B from MET

506 | Jan 18 2022

Wei-Chieh Huang et al. found that non-cytotoxic dosages of cryptotanshinone (CPT) could potently inhibit cancer stemness, chemoresistance and tumorigenicity by suppressing expression of THEMIS2. [Read the Full Post]

RSL3 Drives Ferroptosis through NF- κ B Pathway Activation and GPX4 Depletion in Glioblastoma

409 | Jan 14 2022

Shengbiao Li et al. found that the NF-κB pathway played a novel role in RSL3-induced ferroptosis in glioblastoma cells. [Read the Full Post]

Protein Kinase A (PRKA) Activity Is Regulated by the Proteasome at the Onset of Human Sperm Capacitation

407 | Jan 13 2022

Héctor Zapata-Carmona et al. suggested that PRKAR1 was the target of PRKA regulation by the proteasome. [Read the Full Post]

Combined Drug Targeting of p53-dependent and -independent Pathways Depletes Myelofibrosis Hematopoietic Stem/Progenitor Cells

297 | Jan 11 2022

Min Lu et al. thought that treatment with ONC201 combined with RG7112 could be a potentially effective strategy for treating MF patients. [Read the Full Post]

Osteoprotegerin regulates vascular function through syndecan-1 and NADPH oxidase-derived reactive oxygen species

628 | Jan 08 2022

Rhéure Alves-Lopes et al. identified novel molecular mechanisms beyond calcification for OPG, which might underlie vascular injurious effects of osteogenic factors in conditions such as hypertension and/or diabetes. [Read the Full Post]

Disruptor of telomeric silencing 1-like promotes ovarian cancer tumor growth by stimulating pro-tumorigenic metabolic pathways and blocking apoptosis

0 | Jan 07 2022

Suresh Chava et al. found that DOT1L promoted ovarian cancer tumor growth by regulating apoptotic and metabolic pathways as well as NK cell-mediated eradication of ovarian cancer. [Read the Full Post]

DR-5 and DLL-4 mAb Functionalized SLNs of Gamma-Secretase Inhibitors- An Approach for TNBC Treatment

534 | Jan 06 2022

Mamta Kumari et al. found that DLL4 mAb and GSIs were expected to act synergistically to block the Notch signal mediated BCSCs proliferation, differentiation, and metastasis. [Read the Full Post]

Dysmyelination by Oligodendrocyte-Specific Ablation of Ninj2 Contributes to Depressive-Like Behaviors

236 | Jan 06 2022

Yuxia Sun et al. found the role of Ninj2 in the development of depression and myelination. [Read the Full Post]

Fibroblast growth factor (FGF), FGF receptor (FGFR), and cyclin D1 (CCND1) DNA methylation in head and neck squamous cell carcinomas is associated with transcriptional activity, gene amplification, human papillomavirus (HPV) status, and sensitivity to tyrosine kinase inhibitors

382 | Jan 05 2022

Yilin Bao et al. found significant correlations of DNA methylation of specific CpG sites with response to the FGFR1/3-selective inhibitors PD 173074 and AZD4547, predominantly within the transcription start site of CCND1. [Read the Full Post]

CYT387 Inhibits the Hyperproliferative Potential of Fibroblast-like Synoviocytes via Modulation of IL-6/JAK1/STAT3 Signaling in Rheumatoid Arthritis

640 | Jan 04 2022

Susmita Srivastava et al. found that CYT387 inhibits proliferation, migration, and pathogenic diseased potential of FLS isolated from adjuvant-induced arthritic (AA) rats via targeting IL-6/JAK1/STAT3 signaling cascade. [Read the Full Post]

Combination of Ocimum sanctum extract and Levetiracetam ameliorates cognitive dysfunction and hippocampal architecture in rat model of Alzheimer's disease

769 | Jan 03 2022

H S Nandini et al. provided evidence for use of OSE, LEV and OSE+LEV against AD and epilepsy associated with AD in Aβ induced AD animal model. [Read the Full Post]

A phase 1b study of erlotinib and momelotinib for the treatment of EGFR-mutated, tyrosine kinase inhibitor-naive metastatic non-small cell lung cancer

698 | Jan 03 2022

Sukhmani K Padda et al. showed that the JAK1/2 and TBK1 inhibitor momelotinib in combination with erlotinib did not appear to enhance benefit over the historical data of erlotinib monotherapy in patients with EGFR-mutated NSCLC. [Read the Full Post]

Collagen XV Promotes ER Stress-Induced Inflammation through Activating Integrin β1/FAK Signaling Pathway and M1 Macrophage Polarization in Adipose Tissue

562 | Jan 02 2022

Changxing Li et al. provided new ideas for solving the problems of adipose tissue metabolism disorders caused by abnormal accumulation of ECM. [Read the Full Post]

Protective Effects of Hif2 Inhibitor PT-2385 on a Neurological Disorder Induced by Deficiency of Irp2

407 | Dec 29 2021

Jiaqi Shen et al. found that Irp2 depletion-induced Hif2α was, in vivo, in charge of the switch between OXPHOS and glycolysis. [Read the Full Post]

Small Dense Low-Density Lipoprotein Cholesterol and Cardiovascular Risk in Statin-Treated Patients with Coronary Artery Disease

585 | Dec 28 2021

Junnichi Ishii et al. investigated the relationship between small dense low-density cholesterol (sdLDL-C) and risk of major adverse cardiovascular events (MACE) in patients treated with high- or low-dose statin therapy. [Read the Full Post]

Proliferation of bovine endometrial epithelial cells is promoted by prostaglandin E 2-PTGER2 signaling through cell cycle regulation

298 | Dec 26 2021

Bo Liu et al. demonstrated that PGE2-PTGER2 signaling activation had a direct molecular association with cell cycle regulation and cell proliferation in bEECs. [Read the Full Post]

The role of RIPK1 mediated cell death in acute on chronic liver failure

675 | Dec 24 2021

Takayuki Kondo et al. thought that inhibition of RIPK1 was a potential novel therapeutic approach to prevent progression of susceptible patients from no ACLF to ACLF. [Read the Full Post]

Mini-Review: GSDME-Mediated Pyroptosis in Diabetic Nephropathy

412 | Dec 23 2021

Wen Li et al. described the discovery and history of research in this pyroptosis pathway and reviewed the function of proteins in the gasdermin family, with a focus on the role of GSDME-mediated pyroptosis in DN. [Read the Full Post]

4-Acyl Pyrrole Capped HDAC Inhibitors: A New Scaffold for Hybrid Inhibitors of BET Proteins and Histone Deacetylases as Antileukemia Drug Leads

665 | Dec 22 2021

Linda Schäker-Hübner et al. suggested an advantage of dual HDAC/BET inhibitors over the combination of two single targeted compounds. [Read the Full Post]

Drug repurposing for COVID-19 using computational screening: Is Fostamatinib/R406 a potential candidate?

682 | Dec 18 2021

Sovan Saha et al. found that Fostamatinib (R406 as its active promoiety) may also be considered as one of the potential candidates for further clinical trials in pursuit to counter the spread of COVID-19. [Read the Full Post]

GLI1-targeting drugs induce replication stress and homologous recombination deficiency and synergize with PARP-targeted therapies in triple negative breast cancer cells

765 | Dec 17 2021

Chinnadurai Mani et al. found that Aberrantly activated GLI1 regulated HR-mediated DNA repair by transcriptionally regulating FANCD2 to overcome chemotherapy-induced replication stress and DNA damage. [Read the Full Post]

Chk1 and the Host Cell DNA Damage Response as a Potential Antiviral Target in BK Polyomavirus Infection

588 | Dec 14 2021

Lydia E Hainley et al. found that Chk1 inhibitors were safe and effective in clinical trials for cancer should also be evaluated for antiviral activity against BKPyV. [Read the Full Post]

d-mannose attenuates lipopolysaccharide-induced osteolysis via CPT1A-Mediated lipid metabolic regulation in macrophages

432 | Dec 13 2021

Zhenzhen Zhang et al. implied that d-mannose attenuated LPS-induced osteolysis by manipulating CPT1A-mediated lipid metabolism in macrophages. [Read the Full Post]

HSP90 inhibition downregulates DNA replication and repair genes via E2F1 repression

820 | Dec 05 2021

Hanqing Liu et al. found that HSP90 inhibitors might be useful in combination therapies for MCL. [Read the Full Post]

Investigation of anticancer activities of STA-9090 (ganetespib) as a second generation HSP90 inhibitor in Saos-2 osteosarcoma cells

816 | Dec 05 2021

Aykut Özgür found the down-regulation of the expression levels of oncogenic genes. [Read the Full Post]

Poziotinib in Non-Small-Cell Lung Cancer Harboring HER2 Exon 20 Insertion Mutations After Prior Therapies: ZENITH20-2 Trial

704 | Dec 02 2021

Xiuning Le et al. found that Poziotinib demonstrated antitumor activity in previously treated patients with HER2 exon 20 insertion NSCLC. [Read the Full Post]

Lapatinib and poziotinib overcome ABCB1-mediated paclitaxel resistance in ovarian cancer

664 | Dec 02 2021

J Robert McCorkle et al. thought that lapatinib and poziotinib combined with paclitaxel synergizes to inhibit the proliferation of ABCB1-overexpressing ovarian cancer cells in vitro. [Read the Full Post]

Evaluation of protein kinase D auto-phosphorylation as biomarker for NLRP3 inflammasome activation

456 | Dec 01 2021

Diane Heiser et al. found thta PKD auto-phosphorylation could be triggered by a broad range of stimuli unrelated to NLRP3 inflammasome assembly. [Read the Full Post]

Comparing the Effect of Multiple Histone Deacetylase Inhibitors on SSTR2 Expression and [ 111 In]In-DOTATATE Uptake in NET Cells

591 | Nov 30 2021

Maria J Klomp rt al. suggested that proper timing of HDACi treatment was most likely essential for a beneficial outcome. [Read the Full Post]

Butyrate and Class I Histone Deacetylase Inhibitors Promote Differentiation of Neonatal Porcine Islet Cells into Beta Cells

968 | Nov 29 2021

Yichen Zhang et al. revealed that butyrate treatment had the capacity to increase the number of beta cells, which might be predominantly mediated through its HDAC inhibitory activity. [Read the Full Post]

Preclinical Test of Dacomitinib, an Irreversible EGFR Inhibitor, Confirms Its Effectiveness for Glioblastoma

0 | Nov 26 2021

Cristina Zahonero et al. found that dacomitinib clearly affected receptor signaling in vivo and that its strong antitumoral effect was independent of the presence of mutant receptor isoforms although it could be affected by the PTEN status. [Read the Full Post]

Lipophagy deficiency exacerbates ectopic lipid accumulation and tubular cells injury in diabetic nephropathy

347 | Nov 22 2021

Yachun Han et al. found that autophagy-mediated lipophagy deficiency played a critical role in the ELD and lipid-related renal injury of DN. [Read the Full Post]

First-in-human phase 1 study of the anti-TIGIT antibody vibostolimab as monotherapy or with pembrolizumab for advanced solid tumors, including non-small cell lung cancer

477 | Nov 22 2021

J Niu et al. found that vibostolimab plus pembrolizumab was well tolerated and demonstrated antitumor activity in patients with advanced solid tumors, including patients with advanced NSCLC. [Read the Full Post]

Multimodal obstruction of tumorigenic energy supply via bionic nanocarriers for effective tumor therapy

478 | Nov 19 2021

Xiaoqian Yu et al. found that the CA4P/VK2-MSNs-TBAM/TSAG-HA (CVMMGH for short) nanocarrier combined well-controllable manipulation of tumor vasculature and tumor mitochondria to effectivly cut off the tumorigenic energy supply. [Read the Full Post]

First-in-child phase I/II study of the dual mTORC1/2 inhibitor vistusertib (AZD2014) as monotherapy and in combination with topotecan-temozolomide in children with advanced malignancies: arms E and F of the AcSé-ESMART trial

359 | Nov 19 2021

Raphael J Morscher et al. found that vistusertib was well tolerated in paediatric patients. [Read the Full Post]

A high-throughput and simultaneous determination of combretastatin A-4 phosphate and its metabolites in human plasma using HPLC-MS/MS: Application to a clinical pharmacokinetic study

482 | Nov 18 2021

Qizhen Wu et al. thought that an abundant ammonium adduct ion of CA4G in ESI+ was observed as an ideal precursor ion. [Read the Full Post]

Sequential drug delivery by injectable macroporous hydrogels for combined photodynamic-chemotherapy

498 | Nov 18 2021

Yuanyuan Zhong et al. found that dual drugs treated groups had better tumor inhibition than solo drug under near infrared laser irradiation [Read the Full Post]

Discovery of novel quinazoline-based covalent inhibitors of KRAS G12C with various cysteine-targeting warheads as potential anticancer agents

585 | Nov 13 2021

Ling Li et.al suggested that the novel covalent inhibitors of KRAS G12C with different warheads deserve further investigation as potential anticancer agents. [Read the Full Post]

Pim kinase inhibitor co-treatment decreases alternative non-homologous end-joining DNA repair and genomic instability induced by topoisomerase 2 inhibitors in cells with FLT3 internal tandem duplication

766 | Nov 12 2021

Mario Scarpa et al. found that Pim kinase inhibitor co-treatment both enhanced TOP2 inhibitor cytotoxicity and decreased TOP2 inhibitor-induced genomic instability in cells with FLT3-ITD. [Read the Full Post]

Dexmedetomidine attenuates propofol-induced apoptosis of neonatal hippocampal astrocytes by inhibiting the Bcl2l1 signaling pathway

294 | Nov 11 2021

Wen-Chong Sun et al. found that DEX pretreatment reduced propofol-associated pro-apoptosis in developing astrocytes via downregulation of anti-apoptotic signaling mediated by Bcl2l1. [Read the Full Post]

FILIP1L-mediated cell apoptosis, epithelial-mesenchymal transition and extracellular matrix synthesis aggravate posterior capsular opacification

266 | Nov 10 2021

Ruihua Jing et al. found the role of apoptosis in PCO development and provided new drug targets. [Read the Full Post]

Intermittent hypoxia aggravates non-alcoholic fatty liver disease via RIPK3-dependent necroptosis-modulated Nrf2/NFκB signaling pathway

232 | Nov 09 2021

Huojun Zhang et al. found that RIPK3 inhibitor GSK-872 or TBHQ administration obviously alleviated hepatic injury, including histology, transaminase activities, and triglyceride contents in vivo. [Read the Full Post]

Rapalogs induce non-apoptotic, autophagy-dependent cell death in HPV-negative TP53 mutant head and neck squamous cell carcinoma

516 | Nov 08 2021

Md Maksudul Alam et al. found that rapalogs promoted non-apoptotic ADCD in HPV-negative mutTP53 HNSCC via the ULK1 pathway. [Read the Full Post]

Histone chaperone FACT complex inhibitor CBL0137 interferes with DNA damage repair and enhances sensitivity of medulloblastoma to chemotherapy and radiation

366 | Nov 07 2021

Heyu Song et al. concluded that FACT complex promoted chemo-radiation resistance in MB, and FACT inhibitor CBL0137 could be used as a chemo-radiation sensitizer to augment treatment efficacy and reduce therapy-related toxicity in high-risk pediatric patients. [Read the Full Post]

The mTOR Inhibitor Temsirolimus Added to Rituximab Combined With Dexamethasone, Cytarabine, and Cisplatinum (R-DHAP) for the Treatment of Patients With Relapsed or Refractory DLBCL - Results From the Phase-II STORM Trial

489 | Nov 07 2021

Mathias Witzens-Harig et al. concluded that temsirolimus could be safely added to rituximab and DHAP with promising activity. [Read the Full Post]

Oxidative Phosphorylation Is a Metabolic Vulnerability in Chemotherapy-Resistant Triple-Negative Breast Cancer

455 | Nov 05 2021

Kurt W Evans et al. suggested that triple-negative breast cancer was highly reliant on OXPHOS and that inhibiting OXPHOS might be a novel approach to enhance efficacy of several targeted therapies. [Read the Full Post]

Zebrafish BID Exerts an Antibacterial Role by Negatively Regulating p53, but in a Caspase-8-Independent Manner

437 | Oct 27 2021

Zhitao Qi et al. found a novel antibacterial activity of fish Bid, providing evidence for understanding the function of apoptosis associated gene in pathogen infection. [Read the Full Post]

Co-Expression of CD34, CD90, OV-6 and Cell-Surface Vimentin Defines Cancer Stem Cells of Hepatoblastoma, Which Are Affected by Hsp90 Inhibitor 17-AAG

974 | Oct 26 2021

Mieun Lee-Theilen et al. identified CSCs of hepatoblastoma using CD34, CD90, OV-6 and csVimentin. [Read the Full Post]

Identification of a circRNA-miRNA-mRNA regulatory network for exploring novel therapeutic options for glioma

1023 | Oct 25 2021

Yi He et al. highlighted the potential pathogenesis of the circRNA-miRNA-mRNA regulatory network and identified novel therapeutic options for glioma. [Read the Full Post]

A Novel Small Molecule, LCG-N25, Inhibits Oral Streptococcal Biofilm

473 | Oct 23 2021

Xiaoying Lyu et al. suggested that LCG-N25 may represent a promising antimicrobial agent that can be used as an adjuvant to the management of dental caries. [Read the Full Post]

Arsenic sulfide reverses cisplatin resistance in non-small cell lung cancer in vitro and in vivo through targeting PD-L1

519 | Oct 22 2021

Wei Tian et al. found that As4 S4 might sensitize NSCLC cells to DDP through targeting p53/miR-34a-5p/PD-L1 axis. [Read the Full Post]

Roxadustat (FG-4592) protects against ischemia/reperfusion-induced acute kidney injury through inhibiting the mitochondrial damage pathway in mice

672 | Oct 21 2021

Mei Zhang et al. found that pretreatment with FG-4592 might effectively prevent kidney from IRI possibly by via diminishing tubular cells injuries and protection of mitochondrial damage pathway. [Read the Full Post]

Fabrication of a pH-responsive core-shell nanosystem with a low-temperature photothermal therapy effect for treating bacterial biofilm infection

573 | Oct 21 2021

Dan Peng et al. found that the release of Zn2+ had an antibacterial/antibiofilm effect. [Read the Full Post]

AZD8055 ameliorates experimental autoimmune encephalomyelitis via the mTOR/ROS/NLRP3 pathway

599 | Oct 20 2021

Miao He et al. provided insights into the interactions between autophagy and pyroptosis and might facilitate the development of novel treatments for MS. [Read the Full Post]

C646 Protects Against DSS-Induced Colitis Model by Targeting NLRP3 Inflammasome

623 | Oct 20 2021

Xueming Xu et al. demonstrated the ability of C646 to suppress the NLRP3 inflammasome activity and its potential application in the treatment of inflammatory bowel disease. [Read the Full Post]

Nuclear receptor coactivator 4-mediated ferritinophagy contributes to cerebral ischemia-induced ferroptosis in ischemic stroke

330 | Oct 15 2021

Chong Li et al. suggested a novel and effective target for treating ischemic stroke. [Read the Full Post]

HSP90 inhibition acts synergistically with heat to induce a pro-immunogenic form of cell death in colon cancer cells

1294 | Oct 14 2021

Petros X E Mouratidis et al. found that sub-ablative heating could act synergistically with the clinically relevant HSP90 inhibitor NVP-AUY922 to induce a pro-immunogenic form of cell death in colon cancer cells. [Read the Full Post]

CHK1 inhibitor sensitizes resistant colorectal cancer stem cells to nortopsentin

498 | Oct 14 2021

Simone Di Franco et al. found that synergistic combination of NORA234 and CHK1 (rabusertib) targeting was synthetic lethal inducing death of both CD44v6-negative and CD44v6-positive CRC stem cell fractions, aside from Wnt pathway activity. [Read the Full Post]

Evolution of kinase polypharmacology across HSP90 drug discovery

1295 | Oct 13 2021

Albert A Antolin et al. found that the resorcinol clinical candidates ganetespib and, to a lesser extent, luminespib, displayed unique off-target kinase pharmacology as compared with other HSP90 inhibitors. [Read the Full Post]

Successful treatment of hepatosplenic T-cell lymphoma with fludarabine, high-dose cytarabine and subsequent unrelated umbilical cord blood transplantation

838 | Oct 04 2021

Takaya Honda et al. found a heterozygous nonsense c.2961C>G (p.Tyr987Ter) variant of the KMT2C gene. [Read the Full Post]

The imbalance of Th17/Treg via STAT3 activation modulates cognitive impairment in P. gingivalis LPS-induced periodontitis mice

515 | Oct 03 2021

Xu Zhang et al. thought that the STAT3 signaling pathway might have immunoregulatory effects on the mouth-to-brain axis. [Read the Full Post]

circBTBD7 Promotes Immature Porcine Sertoli Cell Growth through Modulating miR-24-3p/ MAPK7 Axis to Inactivate p38 MAPK Signaling Pathway

523 | Sep 28 2021

Qiao Bian et al. expanded our knowledge of noncoding RNAs in porcine normal spermatogenesis through deciding the fate of Sertoli cells. [Read the Full Post]

Constitutive BAK/MCL1 complexes predict paclitaxel and S63845 sensitivity of ovarian cancer

297 | Sep 26 2021

Dongyan Liu et al. found that the assessment of BAK/MCL1 complexes might be useful for predicting response to paclitaxel alone or in combination with BH3 mimetics. [Read the Full Post]

Machine learning identifies molecular regulators and therapeutics for targeting SARS-CoV2-induced cytokine release

765 | Sep 22 2021

Marina Chan et al. proposed that agented targeting multiple kinases required for SARS-CoV-2-mediated cytokine release, such as ponatinib, might represent an attractive therapeutic option for treating moderate to severe COVID-19. [Read the Full Post]

Neoantigen-Specific T-Cell Immune Responses: The Paradigm of NPM1-Mutated Acute Myeloid Leukemia

663 | Sep 20 2021

Fabio Forghieri et al. thought that future studies were warranted to further investigate dynamics of NPM1-mutated-specific immunity and explore whether novel individualized immunotherapies might have potential clinical utility in NPM1-mutated AML patients. [Read the Full Post]

The Combined Treatment With the FLT3-Inhibitor AC220 and the Complex I Inhibitor IACS-010759 Synergistically Depletes Wt- and FLT3-Mutated Acute Myeloid Leukemia Cells

613 | Sep 20 2021

Xiyuan Lu et al. identified a novel drug combination, AC220 and IACS-010759. [Read the Full Post]

Cannabinoid receptor 2 plays a central role in renal tubular mitochondrial dysfunction and kidney ageing

751 | Sep 16 2021

Shan Zhou et al. showed CB2 played a central role in renal tubular mitochondrial dysfunction and kidney ageing. [Read the Full Post]

High WHSC1L1 Expression Reduces Survival Rates in Operated Breast Cancer Patients with Decreased CD8+ T Cells: Machine Learning Approach

784 | Sep 15 2021

Hyung-Suk Kim et al. found that VX-11e, CZC24832, LY2109761, oxaliplatin and erlotinib were effective in inhibiting breast cancer cell lines with high WHSC1L1 expression. [Read the Full Post]

Small Molecule "Silmitasertib" Repurposed as Inhibitor of Transforming Growth Factor Beta 1 for the Development of Therapeutics for Oral Submucous Fibrosis

1377 | Sep 10 2021

Nezar Boreak et al. suggested that the molecule could be validated and implemented for the treatment of OSMF. [Read the Full Post]

An Iron Shield to Protect Epigallocatehin-3-Gallate from Degradation: Multifunctional Self-Assembled Iron Oxide Nanocarrier Enhances Protein Kinase CK2 Intracellular Targeting and Inhibition

1080 | Sep 10 2021

Luca Fasolato et al. found that the nanohybrid was able to successfully deliver EGCG into cancer cells, displaying impressive protein kinase CK2 inhibition comparable to that obtained with the most specific CK2 inhibitor, CX-4945 (5.5 vs. 3 µM). [Read the Full Post]

Protective effects of the NLRP3 inflammasome against infectious bursal disease virus replication in DF-1 cells

552 | Sep 09 2021

Zhiyuan He et al. found that IBDV could induce NLRP3 inflammasome activation in DF-1 cells through a mechanism requiring viral replication. [Read the Full Post]

VX-765 ameliorates renal injury and fibrosis in diabetes by regulating caspase-1-mediated pyroptosis and inflammation

485 | Sep 09 2021

Si Wen et al. found that caspase-1-mediated pyroptosis drove renal inflammation and fibrosis in diabetes. [Read the Full Post]

Antitumor effects of AZD2014, a dual mTORC1/2 inhibitor, against human hepatocellular carcinoma xenograft in nude mice

672 | Sep 07 2021

H Liao et al. found that AZD2014 was a highly potent antitumor agent for HCC in nude mice bearing HCC xenografts. [Read the Full Post]

The balance between p53 isoforms modulates the efficiency of HIV-1 infection in macrophages

558 | Sep 06 2021

Yann Breton et al. demonstrated the involvement of p53 isoforms, which regulated p53 activity and defined the cellular environment influencing viral replication. [Read the Full Post]

P53 Is Involved in Sunitinib Resistance and Poor Progression-free Survival After Sunitinib Treatment of Renal Cell Carcinoma

577 | Sep 05 2021

Yohei Sekino et al. thought that p53 might be involved in sunitinib resistance and represent a valuable marker for sunitinib treatment in mRCC. [Read the Full Post]

Effect of Dickkopf-1 (Dkk-1) and SP600125, a JNK Inhibitor, on Wnt Signaling in Canine Prostate Cancer Growth and Bone Metastases Wachiraphan Supsavhad 1 2, Bardes B Hassan 1 3,

1494 | Sep 05 2021

Wachiraphan Supsavhad et al. showed that SP600125 had the potential to serve as an alternative adjuvant therapy in some early-stage PCa patients, especially those with high Dkk-1 expression. [Read the Full Post]

Tyrosine Kinase Inhibitors Stimulate HLA Class I Expression by Augmenting the IFNγ/STAT1 Signaling in Hepatocellular Carcinoma Cells

371 | Sep 02 2021

Aya Takahashi et al. found that regorafenib had an activating effect on signal transducers and activators of transcription 1 (STAT1), and that regorafenib-induced HLA-I expression was dependent on the augmented IFNγ/STAT1 signaling pathway. [Read the Full Post]

PI3K Promotes Basal Cell Carcinoma Growth Through Kinase-Induced p21 Degradation

402 | Sep 02 2021

Rachel Y Chow et al. suggested that PI3K promoted BCC tumor growth by kinase-induced p21 degradation without altering HH signaling. [Read the Full Post]

High-Throughput Screening Identifies Ascorbyl Palmitate As a SIRT2 Deacetylase and Defatty-Acylase Inhibitor

544 | Aug 31 2021

Jun Young Hong et al. discovered novel SIRT2 deacylase inhibitors and presented a screening approach that could be applied on a larger scale. [Read the Full Post]

Abbreviated Profile of Drugs (APOD): modeling drug safety profiles to prioritize investigational COVID-19 treatments

549 | Aug 31 2021

Chaitanya N Hiremath found that drugs with strong safety profiles included molnupiravir (EIDD-2801), moderate safety profiles included dexamethasone, and weak safety profiles included lopinavir. [Read the Full Post]

Impact of FasL Stimulation on Sclerostin Expression and Osteogenic Profile in IDG-SW3 Osteocytes

697 | Aug 30 2021

Adela Kratochvilova et al. found the caspase-independent impact of FasL stimulation. [Read the Full Post]

Inhibition of Cdc20 suppresses the metastasis in triple negative breast cancer (TNBC)

0 | Aug 29 2021

Christine Song et al.found an essential role of Cdc20 in tumor formation and metastasis of TNBC, which might be a potential target therapy for TNBC treatment. [Read the Full Post]

Phase I study of daily and weekly regimens of the orally administered MDM2 antagonist idasanutlin in patients with advanced tumors

343 | Aug 29 2021

Antoine Italiano et al. demonstrated dose- and schedule-dependent p53 activation with durable disease stabilization in some patients. [Read the Full Post]

Immunotherapy in Hepatocellular Carcinoma

1271 | Aug 27 2021

Claudia A M Fulgenzi et al. thought that in the absence of predictive biomarkers, choice of immunotherapy over kinase inhibitors would continue to remain an empirical exercise, guided by balancing anti-tumour efficacy with toxicity considerations in the individual patient. [Read the Full Post]

ARTEMIN Promotes Oncogenicity and Resistance to 5-Fluorouracil in Colorectal Carcinoma by p44/42 MAPK Dependent Expression of CDH2

1111 | Aug 25 2021

Qiu-Shi Zhuang et al. thought that ARTN might be of prognostic and theranostic utility in CRC. [Read the Full Post]

Local FK506 implants in non-human primates to prevent early acute rejection in vascularized composite allografts

984 | Aug 24 2021

Alexandre G Lellouch et al. showed preliminary results of local FK506 implants in potentially mitigating VCA acute rejection for tolerance protocols based on mixed chimerism approach. [Read the Full Post]

Phase II trial of veliparib and temozolomide in metastatic breast cancer patients with and without BRCA1/2 mutations

819 | Aug 23 2021

Jing Xu et al. found that veliparib and temozolomide demonstrated clinical activity in platinum-naïve BRCA-associated metastatic breast cancer with manageable toxicity at doses of veliparib well below the single-agent active dose. [Read the Full Post]

Poly (ADP-Ribose) Polymerase Inhibitor, ABT888, Improved Cisplatin Effect in Human Oral Cell Carcinoma

831 | Aug 23 2021

Irene Paterniti et al. indicated PARP inhibitors as adjuvants for therapeutic strategy of oral cancer. [Read the Full Post]

Interleukin-6 promotes ferroptosis in bronchial epithelial cells by inducing reactive oxygen species-dependent lipid peroxidation and disrupting iron homeostasis

318 | Aug 18 2021

Fei Han et al. found that IL-6 promoted ferroptosis in bronchial epithelial cells by inducing reactive oxygen species (ROS)-dependent lipid peroxidation and disrupting iron homeostasis. [Read the Full Post]

Ferrostatin-1 alleviated TNBS induced colitis via the inhibition of ferroptosis

380 | Aug 17 2021

Junxuan Xu et al. provided a new hopeful therapeutic strategy in treating CD, especially for those who suffered from the tolerance of existing immunosuppressive agent drugs. [Read the Full Post]

MiR-221 confers lapatinib resistance by negatively regulating p27 kip1 in HER2-positive breast cancer

1063 | Aug 16 2021

Thanh Kieu Huynh et al. suggested Src inhibition as a potential strategy to overcome lapatinib resistance. [Read the Full Post]

Calcyphosine promotes the proliferation of glioma cells and serves as a potential therapeutic target

537 | Aug 15 2021

Zheng Zhu et al. suggested that CAPS promoted the proliferation of glioma by regulating cell cycle and PLK1 inhibitor volasertib might be a chemosensitizer of glioma. [Read the Full Post]

Thermal proteome profiling identifies PIP4K2A and ZADH2 as off-targets of Polo-like kinase 1 inhibitor volasertib

502 | Aug 15 2021

Oksana Goroshchuk et al. suggested that PIP4K2A was a true off-target of volasertib. [Read the Full Post]

Sinus rhythm heart rate increase after atrial fibrillation ablation is associated with lower risk of arrhythmia recurrence

1056 | Aug 11 2021

Ammar M Killu et al. showed that relative changes in HR post AF ablation correlates with AF recurrence. [Read the Full Post]

Efficacy and Safety of Emricasan in Liver Cirrhosis and/or Fibrosis

748 | Aug 10 2021

Li-Ya Mu et al. found that treatment with emricasan was more effective in improving liver function and apoptosis parameters compared to placebo, with a well-tolerated safety profile. [Read the Full Post]

Predictors of Response and Survival to Multikinase Inhibitors in Radioiodine Resistant Differentiated Thyroid Cancer

1029 | Aug 08 2021

Tiziana Feola et al. provided an overview of the predictive factors for the response and survival of sorafenib and lenvatinib in RR-DTC. [Read the Full Post]

Verticillin A increases the BIM EL/MCL-1 ratio to overcome ABT-737-resistance in human colon cancer cells by targeting the MEK/ERK pathway

438 | Aug 08 2021

Yuelin Guan et al. suggested the potential application of Verticillin A as a MEK inhibitor in BH3-mimetic-based therapy. [Read the Full Post]

HDAC inhibitors induce LIFR expression and promote a dormancy phenotype in breast cancer

953 | Aug 06 2021

Miranda E Clements et al. suggested HDACi as a potential therapeutic avenue to promote dormancy, prevent recurrence, and improve patient outcomes in breast cancer. [Read the Full Post]

Phase I Study and Pilot Efficacy Analysis of Entinostat, a Novel Histone Deacetylase Inhibitor, in Chinese Postmenopausal Women with Hormone Receptor-Positive Metastatic Breast Cancer

1000 | Aug 06 2021

Jiani Wang et al. found that entinostat with exemestane showed reasonable safety, tolerability, and encouraging efficacy in Chinese patients with HR+/HER2- MBC. [Read the Full Post]

Local ablation of gastric cancer by reconstituted apolipoprotein B lipoparticles carrying epigenetic drugs

1298 | Aug 03 2021

Chia-Lung Yang et al. established rABL-based nanoparticles embedded epigenetic inhibitors for local treatment of gastric cancer, which had good therapeutic effects but do not cause severe side effects. [Read the Full Post]

High-Throughput Mechanistic Screening of Epigenetic Compounds for the Potential Treatment of Meningiomas

1310 | Aug 02 2021

Philip D Tatman et al. suggested an important role of HDACs in meningioma biology and as a targetable mechanism. [Read the Full Post]

Bruton's tyrosine kinase (BTK) mediates resistance to EGFR inhibition in non-small-cell lung carcinoma

801 | Aug 01 2021

Chi-Tai Yeh et al. suggested that BTK mediated stemness and EMT properties, and inhibition of BTK potentiated the effect of Gefitinib and Osimertinib in NSCLC cells resistant to TKI. [Read the Full Post]

Identification of DNA-Repair-Related Five-Gene Signature to Predict Prognosis in Patients with Esophageal Cancer

688 | Jul 30 2021

Lin Wang et al. found that small-molecule drugs (trametinib, selumetinib, and refametinib) could help to improve patient survival. [Read the Full Post]

The newly identified MEK1 tyrosine phosphorylation target MACC1 is druggable by approved MEK1 inhibitors to restrict colorectal cancer metastasis

538 | Jul 30 2021

Dennis Kobelt et al. found that MAP kinase signaling was not linear leading to ERK activation, but branched at the level of MEK1. [Read the Full Post]

BCL-XL antagonism selectively reduces neutrophil life span within inflamed tissues without causing neutropenia

341 | Jul 29 2021

Emma M Carrington et al. showed a differential survival requirement in activated neutrophils for BCL-XL and revealed a new therapeutic approach to neutrophil-mediated diseases. [Read the Full Post]

Pre-incubation with OATP1B1 and OATP1B3 inhibitors potentiates inhibitory effects in physiologically relevant sandwich-cultured primary human hepatocytes

763 | Jul 28 2021

Taleah Farasyn et al. thought that IC50 values after inhibitor-preincubation in transporter-expressing cell lines might be used for DDI prediction for the purpose of mitigating false-negative OATP-mediated DDI prediction. [Read the Full Post]

Phase 1 study combining alisertib with nab-paclitaxel in patients with advanced solid malignancies

902 | Jul 23 2021

Kian-Huat Lim et al. thought that the combination of alisertib and nab-paclitaxel had manageable side-effect profile and showed promising preliminary efficacy in high-grade NETs, warranting further testing. [Read the Full Post]

Alpelisib and radiotherapy treatment enhances Alisertib-mediated cervical cancer tumor killing

789 | Jul 23 2021

Yaman Tayyar et al. found that both RT and Alpelisib significantly improved Alisertib-mediated tumor killing. [Read the Full Post]

Incidence, predictors, and outcomes of DAPT non-compliance in planned vs. ad hoc PCI in chronic coronary syndrome

1175 | Jul 21 2021

Jahanzeb Malik et al. provided an insight on additional predictors of non-compliance to DAPT, helping us to identify and address specific patient-related factors for disruption. [Read the Full Post]

Cost-effectiveness analysis of olaparib and niraparib as maintenance therapy for women with recurrent platinum-sensitive ovarian cancer

751 | Jul 20 2021

John Hang Leung et al. showed that olaparib was considered to be a cost-effective maintenance therapy for patients with recurrent platinum-sensitive ovarian cancer from the Taiwan NHIA perspective. [Read the Full Post]

Peptide 11R‑VIVIT promotes fracture healing in osteoporotic rats

2957 | Jul 20 2021

Changju Hou et al. demonstrated that 11R‑VIVIT promoted fracture healing in osteoporotic rats and enhanced the osteogenic differentiation of osteoporotic BMSCs by dysregulating the AKT/NFATc1 signaling pathway. [Read the Full Post]

The mechanisms involved in the resistance of estrogen receptor-positive breast cancer cells to palbociclib are multiple and change over time

570 | Jul 19 2021

Mayu Ono et al. found that ER-positive breast cancer cells used multiple molecular mechanisms to survive in the presence of palbociclib. [Read the Full Post]

Targeting Pyruvate Kinase M2 phosphorylation reverses aggressive cancer phenotypes

695 | Jul 19 2021

Maria Apostolidi et al. found that combinations of Dinaciclib with TEPP-46 reduced cell invasion, impaired redox balance, and triggered cancer cell death. [Read the Full Post]

Mechanism of Ferroptosis and Its Role in Type 2 Diabetes Mellitus

681 | Jul 15 2021

Wenxin Sha et al. summarized the mechanism of ferroptosis and especially its association with type 2 diabetes mellitus (T2DM). [Read the Full Post]

Detection of autophagic flux in primary cerebral cortical neurons after oxygen glucose deprivation/reperfusion (OGD/R) using various methods

724 | Jul 12 2021

Lei Zhang et al. showed that different methods and indicators could be used to monitor different stages of autophagy. [Read the Full Post]

Successful Treatment of a Locally Recurrent and Metastatic Malignant Phyllodes Tumor with Accelerated Radiotherapy and Nab-Paclitaxel, Cisplatin, and Liposomal Doxorubicin Chemotherapy

1498 | Jul 08 2021

Ioannis M Koukourakis et al. found that the combination of cisplatin with nab-paclitaxel and liposomal doxorubicin chemotherapy had acceptable toxicity and was highly effective in eradicating metastatic lesions. [Read the Full Post]

Diffuse optical tomography breast imaging measurements are modifiable with pre-surgical targeted and endocrine therapies among women with early stage breast cancer

629 | Jul 06 2021

Julia E McGuinness et al. demonstrated that DOTBIS-derived measurements are modifiable with pre-surgical AKT inhibition and endocrine therapy. [Read the Full Post]

Differential Expression of Inflammasome-Related Genes in Induced Pluripotent Stem-Cell-Derived Retinal Pigment Epithelial Cells with or without History of Age-Related Macular Degeneration

695 | Jul 05 2021

Maria Hytti et al. suggested that cellular clearance mechanisms might already be dysfunctional, and the inflammasome activated, in cells with a disease origin. [Read the Full Post]

Monitoring of plasma concentrations of dabrafenib and trametinib in advanced BRAFV600 mut melanoma patients

704 | Jul 02 2021

M Raynal et al. thought that monitoring PCD and PCT alone was unlikely to be useful in assessing response to treatment. [Read the Full Post]

The effects of Benjakul extract and its isolated compounds on cell cycle arrest and apoptosis in human non-small cell lung cancer cell line NCI-H226

456 | Jul 02 2021

Arunporn Itharat et al. demonstrated the effects of Benjakul and its compounds on S-G2/M or G2/M phase arrest and caspase-dependent apoptosis in lung cancer cells. [Read the Full Post]

Using JAK inhibitor to treat cytokine release syndrome developed after chimeric antigen receptor T cell therapy for patients with refractory acute lymphoblastic leukemia: A case report

1000 | Jun 30 2021

Fu Ming Zi et al. found that Ruxolitinib could be used as an alternative therapeutic approach for severe and refractory CRS without impairing CAR-T amplification and anti-tumor effect. [Read the Full Post]

Suppression of Microgliosis With the Colony-Stimulating Factor 1 Receptor Inhibitor PLX3397 Does Not Attenuate Memory Defects During Epileptogenesis in the Rat

589 | Jun 29 2021

Season K Wyatt-Johnson eal. revealed that PLX3397 did not improve or worsen the memory deficits in rats that sustained pilocarpine-induced SE. [Read the Full Post]

Recurrent Mutations in Cyclin D3 Confer Clinical Resistance to FLT3 Inhibitors in Acute Myeloid Leukemia

702 | Jun 28 2021

Catherine C Smith et al. thought that Mutations in CCND3, a gene not commonly mutated in AML, were a novel cause of clinical primary resistance to FLT3 inhibitors in AML and might have sensitivity to CDK4/6 inhibition. [Read the Full Post]

Identification of autophagy-related genes as targets for senescence induction using a customizable CRISPR-based suicide switch screen

259 | Jun 27 2021

Arnout Schepers et al. presented a suicide switch system that allowed genome-wide CRISPR screening in growth-arrested subpopulations by eliminating the proliferating cells during the screen through activation of a suicide switch in proliferating cells. [Read the Full Post]

Structure-Based Design of A-1293102, a Potent and Selective BCL-X L Inhibitor

294 | Jun 25 2021

Zhi-Fu Tao et al. thought that A-1293102 represented one of the few distinct structural series of selective BCL-XL inhibitors, and thus served as a useful tool for biological studies as well as a lead compound for further optimization. [Read the Full Post]

Immunomodulatory effects of different intravenous immunoglobulin preparations in chronic lymphocytic leukemia

412 | Jun 24 2021

Ana Colado et al. showed that the IgM/IgA enriched preparation not only affected relevant mechanisms involved in CLL pathogenesis but also had a particular profile of immunomodulatory effects on T cells that deserved further investigation. [Read the Full Post]

The KRAS G12C Inhibitor MRTX849 Reconditions the Tumor Immune Microenvironment and Sensitizes Tumors to Checkpoint Inhibitor Therapy

785 | Jun 22 2021

David M Briere et al. demonstrated KRAS inhibition reversed an immunosuppressive tumor microenvironment and sensitized tumors to CIT through multiple mechanisms. [Read the Full Post]

Ivacaftor-elexacaftor-tezacaftor and tacrolimus combination in cystic fibrosis

626 | Jun 21 2021

Megan Smith et al. described a pediatric liver transplant recipient with clinical decline related to cystic fibrosis who improved substantially with ETI, without significant impact on the systemic exposure of either ETI or tacrolimus. [Read the Full Post]

Flurbiprofen as a biphenyl scaffold for the design of small molecules binding to PD-L1 protein dimer

977 | Jun 20 2021

Christian Bailly et al. found that the longer FLB derivative HCT1026 appeard as a suitable binder of the PD-L1 dimer, sliding well along the BMS binding cavity. [Read the Full Post]

Inhibitory Effect of a Glutamine Antagonist on Proliferation and Migration of VSMCs via Simultaneous Attenuation of Glycolysis and Oxidative Phosphorylation

868 | Jun 19 2021

Hyeon Young Park et al. found that treatment with a glutamine antagonist is a promising approach to prevent progression of atherosclerosis and restenosis. [Read the Full Post]

Genetic variant within CDK6 regulates immune response to palbociclib treatment

677 | Jun 17 2021

Valentina Serra et al. suggested that the effect of palbociclib treatment might depend on underlying genetically encoded individual immune response as well as the direct response to the drug. [Read the Full Post]

Treatment outcomes of erlotinib plus gemcitabine as late-line chemotherapy in unresectable pancreatic cancer

847 | Jun 16 2021

Takafumi Mie et al. found that benefits of erlotinib plus gemcitabine as late-line chemotherapy were limited, particularly with respect to PFS. [Read the Full Post]

Impact of tumor growth rate during preceding treatment on tumor response to nivolumab or irinotecan in advanced gastric cancer

721 | Jun 15 2021

K Kato et al. suggested that NIVO treatment was a more favorable option for patients with slow-growing tumors, and NIVO and IRI were similarly recommended for patients with rapid-growing tumors in refractory AGC. TGR and NL emergence during preceding treatment might be helpful for drug selection and warrant further investigation. [Read the Full Post]

YAP/TAZ suppress drug penetration into hepatocellular carcinoma via stromal activation

1246 | Jun 15 2021

Kyungjoo Cho et al. indicated that drug delivery into liver cancer was impaired by YAP/TAZ signaling in tumor cells and subsequent activation of stroma by the signaling. [Read the Full Post]

Pralsetinib for patients with advanced or metastatic RET-altered thyroid cancer (ARROW): a multi-cohort, open-label, registrational, phase 1/2 study

640 | Jun 14 2021

Vivek Subbiah et al. found that Pralsetinib was a new, well-tolerated, potent once-daily oral treatment option for patients with RET-altered thyroid cancer. [Read the Full Post]

Real-world-evidence-for-carfilzomib-dosing-intensity-on-overall-survival-and-treatment-progression-in-multiple-myeloma-patients

849 | Jun 13 2021

Noopur Raje found that patient outcomes could be improved if eligible MM patients are treated with the optimized [Read the Full Post]

Early Exanthema Upon Vemurafenib Plus Cobimetinib Is Associated With a Favorable Treatment Outcome in Metastatic Melanoma: A Retrospective Multicenter DeCOG Study

501 | Jun 13 2021

Katharina C Kähler et al. found that favorable therapy outcome upon vemurafenib plus cobimetinib. [Read the Full Post]

Tofacitinib Therapy in Children and Young Adults with Pediatric-Onset Medically-Refractory Inflammatory Bowel Disease

758 | Jun 07 2021

Hillary Moore et al. found that tofacitinib induced rapid clinical response with sustained efficacy in nearly half of subjects. [Read the Full Post]

Modeling clinical responses to targeted therapies by patient-derived organoids of advanced lung adenocarcinoma

730 | Jun 06 2021

Seok-Young Kim et al. demonstrated translational relevance of PDOs in advanced lung adenocarcinoma. [Read the Full Post]

[Molecular background of BRAF inhibitor induced resistance in BRAFV600E mutant melanoma cell lines]

506 | Jun 04 2021

István Szász et al. found that withdrawal of the inhibitor reduced cell proliferation in the resistant cells. [Read the Full Post]

Analysis of chemotherapy-induced peripheral neuropathy using the Japanese Adverse Drug Event Report database

981 | Jun 02 2021

Misaki Inoue et al. revealed several drugs associated with a high risk for CIPN development. [Read the Full Post]

Bintrafusp alfa (M7824), a bifunctional fusion protein targeting TGF-β and PD-L1: results from a phase I expansion cohort in patients with recurrent glioblastoma Mustafa Khasraw 1 2,

704 | Jun 01 2021

[Read the Full Post]

TIP30 overcomes gefitinib resistance by regulating cytoplasmic and nuclear EGFR signaling in non-small cell lung cancer

679 | Jun 01 2021

Shuai Shuai et al. revealed that TIP30 overexpression restored gefitinib sensitivity in NSCLC cells and attenuated the cytoplasmic and nuclear EGFR signaling pathways. [Read the Full Post]

Ivacaftor Inhibits Glioblastoma Stem Cell Maintenance and Tumor Progression

991 | May 30 2021

Kun Liu et al. demonstrated that ivacaftor decreased stemness marker gene expressions of GSCs, including CD133, CD44, and Sox2. [Read the Full Post]

The efficacy and safety of niraparib for ovarian cancer: a single-center observational study from China

1229 | May 28 2021

Jing Ni et al. found that it was feasible that patients receiving a bolus of 200 mg/d in patients from Chinese population could acquire promising efficacy and tolerance. [Read the Full Post]

High response rate and durability driven by HLA genetic diversity in kidney cancer patients treated with the immunotherapy combination lenvatinib and pembrolizumab

562 | May 28 2021

Chung-Han Lee et al. identified lenvatinib plus pembrolizumab as a highly active treatment strategy in RCC and reveal HLA-I diversity as a critical determinant of efficacy for this combination. [Read the Full Post]

ALK-negative lung inflammatory myofibroblastic tumor in a young adult: A case report and literature review of molecular alterations

961 | May 24 2021

Silvia Angela Debonis et al. thought that although there was no standard of care for the treatment of IMT, identifying genomic alterations could help to redefine the management of patients with negative-ALK disease. [Read the Full Post]

Treatment of Luminal Metastatic Breast Cancer beyond CDK4/6 Inhibition: Is There a Standard of Care in Clinical Practice?

1586 | May 21 2021

Athanasios Mavratzas et al. thought that treatment of metastatic luminal breast cancer after progression on CDK4/6 inhibitors remained a challenge. [Read the Full Post]

Thyroglobulin as a negative marker for malignancy in canine and human breast tumors

946 | May 19 2021

Sung-Hyun Hwang et al. found that Tg could be a negative indicator of malignancy in canine and human breast neoplasia. [Read the Full Post]

Liver injury in COVID-19 and IL-6 trans-signaling-induced endotheliopathy

713 | May 17 2021

Matthew J McConnell et al. thought that COVID-19 was associated with coagulopathy and endotheliopathy in the liver endothelium driven by IL-6 trans-signaling, a possible mechanism of liver injury. [Read the Full Post]

Inhibition of the Histone Methyltransferase EZH2 Enhances Protumor Monocyte Recruitment in Human Mesothelioma Spheroids

1042 | May 17 2021

Silvia Mola et al. found that TAMs were a driving force for MPM growth, progression, and resistance to tazemetostat. [Read the Full Post]

Effects of orlistat combined with enzalutamide and castration through inhibition of fatty acid synthase in a PC3 tumor-bearing mouse model

356 | May 12 2021

Yeu-Sheng Tyan et al. found the synergistic effects of orlistat combined with enzalutamide in vitro and castration in vivo on human prostate cancer. [Read the Full Post]

Nonsense-mediated mRNA decay efficiency influences bleeding severity in ITGA2B c.2659C > T (p.Q887X) knock-in mice

824 | May 10 2021

Zhanli Xie et al. found that NMD efficiency potentially influenced bleeding severity in ITGA2B c.2659C > T (p.Q887X) KI mice. [Read the Full Post]

High BRCA2 Gene Expression is Associated with Aggressive and Highly Proliferative Breast Cancer

742 | May 10 2021

Vikas Satyananda et al. thought that BRCA2 gene expression might become a candidate marker for aggressive biology and to tailor specific treatment strategies in the future. [Read the Full Post]

Novel human-derived RET fusion NSCLC cell lines have heterogeneous responses to RET inhibitors and differential regulation of downstream signaling

551 | May 09 2021

Laura Schubert et al. demonstrated that the RET inhibitor BLU-667 was effective at inhibiting tumor growth in CUTO42 tumors, but had a much less profound effect in CUTO32 tumors, consistent with in vitro experiments. [Read the Full Post]

Targeting MCL-1 dysregulates cell metabolism and leukemia-stroma interactions and resensitizes acute myeloid leukemia to BCL-2 inhibition

233 | May 05 2021

Bing Z Carter et al. found that co-targeting MCL-1 and BCL-2 improved the efficacy of and overcame preexisting and acquired resistance to BCL-2 inhibition. [Read the Full Post]

Discovery of S64315, a Potent and Selective Mcl-1 Inhibitor

375 | May 04 2021

Zoltan Szlavik et al. reported the discovery of clinical candidate S64315, a selective small molecule inhibitor of Mcl-1. [Read the Full Post]

Simultaneously Inhibiting BCL2 and MCL1 Is a Therapeutic Option for Patients with Advanced Melanoma

289 | May 04 2021

Nabanita Mukherjee et al. suggested that several pro-apoptotic BCL2 family members, BCL2-like 11 (apoptosis facilitator) (BIM), phorbol-12-myristate-13-acetate-induced protein 1 (NOXA) or BID, played a role in the combination-induced effects. [Read the Full Post]

Direct Conjugation of NEDD8 to the N-Terminus of a Model Protein Can Induce Degradation

673 | May 03 2021

Kartikeya Vijayasimha et al. suggested that under certain conditions, such as the model system described here, the covalent linkage of NEDD8 to a protein substrate might result in the target proteins degradation. [Read the Full Post]

SLFN11 inactivation induces proteotoxic stress and sensitizes cancer cells to ubiquitin activating enzyme inhibitor TAK-243

658 | May 01 2021

Yasuhisa Murai et al. found that findings uncover a previously unknown function of SLFN11 as a regulator of protein quality control and attenuator of ER stress and UPR. Moreover, they suggest the potential value of TAK-243 in SLFN11-deficient tumors. [Read the Full Post]

Glutamine deficiency promotes stemness and chemoresistance in tumor cells through DRP1-induced mitochondrial fragmentation

569 | Apr 27 2021

Parash Prasad et al. suggested that glutamine deficiency in the core of tumors could increase the cancer stem cell population and the combination therapy with MDiVi-1 and L-DON was a useful approach to reduce CSCs population in tumor. [Read the Full Post]

Loss of FADD and Caspases Affects the Response of T-Cell Leukemia Jurkat Cells to Anti-Cancer Drugs

551 | Apr 26 2021

Zuzana Mrkvová et al. thought that a combination of TNF-α and smac mimetic could be a suitable strategy for overcoming resistance to therapy in cells unable to trigger apoptosis. [Read the Full Post]

H3K36 methylation reprograms gene expression to drive early gametocyte development in Plasmodium falciparum

776 | Apr 25 2021

Jessica Connacher et al. found that H3K36me2&3-associated repression of genes was therefore involved in key transcriptional shifts that accompanied the transition from early gametocyte differentiation to intermediate development. [Read the Full Post]

Synthesis and Evaluation of Biphenyl-1,2,3-Triazol-Benzonitrile Derivatives as PD-1/PD-L1 Inhibitors

710 | Apr 23 2021

Suresh Narva et al. thought that compound 7 was thus a promising candidate for further optimization as an inhibitor of the PD-1/PD-L1 signaling pathway. [Read the Full Post]

Therapeutic targeting PLK1 by ON-01910.Na is effective in local treatment of retinoblastoma

857 | Apr 21 2021

Huan Ma et al. demonstrated targetability of PLK1 in retinoblastoma by efficiently causing cell cycle arrest and apoptosis. [Read the Full Post]

A Contaminant Impurity, Not Rigosertib, Is a Tubulin Binding Agent

884 | Apr 21 2021

Stacey J Baker et al. found that these cells failed to proliferate in the presence of rigosertib at concentrations that are lethal to wild-type cells. [Read the Full Post]

The molecular context of vulnerability for CDK9 suppression in triple wild-type melanoma

455 | Apr 19 2021

Samantha M Guhan et al. found that transcriptional blockade through selective targeting of CDK9 was an effective method of suppressing therapeutically-orphaned BRAF/NRAS/NF1 wild-type melanomas. [Read the Full Post]

Inhibiting Importin 4-mediated nuclear import of CEBPD enhances chemosensitivity by repression of PRKDC-driven DNA damage repair in cervical cancer

543 | Apr 19 2021

Yang Zhou et al. demonstrated that IPO4 and CEBPD knockdown improved CDDP-induced cytotoxicity in vitro and in vivo. [Read the Full Post]

The clinical significance of histone deacetylase-8 in human breast cancer

688 | Apr 13 2021

Golebagh Rahmani et al. highlighted the role and existing inhibitors of HDAC8 in BC pathogenesis and therapy. [Read the Full Post]

Porcine Picornavirus 3C Protease Degrades PRDX6 to Impair PRDX6-mediated Antiviral Function

443 | Apr 12 2021

Congcong Wang et al. found that PRDX6 played an important antiviral role during porcine picornavirus infection, and the viral 3Cpro induced the degradation of PRDX6 to overcome PRDX6-mediated antiviral function. [Read the Full Post]

Emerging Effects of Sepantronium Bromide (YM155) on MOLT-4 Cell Line Apoptosis Induction and Expression of Critical Genes Involved in Apoptotic Pathways

480 | Apr 11 2021

Kobra Shojaei Moghadam found that use of YM155 could be a potential drug therapy in T-ALL patients with promising effects on apoptosis induction. [Read the Full Post]

A transposon screen identifies enhancement of NF-κB pathway as a mechanism of resistance to eribulin

1046 | Apr 08 2021

Xiaozhong Teng et al. supported the use of a combination strategy of eribulin with NF-κB inhibitors, and provided evidence that transposon mutagenesis screens were capable of identifying drug-resistant genes. [Read the Full Post]

LncRNA XIST promotes inflammation by downregulating GRα expression in the adenoids of children with OSAHS

492 | Apr 08 2021

Zhen Zhou et al. demonstrated that the XIST-GRα-NF-κB signaling pathway contributed to inflammation in the adenoids of patients with OSAHS. [Read the Full Post]

Melanin Distribution in Human Skin: Influence of Cytoskeletal, Polarity, and Centrosome-Related Machinery of Stratum basale Keratinocytes

1383 | Apr 06 2021

Irene Castellano-Pellicena et al. explored the role of actin, microtubules, and centrosome-associated machinery in distributing melanin within KCs. [Read the Full Post]

In vivo Pharmacokinetic Drug-Drug Interaction Studies Between Fedratinib and Antifungal Agents Based on a Newly Developed and Validated UPLC/MS-MS Method

1102 | Apr 04 2021

Congrong Tang et al. thought that the toxicity of fedratinib should be avoided when the concurrent use of fedratinib with CYP3A4 inhibitors might occur. [Read the Full Post]

Current Clinical Investigations in Myelofibrosis

1217 | Apr 04 2021

Sangeetha Venugopal et al. provided insight into the novel therapies under clinical evaluation. [Read the Full Post]

Protective effects of NAC and salubrinal on apoptosis of retinal pigment epithelial cells induced by all-trans retinoic acid

1287 | Apr 02 2021

Juan Wu et al. thought that ATRA might play an important role in the prevention, diagnosis and treatment of age-related macular degeneration. [Read the Full Post]

Nucleotide variation in histone H2BL drives crossalk of histone modification and promotes tumour cell proliferation by upregulating c-Myc

634 | Mar 30 2021

Lei Zhang et al. revealed that an H2BK5ac-H2BK120ubi crosstalk which regulates gene transcription. [Read the Full Post]

Pharmacological inhibition of IKKβ dampens NLRP3 inflammasome activation after priming in the human myeloid cell line THP-1

975 | Mar 25 2021

Adeline Unterreiner et al. suggested that IκKβ might fulfill a dual role in coupling priming and activation of the NLRP3 inflammasome. [Read the Full Post]

Inhibition of HDAC6 by Tubastatin A reduces chondrocyte oxidative stress in chondrocytes and ameliorates mouse osteoarthritis by activating autophagy

761 | Mar 24 2021

Zhonghai Shen et al. thought that HDAC6 inhibition prevented OA development, and HDAC6 could be applied as a potential therapeutic target for OA management. [Read the Full Post]

Targeting phosphoinositide 3-kinases and histone deacetylases in multiple myeloma

851 | Mar 19 2021

Seiichi Okabe et al. suggested that the administration of CUDC-907 might be a powerful strategy against myeloma cells, to enhance the cytotoxic effects of proteasome inhibitors. [Read the Full Post]

Reversal of Cancer Multidrug Resistance (MDR) Mediated by ATP-Binding Cassette Transporter G2 (ABCG2) by AZ-628, a RAF Kinase Inhibitor

298 | Mar 16 2021

Jing-Quan Wang et al. indicated that AZ-628 could be used in combination chemotherapy against ABCG2-mediated MDR in cancers. [Read the Full Post]

Cardioautonomic control in healthy singleton and twin pregnancies

828 | Mar 16 2021

Victoria L Meah wt al. suggested that individuals with twin pregnancies had greater sympathetic and lower parasympathetic contributions to heart rate and that cardiac, but not vascular, autonomic control was impacted during twin compared to singleton pregnancy. [Read the Full Post]

Differential Outcomes in Codon 12/13 and Codon 61 NRAS-Mutated Cancers in the Phase 2 NCI-MATCH Trial of Binimetinib in Patients with NRAS-Mutated Tumors

678 | Mar 07 2021

James M Cleary et al. thought that the observation of increased OS and PFS in codon 61 NRAS-mutated colorectal cancer patients merited further investigation. [Read the Full Post]

Mnk inhibitors: a patent review

1533 | Mar 07 2021

Ahmed M Abdelaziz et al. provided a succinct review of the current state of development of pyridone-aminal-derived Mnk inhibitors through the analysis of relevant patent applications filed in the last 5 years. [Read the Full Post]

Kinesin-7 CENP-E regulates the formation and structural maintenance of the acrosome

710 | Mar 06 2021

Zhen-Yu She et al. found that light on the molecular mechanisms involved in vesicle trafficking and architecture maintenance of the acrosome. [Read the Full Post]

Manipulating bovine granulosa cell energy metabolism limits inflammation

868 | Mar 03 2021

Anthony D Horlock et al. implied that energy stress compromised ovarian follicle immune defences. [Read the Full Post]

CD8 lymphocyte depletion enhances the latency reversal activity of the SMAC mimetic AZD5582 in ART-suppressed SIV-infected rhesus macaques

384 | Mar 01 2021

Maud Mavigner et al. suggested that the latency reversal induced by activation of the ncNF-κB signaling pathway with AZD5582 could be enhanced by CD8α+ cell depletion. [Read the Full Post]

Inhibition of ATM induces hypersensitivity to proton irradiation by upregulating toxic end joining

541 | Feb 28 2021

Qin Zhou et al. found that inherent defects in HR or administration of an ATM inhibitor in HR proficient tumors selectively enhanced the relative biological effectiveness of proton Bragg peak irradiation. [Read the Full Post]

Sensitization of head and neck squamous cell carcinoma to apoptosis by combinational SMAC mimetic and Fas ligand-Fc treatment in vitro

272 | Feb 26 2021

Roman C Brands et al. identified SMAC mimetics, particularly BV-6 as the compound with the highest pro-apoptotic potency, as promising antitumor agents. [Read the Full Post]

Discovery of repurposing drug candidates for the treatment of diseases caused by pathogenic free-living amoebae

1023 | Feb 25 2021

Christopher A Rice et al. demonstrated the utility of phenotypic screens for discovery of new drugs for pathogenic free-living amoebae, including Acanthamoeba for the first time. [Read the Full Post]

Correction of eIF2-dependent defects in brain protein synthesis, synaptic plasticity, and memory in mouse models of Alzheimer's disease

898 | Feb 24 2021

Mauricio M Oliveira et al. found that attenuating the ISR downstream of phosphorylated eIF2α might restore hippocampal protein synthesis and delay cognitive decline in AD patients. [Read the Full Post]

Priming with HDAC Inhibitors Sensitizes Ovarian Cancer Cells to Treatment with Cisplatin and HSP90 Inhibitors

895 | Feb 24 2021

Ana J Rodrigues Moita et al. found that priming with HDACi sensitized ovarian cancer cells to treatment with HSP90i or cisplatin and had an influence on the development of cisplatin resistance, both of which might contribute to an improved ovarian cancer treatment. [Read the Full Post]

Structure-based discovery of 1H-indole-2-carboxamide derivatives as potent ASK1 inhibitors for potential treatment of ulcerative colitis

730 | Feb 23 2021

Shaohua Hou et al. suggested that ASK1 inhibitors could potentially be used as a therapeutic strategy for UC. [Read the Full Post]

EGR1 knockdown alleviates the cerebral injury in rats with intracerebral hemorrhage (ICH) via STAT3/NF-κB pathway by reducing RXRα acetylation level

707 | Feb 23 2021

Lijuan Xie et al. found that EGR1 increased RXRα acetylation level by regulating p300, thereby aggravating brain damage in ICH rat model and dysfunction in BMECs, which might through the STAT3/NF-κB pathway. [Read the Full Post]

Selonsertib, a potential drug for liver failure therapy by rescuing the mitochondrial dysfunction of macrophage via ASK1-JNK-DRP1 pathway

763 | Feb 22 2021

Guohua Lou et al. thought that selonsertib protected against LPS/GalN-induced ALF by attenuating JNK-mediated DRP1 mitochondrial translocation and then rescuing mitochondrial damage in macrophages and might have therapeutic potential for early ALF patients. [Read the Full Post]

More Insights on the Use of γ-Secretase Inhibitors in Cancer Treatment

864 | Feb 21 2021

Pilar López-Nieva et al. suggested that selective targeting γ-secretase might offer an improved efficacy and toxicity profile over the effects caused by broad-spectrum GSIs. [Read the Full Post]

Active notch protects MAPK activated melanoma cell lines from MEK inhibitor cobimetinib

834 | Feb 19 2021

Letizia Porcelli et al. unveiled a coordinate action of MAPK and Notch signaling in promoting proliferation of BRAFV600E MM and GNAQQ209L UM cells. [Read the Full Post]

Multi-functionalised graphene nanoflakes as tumour-targeting theranostic drug-delivery vehicles

695 | Feb 16 2021

Jennifer Lamb et al. showed that GNFs were suitable candidates for use in theranostic drug design. [Read the Full Post]

enAsCas12a Enables CRISPR-Directed Evolution to Screen for Functional Drug Resistance Mutations in Sequences Inaccessible to SpCas9

624 | Feb 14 2021

Jasper Edgar Neggers et al. demonstrated that enAsCas12a is a promising new addition to the CRISPR screening toolbox and allows targeting sites not readily accessible to SpCas9. [Read the Full Post]

The application of nanoparticles in cancer immunotherapy: Targeting tumor microenvironment

1012 | Feb 13 2021

Muyue Yang et al. found that the changes of TME at various stages during tumor development are required to be further elucidated so that more individualized nanoplatforms could be designed. [Read the Full Post]

Selective reactivation of STING signaling to target Merkel cell carcinoma

1100 | Feb 13 2021

Wei Liu et al. found that targeted delivery and activation of STINGS162A/G230I/Q266I in tumor cells held great therapeutic promise for the treatment of MCC and many other STING-deficient cancers. [Read the Full Post]

Hospitalization and Mortality in Patients With Heart Failure Treated With Sacubitril/Valsartan vs. Enalapril: A Real-World, Population-Based Study

791 | Feb 12 2021

Swathi Pathadka et al. found that in real-world settings, sacubitril/valsartan was associated with improved survival and reduced heart failure-related hospitalization compared to enalapril in Asian patients with heart failure. [Read the Full Post]

Albendazole-Induced SIRT3 Upregulation Protects Human Leukemia K562 Cells from the Cytotoxicity of MCL1 Suppression

245 | Feb 12 2021

Liang-Jun Wang et al. demonstrated that ABZ-induced SIRT3 upregulation delayed the apoptosis-inducing effect of MCL1 suppression on apoptosis induction in K562 cells. [Read the Full Post]

BMI1-Inhibitor PTC596 in Combination with MCL1 Inhibitor S63845 or MEK Inhibitor Trametinib in the Treatment of Acute Leukemia

422 | Feb 08 2021

Katja Seipel et al. thought that the combination of PTC596 and S63845 might be an effective treatment in CD34+ adverse risk AML with elevated MN1 gene expression and MCL1 protein levels. [Read the Full Post]

A thiol-bound drug reservoir enhances APR-246-induced mutant p53 tumor cell death

506 | Feb 08 2021

Sophia Ceder et al. found that redox homeostasis was a critical determinant of the response to mutant p53-targeted cancer therapy. [Read the Full Post]

STAT3 Is an Upstream Regulator of Granzyme G in the Maternal-To-Zygotic Transition of Mouse Embryos

513 | Feb 05 2021

Huan Ou-Yang et al. suggested that STAT3, a maternal protein, was a critical transcription factor and regulated Gzmg transcription activity in preimplantation mouse embryos. [Read the Full Post]

Canadian Consensus for Biomarker Testing and Treatment of TRK Fusion Cancer in Adults

596 | Feb 01 2021

D Gwyn Bebb et al. recommend considering a TRK inhibitor in all patients with TRK fusion cancer with no other effective treatment options. [Read the Full Post]

Neutrophil Extracellular Traps in Atherosclerosis and Thrombosis

918 | Jan 30 2021

Thomas M Hofbaue et al. found mechanisms of NET formation, evidence for their involvement in atherosclerosis and thrombosis, and potential therapeutic regimens specifically targeting NET components. [Read the Full Post]

Differential functional roles of fibroblasts and pericytes in the formation of tissue-engineered microvascular networks in vitro

803 | Jan 27 2021

Natalia Kosyakova et al. described the differential effects that two widely used stromal cell populations, fibroblasts (FBs) and pericytes (PCs), had on μVN formation. [Read the Full Post]

De novo protein synthesis is necessary for priming in preclinical models of migraine

1148 | Jan 26 2021

Jacob Lackovic et al. suggested that targeting the regulation of protein synthesis might be a novel approach for new migraine treatment strategies. [Read the Full Post]

Suppression of MET signaling mediated by pitavastatin and capmatinib inhibits oral and esophageal cancer cell growth

869 | Jan 26 2021

Bo Xu et al. suggested that the combination of pitavastatin with capmatinib was a useful therapeutic strategy in OSCC and ESCC. [Read the Full Post]

Valve endothelial-interstitial interactions drive emergent complex calcific lesion formation in vitro

644 | Jan 24 2021

Terence W Gee et al. established that VEC actively induced VIC pathological remodeling and calcification via EndMT and paracrine signaling. [Read the Full Post]

Hypoxic modulation of fetal vascular MLCK abundance, localization, and function

634 | Jan 23 2021

Dane W Sorensen et al. found that changes in MLCK distribution are a significant component of fetal vascular responses to hypoxia. [Read the Full Post]

MDM2 inhibition: an important step forward in cancer therapy

567 | Jan 21 2021

Marina Konopleva et al. thought that targeting MDM2 was a promising treatment strategy. [Read the Full Post]

Histone methyltransferase DOT1L coordinates AR and MYC stability in prostate cancer

709 | Jan 17 2021

R Vatapalli et al. thought that DOT1L selectively regulated the tumorigenicity of AR-positive prostate cancer cells and was a promising therapeutic target for PCa. [Read the Full Post]

Salvianolate ameliorates oxidative stress and podocyte injury through modulation of NOX4 activity in db/db mice

883 | Jan 17 2021

Yiran Liang et al. identified that Salvianolate could prevent glucose-induced oxidative podocyte injury through modulation of NOX4 activity in DN and had a novel therapeutic potential for DN. [Read the Full Post]

Role of necroptosis in chronic hepatic inflammation and fibrosis in a mouse model of increased oxidative stress

332 | Jan 16 2021

Sabira Mohammed et al. found that necroptosis-mediated inflammation contributed to fibrosis in a mouse model of increased oxidative stress and accelerated aging, that also exhibited progressive HCC development. [Read the Full Post]

Kanglexin accelerates diabetic wound healing by promoting angiogenesis via FGFR1/ERK signaling

498 | Jan 15 2021

Yixiu Zhao et al. thought that KLX had the potential to be developed as a topical drug to promote diabetic wound healing. [Read the Full Post]

Nanog maintains stemness of Lkb1-deficient lung adenocarcinoma and prevents gastric differentiation

953 | Jan 15 2021

Xinyuan Tong et al. uncovered a previously unappreciated plasticity of LKB1-deficient tumors and identified the Nanog-Notch axis in regulating gastric differentiation, which hold important therapeutic implication for the treatment of mucinous lung cancer. [Read the Full Post]

MOMENTUM: momelotinib vs danazol in patients with myelofibrosis previously treated with JAKi who are symptomatic and anemic

949 | Jan 13 2021

Srdan Verstovsek et al.showed that the MOMENTUM Phase III study was designed to confirm and extend observations of safety and clinical activity of MMB. [Read the Full Post]

CYT387, a Novel JAK2 Inhibitor, Suppresses IL-13-Induced Epidermal Barrier Dysfunction Via miR-143 Targeting IL-13Rα1 and STAT3

1039 | Jan 13 2021

Yan Zu et al. revealed that the protective effects and the underlying mechanisms of CYT387 in AD, which provided evidence that miR-143 might be a novel therapeutic target for AD. [Read the Full Post]

CB 1 Cannabinoid Receptors Stimulate Gβγ-GRK2-Mediated FAK Phosphorylation at Tyrosine 925 to Regulate ERK Activation Involving Neuronal Focal Adhesions

839 | Jan 12 2021

George D Dalton et al. found that FAK 925 Tyr-P occured concurrently with CB1-stimulated ERK2 activation and required the actin cytoskeleton and Gi/oβγ-GRK2-mediated cross-talk between CB1, integrins, and receptor tyrosine kinases (RTKs). [Read the Full Post]

Pergularia daemia alters epileptogenesis and attenuates cognitive impairment in kainate-treated mice: Insight into anti-inflammatory mechanisms

972 | Jan 12 2021

Antoine Kavaye Kandeda et al. suggested that anti-inflammatory mechanisms were involved in the antiepileptogenic effect of P. daemia extract. [Read the Full Post]

Effects and Mechanism of Action of PX-478 in Oxygen-Induced Retinopathy in Mice

636 | Jan 07 2021

Xiaoyan Pan et al. found that HIF-1α played a main role in OIR and could be considered a therapeutic target in OIR by suppressing downstream angiogenic factors, PX-478 decreasing the retinal avascular area and NV. [Read the Full Post]

Repurposing FDA Approved Drugs as JNK3 Inhibitor for Prevention of Neuroinflammation Induced by MCAO in Rats

730 | Jan 06 2021

Zikra Zulfiqar et al. demonstrated that the novel FDA-approved medications attenuate ischemic stroke-induced neuronal degeneration, possibly by inhibiting JNK3. [Read the Full Post]

Kinase activity-independent role of EphA2 in the regulation of M-phase progression

563 | Jan 04 2021

Yuichiro Kaibori et al. suggested that EphA2 regulated M-phase progression in a manner independent of its kinase activity. [Read the Full Post]

Synergistic Utilization of Necrostatin-1 and Z-VAD-FMK Efficiently Promotes the Survival of Compression-Induced Nucleus Pulposus Cells via Alleviating Mitochondrial Dysfunction

825 | Jan 03 2021

Songfeng Chen et al. found that the synergistic utilization of Necrostatin-1 and Z-VAD-FMK was a very worthwhile solution in preventing compression-mediated NP cells death, which might be largely attributed to restored mitochondrial function. [Read the Full Post]

Identification of SARS-CoV-2 3CL Protease Inhibitors by a Quantitative High-Throughput Screening

484 | Jan 02 2021

Wei Zhu et al. demonstrated a set of SARS-CoV-2 3CLpro inhibitors that might have potential for further clinical evaluation as part of drug combination therapies to treating COVID-19 patients and as starting points for chemistry optimization for new drug development. [Read the Full Post]

HDAC6 Degradation Inhibits the Growth of High-Grade Serous Ovarian Cancer Cells

751 | Jan 01 2021

Ahlam Ali et al. found that inhibition of HDAC6 catalytic activity with first generation HDAC6 inhibitors has limited efficacy as a monotherapy in HGSOC. [Read the Full Post]

A High-Content Screen for Mucin-1-Reducing Compounds Identifies Fostamatinib as a Candidate for Rapid Repurposing for Acute Lung Injury

604 | Dec 29 2020

Maria Kost-Alimova et al. suggested fostamatinib as a repurposing drug candidate for ALI. [Read the Full Post]

Gli affects the stemness and prognosis of epithelial ovarian cancer via homeobox protein NANOG

729 | Dec 28 2020

Huan Zhao et al. found that Gli and NANOG might be effective indicators of platinum resistance and prognosis in EOC. [Read the Full Post]

The phosphorylation of CHK1 at Ser345 regulates the phenotypic switching of vascular smooth muscle cells both in vitro and in vivo

469 | Dec 25 2020

Chen Xin et al. demonstrated that phosphorylation of CHK1 under DNA damage stress modulated VSMCs phenotypic switching. [Read the Full Post]

ScatLay: utilizing transcriptome-wide noise for identifying and visualizing differentially expressed genes

556 | Dec 24 2020

Thuy Tien Bui et al. provided a wider coverage of DE genes, and would likely pave way for finding more novel regulatory genes in future works. [Read the Full Post]

HSP90 Inhibitor Ganetespib (STA-9090) Inhibits Tumor Growth in c-Myc-Dependent Esophageal Squamous Cell Carcinoma

872 | Dec 17 2020

Liuliu Guan et al. supported that the HSP90 inhibitor, STA-9090, suppressed the expression of the MYC protein and interferes with HSP90-MYC protein-protein interaction. [Read the Full Post]

Ganetespib in Combination with Pemetrexed-Platinum Chemotherapy in Patients with Pleural Mesothelioma (MESO-02): A Phase Ib Trial

887 | Dec 16 2020

Dean A Fennell et al. found that ganetespib could be combined safely with pemetrexed and platinum chemotherapy to treat patients with MPM. [Read the Full Post]

Poziotinib suppresses ovarian cancer stem cell growth via inhibition of HER4-mediated STAT5 pathway

745 | Dec 15 2020

Heejin Lee et al. suggested that HER4 might be a promising therapeutic target for ovarian CSCs, and that poziotinib might be an effective therapeutic option for the prevention of ovarian cancer recurrence. [Read the Full Post]

Protein Kinase D1, Reduced in Human Pancreatic Tumors, Increases Secretion of Small Extracellular Vesicles From Cancer Cells That Promote Metastasis to Lung in Mice

709 | Dec 14 2020

Milena Armacki et al. found that human pancreatic ductal adenocarcinoma had reduced levels of PRKD1 compared with nontumor pancreatic tissues. [Read the Full Post]

Poziotinib Inhibits the Efflux Activity of the ABCB1 and ABCG2 Transporters and the Expression of the ABCG2 Transporter Protein in Multidrug Resistant Colon Cancer Cells

657 | Dec 14 2020

Yongchao Zhang et al. showed that poziotinib interacted with the ABCB1 and ABCG2 transporter, suggesting that poziotinib might increase the efficacy of certain chemotherapeutic drugs used in treating MDR CRC. [Read the Full Post]

Design, synthesis and evaluation of novel indirubin-based N-hydroxybenzamides, N-hydroxypropenamides and N-hydroxyheptanamides as histone deacetylase inhibitors and antitumor agents

776 | Dec 12 2020

Duong Tien Anh et.al found that the potential of the indirubin-hydroxamic acid hybrids and these compounds should be very promising for further development. [Read the Full Post]

Histone Deacetylase Inhibition Attenuates Aortic Remodeling in Rats under Pressure Overload

998 | Dec 12 2020

Hanna Jung et al. indicated that MGCD, an HDAC inhibitor, attenuated aortic remodeling in rats with TAC-induced pressure overload rats and might serve as a potential therapeutic target of antiaortic remodeling in pressure overload-induced hypertension-related diseases. [Read the Full Post]

Physical Nature of Substituent Effects in XH/π Interactions

705 | Dec 09 2020

Jacob W G Bloom et al. showed that the impact of substituents on XH/π interactions depended strongly on the identity of the XH group, and the strength of these effects increased with increasing polarization of the XH bond. [Read the Full Post]

Preclinical Test of Dacomitinib, an Irreversible EGFR Inhibitor, Confirms Its Effectiveness for Glioblastoma

1003 | Dec 08 2020

Cristina Zahonero et al. confirmd that dacomitinib clearly affected receptor signaling in vivo and that its strong antitumoral effect was independent of the presence of mutant receptor isoforms although it could be affected by the PTEN status (as it was less effective in a PTEN-deleted GBM line). [Read the Full Post]

Novel miRNAs as Potential Regulators of PD-1/PD-L1 Immune Checkpoint, and Prognostic Value of MIR9-1 and MIR124-2 Methylation in Ovarian Cancer

609 | Dec 05 2020

N E Kushlinskii et al. suggested the role of inhibitors of the sPD-L1 immune checkpoint for five miRNAs (miR-124, miR-34b, miR-34c, miR-9, miR-339) and the possibility of using hypermethylated MIR9-1. [Read the Full Post]

NPM1 mutant maintains ULK1 protein stability via TRAF6-dependent ubiquitination to promote autophagic cell survival in leukemia

483 | Dec 04 2020

Yuting Tang et al. suggested that NPM1 mutant interacted with ULK1, and thus, maintained its protein stability, which was required for NPM1 mutant-mediated autophagic cell survival. [Read the Full Post]

Integrated pharmaco-proteogenomics defines two subgroups in isocitrate dehydrogenase wild-type glioblastoma with prognostic and therapeutic opportunities

461 | Dec 02 2020

Sejin Oh et al. guided GBM prognosis and precision treatment strategies. [Read the Full Post]

FXIIIa substrate peptide decorated BLZ945 nanoparticles for specifically remodeling tumor immunity

626 | Nov 30 2020

Qi Wei et al. established a novel combination strategy for anti-tumor therapy. [Read the Full Post]

Design and Evaluation of Rhein-Based MRI Contrast Agents for Visualization of Tumor Necrosis Induced by Combretastatin A-4 Disodium Phosphate

561 | Nov 30 2020

Libang Zhang et al. found that GdP1 might serve as a potential candidate for early evaluation of tumor response to CA4P treatment. [Read the Full Post]

Bevacizumab plus fosbretabulin in recurrent ovarian cancer: Overall survival and exploratory analyses of a randomized phase II NRG oncology/gynecologic oncology group study

436 | Nov 29 2020

Krishnansu S Tewari et al. found that although no significant survival benefit was observed, the trend showing a reduced HR for progression or death with increasing tumor size when fosbretabulin was added to bevacizumab compared to bevacizumab alone warrants further study. [Read the Full Post]

Co-targeting PIM and PI3K/mTOR using multikinase inhibitor AUM302 and a combination of AZD-1208 and BEZ235 in prostate cancer

884 | Nov 22 2020

Sabina Luszczak et al. believed that a co-targeting approach was a viable therapeutic strategy that should be developed further in pre-clinical studies. [Read the Full Post]

An essential role for Argonaute 2 in EGFR-KRAS signaling in pancreatic cancer development

913 | Nov 22 2020

Sunita Shankar et al. supported a biphasic model of pancreatic cancer development: an AGO2-independent early phase of PanIN formation reliant on EGFR-RAS signaling, and an AGO2-dependent phase wherein the mutant KRAS-AGO2 interaction was critical for PDAC progression. [Read the Full Post]

Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity

287 | Nov 20 2020

Zhi-Fu Tao et al. found that A-1155463 represented an excellent tool molecule for studying BCL-XL biology as well as a productive lead structure for further optimization. [Read the Full Post]

Direct Activation of BAX by BTSA1 Overcomes Apoptosis Resistance in Acute Myeloid Leukemia

0 | Nov 19 2020

Denis E Reyna et al. provided proof-of-concept for direct BAX activation as a treatment strategy in AML. [Read the Full Post]

RIP3 dependent NLRP3 inflammasome activation is implicated in acute lung injury in mice

810 | Nov 18 2020

Jingxian Chen et al. showed that RIP3 participated in the NLRP3 inflammasome activation in infiltrating macrophages in ALI induced by LPS. [Read the Full Post]

Rapalogues as hCES2A Inhibitors: In Vitro and In Silico Investigations

530 | Nov 17 2020

Cheng-Cheng Shi et al. demonstrated that several marketed rapalogues were potent and specific hCES2A inhibitors, and these agents could serve as leading compounds for the development of more efficacious hCES2A inhibitors to modulate the pharmacokinetic profiles and toxicity of hCES2A-substrate drugs (such as the anticancer agent irinotecan). [Read the Full Post]

Suppressor of Ty 16 promotes lung cancer malignancy and is negatively regulated by miR-1227-5p

619 | Nov 15 2020

Lu Yang et al. indicated that Spt16 was likely to be an essential regulator for lung cancer malignancy and was negatively regulated by miR-1227-5p. [Read the Full Post]

Target inhibition of caspase-8 alleviates brain damage after subarachnoid hemorrhage

418 | Nov 04 2020

Da-Qiang Ke et al. suggested that caspase-8 inhibition alleviated subarachnoid hemorrhage-induced brain injuries by suppressing inflammation. [Read the Full Post]

VDAC upregulation and αTAT1‑mediated α‑tubulin acetylation contribute to tanespimycin‑induced apoptosis in Calu‑1 cells

2173 | Nov 02 2020

Qilin Wang et al. provided evidence for the use of a combination of drugs that target VDAC1 and tubulin to induce tumour cell apoptosis. [Read the Full Post]

Identification of Subtype-Specific Metastasis-Related Genetic Signatures in Sarcoma

985 | Nov 02 2020

Ya-Ling Li et al. provided new insights into the pathogenesis, diagnosis, treatment, and prognosis of sarcomas and provided new directions for further study of sarcoma. [Read the Full Post]

To inhibit TrxR1 is to inactivate STAT3-Inhibition of TrxR1 enzymatic function by STAT3 small molecule inhibitors

574 | Oct 29 2020

Sander Busker et al. suggested that targeting of TrxR1 might be a common feature for many small molecules that inhibited cellular STAT3 function. [Read the Full Post]

Histone deacetylase 6 inhibition mitigates renal fibrosis by suppressing TGFß and EGFR signaling pathways in obstructive nephropathy

620 | Oct 28 2020

Xingying Chen et al. indicated that HDAC6 inhibition could attenuate development of renal fibrosis by suppression of TGFb1 and EGFR signaling, and suggested that HDAC6 would be a potential therapeutic target for the treatment of renal fibrosis. [Read the Full Post]

Cadmium induces apoptosis via generating reactive oxygen species to activate mitochondrial p53 pathway in primary rat osteoblasts

653 | Oct 27 2020

Jiaming Zheng et al. indicated that Cd could induce apoptosis in osteoblasts by increasing the generation of ROS and activating the mitochondrial p53 signaling pathway, and this mechanism required the transcriptional activation of p53. [Read the Full Post]

Antianemia Drug Roxadustat (FG-4592) Protects Against Doxorubicin-Induced Cardiotoxicity by Targeting Antiapoptotic and Antioxidative Pathways

621 | Oct 26 2020

Guangfeng Long et al.found that the protective effect of FG-4592 on DOX-induced cardiotoxicity possibly through upregulating HIF-1α and its target genes antagonizing apoptosis and oxidative stress. [Read the Full Post]

The therapeutic effect of the BRD4-degrading PROTAC A1874 in human colon cancer cells

798 | Oct 26 2020

An-Cheng Qin et al.thought that A1874-induced anti-colon cancer cell activity was more potent than the known BRD4 inhibitors (JQ1, CPI203, and I-BET151). [Read the Full Post]

mTOR Inhibition Ablates Cisplatin-Resistant Salivary Gland Cancer Stem Cells

486 | Oct 25 2020

T Nakano et al.suggested that a combination of an mTOR inhibitor and platinum-based chemotherapy might be beneficial to patients with salivary gland mucoepidermoid carcinoma. [Read the Full Post]

Piceatannol reduces resistance to statins in hypercholesterolemia by reducing PCSK9 expression through p300 acetyltransferase inhibition

570 | Oct 25 2020

Hyo-Jin Kim et al. indicated that PT was a new nutraceutical candidate to reduce the statin resistance and tolerance that occured in patients with hypercholesterolemia. [Read the Full Post]

Liproxstatin-1 is an effective inhibitor of oligodendrocyte ferroptosis induced by inhibition of glutathione peroxidase 4

343 | Oct 19 2020

Bao-You Fan et al.suggested that GPX4 inhibition induceed ferroptosis in oligodendrocytes, and that liproxstatin-1 was a potent inhibitor of ferroptosis. [Read the Full Post]

Hsp90 Inhibitor; NVP-AUY922 in Combination with Doxorubicin Induces Apoptosis and Downregulates VEGF in MCF-7 Breast Cancer Cell Line

996 | Oct 16 2020

Mahshid Mohammadian et al. indicated an effective action of NVP-AUY922 in combined with DOX in this cell line. [Read the Full Post]

Radiosensitization by Kinase Inhibition Revealed by Phosphoproteomic Analysis of Pancreatic Cancer Cells

546 | Oct 16 2020

Svenja Wiechmann et al.improved the understanding of radioresistance and provided avenues for developing radiotherapeutic strategies. [Read the Full Post]

Heat Shock Protein 90 (Hsp90)-Inhibitor-Luminespib-Loaded-Protein-Based Nanoformulation for Cancer Therapy

1027 | Oct 15 2020

Ankit K Rochani et al.suggested that DNP-based aqueous nanoformulations could be used in both pancreatic (MIA PaCa-2) and breast (MCF-7) cancer therapy. [Read the Full Post]

A study of human leukocyte antigen-haploidentical hematopoietic stem cells transplantation combined with allogenic mesenchymal stem cell infusion for treatment of severe aplastic anemia in pediatric and adolescent patients

864 | Sep 29 2020

Li Ding et al. suggested that cotransplantation of HLA-haploidentical HSC and allogenic mesenchymal stem cell might provide an effective and safe treatment for children and adolescents with SAA who lacked matched donors. [Read the Full Post]

Xanthatin alleviates airway inflammation in asthmatic mice by regulating the STAT3/NF-κB signaling pathway

632 | Sep 28 2020

Jingxia Chang et al. concluded that Xanthatin attenuated airway inflammation in asthmatic mice through blocking the STAT3/NFκB signaling pathway, indicating the potential of Xanthatin as a useful therapeutic agent for asthma. [Read the Full Post]

Transient Receptor Potential Ankyrin 1 (TRPA1) is Up-Regulated in Response to Lipopolysaccharide via P38/ Mitogen-Activated Protein Kinase (MAPK) in Dental Pulp Cells and Promotes Mineralization

441 | Sep 22 2020

Kento Tazawa et al. demonstrated that LPS stimulation induced TRPA1 via the NO-p38 MAPK signaling pathway and TRPA1 agonists promoted differentiation or mineralization of dental pulp cells. [Read the Full Post]

Mcl-1 targeting strategies unlock the proapoptotic potential of TRAIL in melanoma cells

256 | Sep 19 2020

Zina Sarif et al. indicated a high relevance of Mcl-1 targeting also in melanoma therapy. [Read the Full Post]

Flavonoids Restore Platinum Drug Sensitivity to Ovarian Carcinoma Cells in a Phospho-ERK1/2-Dependent Fashion

527 | Sep 15 2020

Yifat Koren Carmi et al. showed the potential of combining flavonoids with standard therapy to restore drug sensitivity to OC cells and overcomed TME-mediated platinum drug resistance. [Read the Full Post]

FLT3 inhibition upregulates HDAC8 via FOXO to inactivate p53 and promote maintenance of FLT3-ITD+ acute myeloid leukemia

670 | Sep 14 2020

Jun Long et al. demonstrated that HDAC8 upregulation was an important mechanism to resist TKIs and promote leukemia maintenance and suggested that combining HDAC8 inhibition with TKI treatment could be a promising strategy to treat FLT3-ITD+ AML and other tyrosine kinase mutation-harboring leukemias. [Read the Full Post]

Quizartinib for the treatment of acute myeloid leukemia

664 | Sep 13 2020

Alejandro Garcia-Horton et al. reviewed the mechanism of action, pharmacology, clinical efficacy, and safety of quizartinib, a FLT3 inhibitor, for the treatment of acute myeloid leukemia. [Read the Full Post]

Anti-inflammatory Effect of AZD6244 on Acrolein-Induced Neuroinflammation

551 | Sep 10 2020

Wen-Chien Ho et al. suggested that ERK inhibition may be a neuroprotective target against acrolein-induced neuroinflammation in the CNS neurodegenerative diseases. [Read the Full Post]

Effective Reconstruction of Functional Urethra Promoted With ICG-001 Delivery Using Core-Shell Collagen/Poly(Llactide-co-caprolactone) [P(LLA-CL)] Nanoyarn-Based Scaffold: A Study in Dog Model

517 | Sep 08 2020

Kaile Zhang et al. applied a novel drug-delivering nanoyarn scaffold in urethroplasty in dog model, which continuously delivered ICG-001 during tissue reconstruction, and could effectively promote urethral recovery and resume fully functional urethra within 12 weeks. [Read the Full Post]

Mast cells (MCs) induce ductular reaction mimicking liver injury in mice via MC-derived TGF-β1 signaling

699 | Sep 02 2020

Konstantina Kyritsi et al. demonstrated that reintroduction of MCs mimics cholestatic liver injury and MC-derived TGF-β1 might be a target in chronic cholestatic liver disease. [Read the Full Post]

Protein Kinase CK2 in Cancer Energetics

1138 | Aug 27 2020

Eduardo Silva-Pavez et al. proposed that the specific inhibition of CK2 might lead to a catastrophic death of cancer cells, which could become a feasible therapeutic strategy to beat this devastating disease. [Read the Full Post]

Casein kinase 2 inhibitor CX-4945 elicits an anti-Warburg effects through the downregulation of TAp73 and inhibits gastric tumorigenesis

1022 | Aug 27 2020

Shengli Tang et al. suggested that CX-4945 elicited an anti-Warburg effects in gastric cancer overexpressing Tap73 and inhibited gastric tumorigenesis. [Read the Full Post]

Cannabinoid 1 Receptor Antagonists Play a Neuroprotective Role in Chronic Alcoholic Hippocampal Injury Related to Pyroptosis Pathway

456 | Aug 26 2020

Dingang Zhang et al. indicated that cannabinoid receptors were regulated during this process, which suggested promising therapeutic strategies against alcohol-induced neurotoxicity through pharmacologic inhibition of CB1R. [Read the Full Post]

Pyroptosis is involved in the inhibitory effect of FL118 on growth and metastasis in colorectal cancer

437 | Aug 26 2020

Zhenxue Tang et al. found that FL118 restrained the growth and metastasis of colorectal cancer by inducing NLRP3-ASC-Caspase-1 mediated pyroptosis, which provided important evidence in the study on the role of pyroptosis and different tumors. [Read the Full Post]

The mTORC1 inhibitor rapamycin and the mTORC1/2 inhibitor AZD2014 impair the consolidation and persistence of contextual fear memory

507 | Aug 23 2020

Phillip E MacCallum et al. indicated the need to further understand the role of mTORC1/2 kinase activity in the molecular mechanisms underlying memory processing and also demonstrated that the effects of mTORC1 inhibition at different timepoints well after learning on memory consolidation and persistence. [Read the Full Post]

Resurrecting a p53 peptide activator - An enabling nanoengineering strategy for peptide therapeutics

666 | Aug 20 2020

Wangxiao He et al. proposed that this clinically viable drug delivery strategy could be applied not only to peptide activators of p53 for cancer therapy, but also to peptide therapeutics in general aimed at targeting intracellular protein-protein interactions for disease intervention. [Read the Full Post]

F-box protein FBXO31 modulates apoptosis and epithelial-mesenchymal transition of cervical cancer via inactivation of the PI3K/AKT-mediated MDM2/p53 axis

608 | Aug 19 2020

Keying Liu et al. revealed that FBXO31 down-regulated CC progression by blocking the PI3K/AKT-mediated MDM2/p53 axis, suggesting that FBXO31 might serve as a promising therapeutic target for CC treatment. [Read the Full Post]

GSK3β-Ikaros-ANXA4 signaling inhibits high-glucose-induced fibroblast migration

1514 | Aug 19 2020

Youpei Wang et al. provided a new regulatory mechanism by which GSK3β negatively regulated human skin fibroblast cell migration. [Read the Full Post]

A phase 2 trial of buparlisib in patients with platinum-resistant metastatic urothelial carcinoma

466 | Aug 17 2020

Victor McPherson et al. proposed that given the modest clinical activity and substantial toxicity of buparlisib, future trials of PI3K inhibitors in patients with UC should focus on isoform-selective PI3K inhibitors in genomically selected patients. [Read the Full Post]

The role of CUDC-907, a dual phosphoinositide-3 kinase and histone deacetylase inhibitor, in inhibiting proliferation of adult T-cell leukemia

366 | Aug 17 2020

Chie Ishikawa et al. showed that CUDC-907 might be a potential therapeutic agent for ATL. [Read the Full Post]

Identification of MYC as an antinecroptotic protein that stifles RIPK1-RIPK3 complex formation

629 | Aug 16 2020

Daehyeon Seong et al. found that MYC-mediated suppression of necroptosis was a mechanism of necroptosis resistance in cancer, and approaches targeting MYC to induce necroptosis represent an attractive therapeutic strategy for cancer. [Read the Full Post]

Macrophages confer resistance to PI3K inhibitor GDC-0941 in breast cancer through the activation of NF-κB signaling

557 | Aug 13 2020

Muhammad Waqas Usman et al. suggested macrophages in microenvironment may contribute to the resistance of breast cancer cells to PI3K inhibition and reveal a new combination paradigm to improve the efficacy of PI3K-targeted therapy. [Read the Full Post]

A PI3K- and GTPase-independent Rac1-mTOR mechanism mediates MET-driven anchorage-independent cell growth but not migration

571 | Aug 12 2020

Alexia Hervieu et al. revealed a GTPase-independent role for Rac1 in mediating a PI3K-independent MET-to-mTOR pathway and suggested alternative or combined strategies that might overcome resistance to RTK inhibitors in patients with cancer. [Read the Full Post]

Targeting p53 for the treatment of cancer

512 | Aug 11 2020

Michael J Duffy et al. indicated that it was likely to usher in a new era in cancer treatment, especially as p53 dysfunction is so prevalent in human cancers if any of the compounds currently being evaluated in clinical trials be shown to have efficacy [Read the Full Post]

Giardia duodenalis induces extrinsic pathway of apoptosis in intestinal epithelial cells through activation of TNFR1 and K63 de-ubiquitination of RIP1 in vitro

666 | Aug 11 2020

Lin Liu et al. suggested that Giardia trophozoite stimulation could activate CASP3/8 signaling pathways via activation of TNFR1 and K63 de-ubiquitination of RIP1 caused by up-regulated expressions of CYLD and A20, and promoted Caco-2 cell apoptosis. [Read the Full Post]

Antiviral activity of PLK1-targeting siRNA delivered by lipid nanoparticles in HBV-infected hepatocytes

846 | Aug 10 2020

Adrien Foca et al. emphasized that a specific PLK1 inhibition could help in achieving an improved HBsAg loss in CHB patients, likely in combination with other HBsAg-targeting strategies. [Read the Full Post]

Targeting BCL-2 proteins in pediatric cancer: Dual inhibition of BCL-X L and MCL-1 leads to rapid induction of intrinsic apoptosis

255 | Aug 09 2020

Sarah Kehr et al. demonstrated the potency of A-1331852/S63845 in pediatric solid tumor cells and to describe the molecular mechanisms of A-1331852/S63845 co-treatment underlining the potential of BCL-XL and MCL-1 inhibition as treatment regime. [Read the Full Post]

Selumetinib for plexiform neurofibromas in neurofibromatosis type 1: a single-institution experience

547 | Aug 09 2020

Vera Espírito Santo et al. showed that the drug was associated with clinical and radiological improvement. [Read the Full Post]

Severe COVID-19 in a renal transplant recipient: A focus on pharmacokinetics

839 | Aug 08 2020

Soufian Meziyerh et al. aimed to achieve increased awareness and improved management of drug-drug interactions associated with the various treatment options for COVID-19 in renal transplant patients. [Read the Full Post]

Regorafenib for Metastatic Colorectal Cancer: An Analysis of a Registry-Based Cohort of 555 Patients

1021 | Aug 06 2020

Alena Novakova-Jiresova ETAL. found that regorafenib was a safe and active treatment option for a subgroup of patients with mCRC who were progressing after other systemic therapies and maintain good performance status. [Read the Full Post]

Gemcitabine combined with cisplatin vs. taxane, cisplatin, and fluorouracil in the treatment of locally advanced nasopharyngeal carcinoma: a retrospective case-control study

830 | Aug 04 2020

Y-M Huang et al. showed that the clinical efficacy of the GP regimen combined with CCRT for the treatment of locoregionally advanced NPC might be better than that of the TPF regimen. [Read the Full Post]

Alcohol-induced CYP2E1, Mitochondrial Dynamics and Retrograde Signaling in Human Hepatic 3D Organoids

1131 | Aug 03 2020

Rajesh Angireddy et al. presented a mechanistic link between CYP2E1 function and alcohol mediated mitochondrial dysfunction, retrograde signaling, and activation of hepatic steatosis in a 3D organoid system that closely recapitulated the in vivo liver response. [Read the Full Post]

In Vitro and In Vivo Efficacy of DNA Damage Repair Inhibitor Veliparib in Combination with Artesunate against Echinococcus granulosus

610 | Aug 02 2020

Y F Li et al. demonstrated that AS or AS in combination with Veliparib was effective for treating CE, especially the combination group. [Read the Full Post]

Evaluation of the Efficacy and Safety of PARP Inhibitors in Advanced-Stage Epithelial Ovarian Cancer

736 | Aug 02 2020

Yifan Jiang et al. found that PARP inhibitors were an effective and well-tolerated treatment for patients with advanced-stage epithelial ovarian cancer. [Read the Full Post]

Induction of ferroptosis in response to graphene quantum dots through mitochondrial oxidative stress in microglia

356 | Jul 26 2020

Tianshu Wu et al. not only provided new insights in the GQDs-induced cell damage performed in multiple types of cell death, but also in the influence of chemical modification on the toxicity of GQDs. [Read the Full Post]

Cigarette smoking is associated with high level of ferroptosis in seminal plasma and affects semen quality

319 | Jul 26 2020

Zhanhui Ou et al. found that cigarette smoking was associated with high level of ferroptosis in seminal plasma and affect semen quality. [Read the Full Post]

Polo-like kinase 1 as a promising diagnostic biomarker and potential therapeutic target for hepatocellular carcinoma

494 | Jul 22 2020

Eman H Yousef et al. found that Polo-like kinase 1 might be a potential biomarker for hepatocellular carcinoma diagnosis and follow-up during treatment with chemotherapies. [Read the Full Post]

Neratinib Plus Capecitabine Versus Lapatinib Plus Capecitabine in HER2-Positive Metastatic Breast Cancer Previously Treated With ≥ 2 HER2-Directed Regimens: Phase III NALA Trial

1101 | Jul 22 2020

Cristina Saura et al.showed that N+C significantly improved PFS and time to intervention for CNS disease versus L+C. No new N+C safety signals were observed. [Read the Full Post]

DrugSniper, a Tool to Exploit Loss-Of-Function Screens, Identifies CREBBP as a Predictive Biomarker of VOLASERTIB in Small Cell Lung Carcinoma (SCLC)

399 | Jul 21 2020

Fernando Carazo et al. showed the potential of genome-wide loss-of-function screens to identify new personalized therapeutic hypotheses in SCLC and potentially in other tumors, which was a valuable starting point for further drug development and drug repositioning projects. [Read the Full Post]

Alisertib plus induction chemotherapy in previously untreated patients with high-risk, acute myeloid leukaemia: a single-arm, phase 2 trial

871 | Jul 17 2020

Andrew M Brunner et al. suggested that alisertib combined with induction chemotherapy is active and safe in previously untreated patients with high-risk acute myeloid leukaemia. [Read the Full Post]

Phase 1 trial of carfilzomib (PR-171) in combination with vorinostat (SAHA) in patients with relapsed or refractory B-cell lymphomas

975 | Jul 16 2020

Beata Holkova et al. showed a decrease in NF-κB activation and an increase in Bim levels in some patients, but these changes did not correlate with clinical response. [Read the Full Post]

Advanced bioinformatics rapidly identifies existing therapeutics for patients with coronavirus disease-2019 (COVID-19)

633 | Jul 15 2020

Jason Kim et al. highlighted the potential use of two bioinformatics technologies to rapidly discover existing therapeutic agents that warranted further investigation for established and emerging disease processes. [Read the Full Post]

The BCL-2 family protein inhibitor ABT-737 as an additional tool for the treatment of EBV-associated post-transplant lymphoproliferative disorders

418 | Jul 14 2020

Aude Robert et al. suggested that the use of agents targeting BCL-2, either alone or in combination with other conventional drugs, represented a novel promising approach for post-transplant EBV-positive B lymphoproliferative disorders. [Read the Full Post]

Protein Acetylation Derepresses Serotonin Synthesis to Potentiate Pancreatic Beta-Cell Function Through HDAC1-PKA-Tph1 Signaling

963 | Jul 13 2020

Yuqing Zhang et al. highlighted a novel role of HDAC1-PKA-Tph1 signaling in governing β-cell functional compensation by derepressing serotonin synthesis. [Read the Full Post]

Lenvatinib and Sorafenib for Differentiated Thyroid Cancer After Radioactive Iodine: A Systematic Review and Economic Evaluation

740 | Jul 13 2020

Nigel Fleeman et al.showed that compared with placebo/BSC, treatment with lenvatinib or sorafenib results in an improvement in PFS, objective tumour response rate and possibly OS, but dose modifications were required to treat AEs. [Read the Full Post]

In Vitro Assessment of the Genotoxic Hazard of Novel Hydroxamic Acid- And Benzamide-Type Histone Deacetylase Inhibitors (HDACi)

1029 | Jul 12 2020

Annabelle Friedrich et al. found that KSK64 revealed the highest genotoxic hazard and DDR stimulating potential, while TOK77 and MPK77 showed the lowest DNA damaging capacity. [Read the Full Post]

Histone Deacetylase Inhibition Prevents the Growth of Primary and Metastatic Osteosarcoma

1379 | Jul 07 2020

Jeremy J McGuire et al. provided rationale for clinical trials in osteosarcoma patients using the approved therapies panobinostat or romidepsin. [Read the Full Post]

Discovery of Novel Dual c-Met/HDAC Inhibitors as a Promising Strategy for Cancer Therapy

799 | Jul 07 2020

Hao Hu et al. provided an efficient strategy for discovery of multitarget antitumor drugs. [Read the Full Post]

Combination BET Family Protein and HDAC Inhibition Synergistically Elicits Chondrosarcoma Cell Apoptosis Through RAD51-Related DNA Damage Repair

983 | Jul 06 2020

Songwei Huan et al. disclosed that BET and HDAC inhibition synergistically inhibited cell growth and induced cell apoptosis through a mechanism that involved the suppression of RAD51-related HR DNA repair in chondrosarcoma cells. [Read the Full Post]

Efficacy of Gefitinib Combined With 125 I Radioactive Particles in the Treatment of Transplanted Lung Cancer Tumors in Nude Mice

866 | Jul 02 2020

Chaojie Li et al. found that Gefitinib combined with 125I radioactive particles brachytherapy could significantly inhibit tumor growth. [Read the Full Post]

MEK Inhibitors Combined With Programmed Cell death-1 Blockade Immunotherapy for Metastatic Uveal Melanoma: Is It Warranted?

572 | Jun 30 2020

Anais Zanella et al. highlighted the need to evaluate the safety and efficacy of new treatment options such as MEKi and anti-PD-1 for mUM. [Read the Full Post]

A New Compound With Increased Antitumor Activity by Cotargeting MEK and Pim-1

688 | Jun 30 2020

Yanan Li et al. uncovered a new MEK inhibitor KZ-02 with significantly enhanced antitumor activity by co-targeting MEK and Pim-1. [Read the Full Post]

Targeting BCL-2 Proteins in Pediatric Cancer: Dual Inhibition of BCL-X L and MCL-1 Leads to Rapid Induction of Intrinsic Apoptosis

349 | Jun 29 2020

Sarah Kehr et al. demonstrated the potency of A-1331852/S63845 in pediatric solid tumor cells and to describe the molecular mechanisms of A-1331852/S63845 co-treatment underlining the potential of BCL-XL and MCL-1 inhibition as treatment regime. [Read the Full Post]

Volumetric Absorptive Microsampling (VAMS) for Assaying Immunosuppressants From Venous Whole Blood by LC-MS/MS Using a Novel Atmospheric Pressure Ionization Probe (UniSpray™)

1881 | Jun 28 2020

Lucía Paniagua-González et al. showed that venous blood VAMS concentrations were correlated to those found in the original liquid venous blood, proving that the VAMS material itself will not bias blood drug concentrations. [Read the Full Post]

Notch Signaling Pathway Is a Potential Therapeutic Target for Extracranial Vascular Malformations

0 | Jun 22 2020

Reema B Davis et al. provided further rationale to support testing of Notch inhibitors in patients with extracranial vascular malformations. [Read the Full Post]

Effects of the PI3K/Akt Signaling Pathway on the Apoptosis of Early Host Cells Infected With Eimeria Tenella

1545 | Jun 21 2020

Xuesong Zhang et al. investigated the role of PI3K/Akt signaling pathway on host cell apoptosis in the early infection of Eimeria tenella,the early development of E. tenella could inhibit host cell apoptosis by downregulating the Caspase-3 activity. [Read the Full Post]

A Systematic Review of the Studies That Evaluate the Performance of the DAPT Score

1090 | Jun 21 2020

Chun Shing Kwok et al. showd that the DAPT score had modest predictive value for ischemic and bleeding outcomes.A prospective randomized controlled trial was needed to evaluate the clinical benefits of utilising the DAPT score in guiding continued DAPT therapy beyond 1 year. [Read the Full Post]

Inhibition of Aurora Kinase A by Alisertib Reduces Cell Proliferation and Induces Apoptosis and Autophagy in HuH-6 Human Hepatoblastoma Cells

664 | Jun 19 2020

Jingyi Tan et al. suggested that AURKA may be a novel therapeutic target and ALS a potential therapeutic drug for the treatment of HB. [Read the Full Post]

DAPT Score and the Impact of Ticagrelor Monotherapy During the Second Year After PCI

1192 | Jun 18 2020

Ply Chichareon et al. found that the DAPT score can stratify ischemic but not bleeding risk in a contemporary PCI population during the second year. [Read the Full Post]

Prediction of Therapeutic Outcome and Survival in a Transgenic Mouse Model of Pancreatic Ductal Adenocarcinoma Treated With Dendritic Cell Vaccination or CDK Inhibitor Using MRI Texture: A Feasibility Study

578 | Jun 17 2020

Aydin Eresen et al. demonstrated that MRI texture features had great potential to generate diagnosis and prognosis models for monitoring early treatment response following dinaciclib drug or DC vaccine treatment and also predicting histopathological tumor markers and long-term clinical outcomes. [Read the Full Post]

Revealing the Selective Mechanisms of Inhibitors to PARP-1 and PARP-2 via Multiple Computational Methods

638 | Jun 17 2020

Hongye Hu et al. provided new insights about how inhibitors specifically bound to PARP-1 over PARP-2, which might help facilitate the design of highly selective PARP-1 inhibitors in the future. [Read the Full Post]

Cooperativity Between Orthosteric Inhibitors and Allosteric Inhibitor 8-Anilino-1-Naphthalene Sulfonic Acid (ANS) in Cyclin-Dependent Kinase 2

715 | Jun 16 2020

Erik B Faber et al. detailed the positive cooperativity between ANS and orthosteric Cdk2 inhibitors dinaciclib and roscovitine, which increased the affinity of ANS toward Cdk2 5-fold to 10-fold, and the relatively noncooperative effects of ATP. [Read the Full Post]

Network Indirect Comparison of 3 BRAF + MEK Inhibitors for the Treatment of Advanced BRAF Mutated Melanoma

747 | Jun 12 2020

F Consoli et al. suggested a similar efficacy and a slightly different safety profile, related to specific molecular properties of the three different BRAF and MEK inhibitors currently approved in the management of advanced MM. [Read the Full Post]

The Application of Ferroptosis in Diseases

468 | Jun 09 2020

Yangmin Qiu et al. summarized the mechanism of ferroptosis regulation and relevance to pathological physiology. [Read the Full Post]

TGF-β1-mediated Repression of SLC7A11 Drives Vulnerability to GPX4 Inhibition in Hepatocellular Carcinoma Cells

588 | Jun 09 2020

Do Hyung Kim et al. showed that TGF-β1 repressed xCT expression via Smad3 activation and enhanced lipid peroxidation in hepatocellular carcinoma cells with an early TGF-β1 signature, which would benefit from the targeting of GPX4. [Read the Full Post]

Exploring the Relevance of Senotherapeutics for the Current SARS-CoV-2 Emergency and Similar Future Global Health Threats

1068 | Jun 05 2020

Marco Malavolta et al. explored the idea that an exacerbated inflammatory response, in particular that mediated by IL-6, migtht drive the deleterious consequences of the infection. [Read the Full Post]

HMGB1-induced Aberrant Autophagy Contributes to Insulin Resistance in Granulosa Cells in PCOS

682 | Jun 04 2020

Chuyue Zhang et al. indicated that increased HMGB1 contributes to IR development in granulosa cells of PCOS patients, which was associated with exacerbation of autophagy by HMGB1. Control of HMGB1 production might be benefical for the improvement of insulin sensitivity in granulosa cells in PCOS. [Read the Full Post]

Berberine Represses Human Gastric Cancer Cell Growth in Vitro and in Vivo by Inducing Cytostatic Autophagy via Inhibition of MAPK/mTOR/p70S6K and Akt Signaling Pathways

650 | Jun 04 2020

Qiang Zhang et al. indicated that berberine repressed human gastric cancer cell growth in vitro and in vivo by inducing cytostatic autophagy via inhibition of MAPK/mTOR/p70S6K and Akt, and provided a molecular basis for the treatment of gastric cancer. [Read the Full Post]

Cell Cycle Arrest and Apoptosis Are Not Dependent on p53 Prior to p53-dependent Embryonic Stem Cell Differentiation

1647 | Jun 02 2020

Sushil K Jaiswal et al. found that the multiple roles of p53 in cell cycle regulation and apoptosis were first acquired during pluripotent stem cell differentiation. [Read the Full Post]

Phase II Trial of AKT Inhibitor MK-2206 in Patients With Advanced Breast Cancer Who Have Tumors With PIK3CA or AKT Mutations, and/or PTEN loss/PTEN Mutation

822 | May 31 2020

Yan Xing et al. found that MK-2206 monotherapy had limited clinical activity in advanced breast cancer patients selected for PIK3CA/AKT1 or PTEN mutations or PTEN loss. This may, in part, be due to inadequate target inhibition at tolerable doses in heavily pre-treated patients with pathway activation, as well as tumor heterogeneity and evolution in markers such as PTEN conferring challenges in patient selection. [Read the Full Post]

Inhibition of Apoptosis by Caspase Inhibitor Z-VAD-FMK Improves Cryotolerance of in Vitro Derived Bovine Embryos

0 | May 26 2020

Maria Elena Pero et al. found that the addition of 20 μM Z-VAD-FMK during vitrification/warming and post-warming culture partially inhibited cryopreservation-induced apoptosis by reducing the level of active caspase 3, suggesting a potential used as an additive to ameliorate the efficiency of embryo cryopreservation in cattle, critical for a further diffusion of IVEP technology in the field. [Read the Full Post]

ABT-263 Exhibits Apoptosis-Inducing Potential in Oral Cancer Cells by Targeting C/EBP-homologous Protein

382 | May 20 2020

In-Hyoung Yang et al. provided evidence that ABT-263 may serve as an effective therapeutic agent for the treatment of human oral cancer. [Read the Full Post]

Preclinical antitumor efficacy of senescence-inducing chemotherapy combined with a nanoSenolytic.

0 | May 19 2020

Galiana I et al. supported targeted senolysis as a new therapeutic opportunity to improve outcomes in breast cancer patients [Read the Full Post]

Endoplasmic reticulum stress mediates resistance to BCL-2 inhibitor in uveal melanoma cells

358 | May 16 2020

Bellini L et al. identified ABT-263 as a valid therapeutic option for patients suffering from uveal melanoma. [Read the Full Post]

Discovery of IAP-recruiting BCL-XL PROTACs as potent degraders across multiple cancer cell lines

362 | May 16 2020

Zhang X et al. expanded the anti-tumor spectra of BCL-XL degraders and further highlight the importance of selecting suitable E3 members to achieve effective cellular activity. [Read the Full Post]

Toll-like Receptor 4 Deficiency Aggravates Airway Hyperresponsiveness and Inflammation by Impairing Neutrophil Apoptosis in a Toluene Diisocyanate-Induced Murine Asthma Model.

311 | May 15 2020

Chen S et al. indicated that TLR4 deficiency promoted neutrophil infiltration by impairing its apoptosis via up-regulation of Bcl-2, thereby resulting in deteriorated AHR and airway inflammation, which suggests that TLR4 could be a negative regulator of TDI-induced neutrophilic inflammation. [Read the Full Post]

"Direct to Drug" screening as a precision medicine tool in multiple myeloma.

385 | May 14 2020

Bonolo de Campos C et al. found that this "direct to drug" screening resource, paired with functional genomics, had the potential to successfully direct appropriate individualized therapeutic approaches in MM and to enrich clinical trials for likely responders. [Read the Full Post]

Dual targeting of BCL2 and MCL1 rescues myeloma cells resistant to BCL2 and MCL1 inhibitors associated with the formation of BAX/BAK hetero-complexes

290 | May 12 2020

Seiller C et al. found that BCLXL remains a major resistant factor of cell death induced by this combination. [Read the Full Post]

FBP1 loss disrupts liver metabolism and promotes tumorigenesis through a hepatic stellate cell senescence secretome

351 | May 09 2020

Li F et.al provided genetic evidence for FBP1 as a metabolic tumour suppressor in liver cancer and establish a critical crosstalk between hepatocyte metabolism and HSC senescence that promotes tumour growth. [Read the Full Post]

Preclinical antitumor efficacy of senescence-inducing chemotherapy combined with a nanoSenolytic

361 | May 08 2020

Galiana I et al. supported targeted senolysis as a new therapeutic opportunity to improve outcomes in breast cancer patients. [Read the Full Post]

Necrostatin-1 protects C2C12 myotubes from CoCl2-induced hypoxia

534 | May 03 2020

Chen R et al. suggested that Nec‑1 protected C2C12 myotubes under conditions of CoCl2-induced hypoxia. [Read the Full Post]

Caspase-3 Inhibitor Z-DEVD-FMK Enhances Retinal Ganglion Cell Survival and Vision Restoration After Rabbit Traumatic Optic Nerve Injury

712 | Apr 28 2020

Yuanyuan Liu et al. showed the caspase-3 inhibitor Z-DEVD-FMK is neuroprotective by inhibiting RGCs apoptosis when injected 30 min after optic nerve damage and significantly promotes restoration of vision. A controlled clinical trial is now needed to evaluate the efficacy and safety of Z-DEVD-FMK in humans. [Read the Full Post]

Multiple myeloma with 1q21 amplification is highly sensitive to MCL-1 targeting

0 | Mar 29 2020

Slomp A et al. indicated that amplification of 1q21 identifies an MM subset highly sensitive to MCL-1 inhibitor treatment and can be used as a predictive marker to guide selection of therapy. [Read the Full Post]

An in vitro assay for biomarker discovery and dose prediction applied to ibrutinib plus venetoclax treatment of CLL

333 | Feb 27 2020

Eide CA et al. suggested that IBR + VEN may represent an effective therapeutic option for patients with AML. [Read the Full Post]

Venetoclax, a BCL-2 Inhibitor, Enhances the Efficacy of Chemotherapeutic Agents in Wild-Type ABCG2-Overexpression-Mediated MDR Cancer Cells

356 | Feb 27 2020

Wang JQ et al. provided useful guidance in combination therapy against wild-type ABCG2-mediated MDR cancer in clinical practice. [Read the Full Post]

Multiple myeloma with 1q21 amplification is highly sensitive to MCL-1 targeting

460 | Feb 14 2020

Slomp A et al. indicated that amplification of 1q21 identifies an MM subset highly sensitive to MCL-1 inhibitor treatment and can be used as a predictive marker to guide selection of therapy. [Read the Full Post]

L-Cystathionine Protects against Homocysteine-Induced Mitochondria-Dependent Apoptosis of Vascular Endothelial Cells

353 | Feb 13 2020

Wang X et al. indicated that L-cystathionine could protect against homocysteine-induced mitochondria-dependent apoptosis of HUVECs. [Read the Full Post]

Venetoclax in acute myeloid leukemia - current and future directions

425 | Feb 11 2020

Lachowiez C et al. provided biological and clinical rationale for current venetoclax based treatments in AML, addresses common adverse events encountered with venetoclax based therapy, and explores emerging clinical data regarding combinations of novel targeted therapeutics used in conjunction with venetoclax for the treatment of AML. [Read the Full Post]

Anticancer drug candidate CBL0137, which inhibits histone chaperone FACT, is efficacious in preclinical orthotopic models of temozolomide-responsive and -resistant glioblastoma

448 | Feb 05 2020

Barone TA et al. indicated that CBL0137 targets GBM according to its proposed mechanism of action, crosses the blood-brain barrier, and is efficacious in both TMZ-responsive and -resistant orthotopic models, making it an attractive new therapy for GBM. [Read the Full Post]

Proteomic Analysis of an Induced Pluripotent Stem Cell Model Reveals Strategies to Treat Juvenile Myelomonocytic Leukemia

628 | Feb 05 2020

Pearson S et al. demonstrated these small molecular inhibitors, JQ1 and CBL0137, preferentially extinguish primitive hematopoietic cells from sporadic JMML patients as opposed to cells from healthy individuals. [Read the Full Post]

Isoflavones Isolated from the Seeds of Millettia ferruginea Induced Apoptotic Cell Death in Human Ovarian Cancer Cells

555 | Jan 18 2020

Wang YY et al. suggested that DMI induced apoptotic cell death through the intrinsic pathway via ROS production, while ferrugone stimulated the extrinsic pathway in human ovarian cancer cells. [Read the Full Post]

Suppression of human T cell proliferation by the caspase inhibitors, z-VAD-FMK and z-IETD-FMK is independent of their caspase inhibition properties

0 | Jan 12 2020

Lawrence CP and Chow SC demonstrated that both z-VAD-FMK and z-IETD-FMK are immunosuppressive in vitro and inhibit T cell proliferation without blocking the processing of caspase-8 and caspase-3. [Read the Full Post]

Napabucasin: An Update on the First-in-Class Cancer Stemness Inhibitor

0 | Jan 05 2020

Hubbard JM and Grothey A indicated that napabucasin may prove useful in targeting cancer stem cells, with the potential to suppress metastasis and prevent relapse in patients with varying cancer types. [Read the Full Post]

P53 inhibitor pifithrin-α prevents the renal tubular epithelial cells against injury

1249 | Jan 02 2020

Shen YL et al. indicated that pifithrin-α can facilitate the progression of renal tubular epithelial cells through G2/M phase, protecting them against injury. [Read the Full Post]

Sesamin suppresses NSCLC cell proliferation and induces apoptosis via Akt/p53 pathway

530 | Jan 02 2020

Chen Y et al. demonstrated that sesamin suppresses NSCLC cell proliferation by induction of G1 phase cell cycle arrest and apoptosis via Akt/p53 pathway. Therefore, sesamin may be a promising adjuvant treatment for NSCLC therapy. [Read the Full Post]

On the Mechanism of Cytoprotection by Ferrostatin-1 and Liproxstatin-1 and the Role of Lipid Peroxidation in Ferroptotic Cell Death

0 | Dec 23 2019

Zilka O et al. demonstrated that potent RTAs subvert ferroptosis and suggest that lipid peroxidation (autoxidation) may play a central role in the process. [Read the Full Post]

CDK5 Inhibitor Downregulates Mcl-1 and Sensitizes Pancreatic Cancer Cell Lines to Navitoclax

381 | Dec 13 2019

Kour S et al. reported the discovery of an aminopyrazole, 2-([1,1'-biphenyl]-4-yl)-N-(5-cyclobutyl-1H-pyrazol-3-yl)acetamide (analog 24), which selectively inhibited cyclin-dependent kinase (CDK) 5 over CDK2 in cancer cell lines. [Read the Full Post]

Fludarabine-PET in a murine model of multiple myeloma

1140 | Dec 08 2019

Hovhannisyan N et al. suggested that [18F]fludarabine-PET might represent an alternative and perhaps more specific modality for MM imaging when compared to [18F]FDG. Nevertheless, more investigations are required to extend this conclusion to humans. [Read the Full Post]

Pre-metastatic niche triggers SDF-1/CXCR4 axis and promotes organ colonisation by hepatocellular circulating tumour cells via downregulation of Prrx1

649 | Dec 04 2019

Tang Y et al. demonstrated that decreased expression of Prrx1 stimulates SDF-1/CXCR4 signalling and contributes to organ colonisation with blood CTCs in HCC. STAT3 inhibition and specific blockade of CXCR4 have clinical potential as therapeutics for eliminating organ metastasis in advanced HCC. [Read the Full Post]

MCL-1 antagonism enhances the anti-invasive effects of dasatinib in pancreatic adenocarcinoma

353 | Nov 25 2019

Castillo L et al. suggested that MCL-1 antagonism, while reducing cell viability, may have an additional benefit in increasing the antimetastatic efficacy of dasatinib for the treatment of PDAC. [Read the Full Post]

Isovitexin Suppresses Cancer Stemness Property And Induces Apoptosis Of Osteosarcoma Cells By Disruption Of The DNMT1/miR-34a/Bcl-2 Axis

329 | Nov 23 2019

Liang X et al. suggested that ISOV-mediated epigenetic regulation involved the DNMT1/miR-34a/Bcl-2 axis and caused the suppression of stemness and induction of apoptosis in the spheres derived from OS cells. The data indicated that ISOV exhibited a novel efficient potential for the treatment of OS. [Read the Full Post]

An integrative pharmacogenomics analysis identifies therapeutic targets in KRAS-mutant lung cancer

748 | Nov 07 2019

Wang H et al. developed a genotype-based strategy that identifies CK2 as a promising co-target in KRAS(G12C) mutant NSCLC by using available pharmacogenomics gene expression datasets. This approach is applicable to other oncogene driven cancers. [Read the Full Post]

The Caspase 1 Inhibitor VX-765 Protects the Isolated Rat Heart via the RISK Pathway

0 | Nov 06 2019

Do Carmo H et al. indicated the caspase 1 inhibitor, VX-765, was able to reduce myocardial infarction in a model of IR injury. However, the addition of IPC did not demonstrate any further protection. [Read the Full Post]

Nutlin-3 enhances the bortezomib sensitivity of p53-defective cancer cells by inducing paraptosis

823 | Nov 01 2019

Lee DM et al. suggested that bortezomib/nutlin-3 perturbs proteostasis, triggering ER/mitochondria stress and irrecoverable impairments in their structure and function, ultimately leading to paraptotic cell death. [Read the Full Post]

Nutlin-3a selects for cells harbouring TP53 mutations

0 | Oct 29 2019

Kucab JE et al. suggested that including a Nutlin-3a counter-screen significantly improves the specificity and efficiency of the HIMA, whereby TP53-mutated clones are selected prior to sequencing and TP53-WT clones can be discarded. [Read the Full Post]

The caspase-8 inhibitor emricasan combines with the SMAC mimetic birinapant to induce necroptosis and treat acute myeloid leukemia

0 | Oct 24 2019

Brumatti G et al. demonstrated antileukemic efficacy and safety of the birinapant/emricasan combination in vivo suggest that induction of necroptosis warrants clinical investigation as a therapeutic opportunity in AML. [Read the Full Post]

Prolonged Idasanutlin (RG7388) Treatment Leads to the Generation of p53-Mutated Cells

555 | Oct 20 2019

Skalniak L et al. showed that although idasanutlin presents much improved activities compared to its precursor, it displays the similar weaknesses, which are limited elimination of cancer cells and the generation of p53-mutated drug-resistant subpopulations. [Read the Full Post]

The anti-caspase inhibitor Q-VD-OPH prevents AIDS disease progression in SIV-infected rhesus macaques

665 | Oct 20 2019

Laforge M et al. demonstrated that Q-VD-OPH injection in SIV-infected RMs may represent an adjunctive therapeutic agent to control HIV infection and delaying disease progression to AIDS. [Read the Full Post]

Genome-wide CRISPR/Cas9 library screening identified PHGDH as a critical driver for Sorafenib resistance in HCC

1076 | Oct 18 2019

Wei L et al. demonstrated that targeting PHGDH is an effective approach to overcome TKI drug resistance in HCC. [Read the Full Post]

The pan-caspase inhibitor Emricasan (IDN-6556) decreases liver injury and fibrosis in a murine model of non-alcoholic steatohepatitis

782 | Oct 15 2019

Barreyro FJ et al. demonstrated that in a murine model of NASH, liver injury and fibrosis are suppressed by inhibiting hepatocytes apoptosis and suggests that Emricasan may be an attractive antifibrotic therapy in NASH. [Read the Full Post]

Recent developments in the treatment of blastic plasmacytoid dendritic cell neoplasm

392 | Oct 06 2019

Future directions in therapy approaches for patients with BPDCN will include the development of other CD123-targeted agents, agents targeting beyond CD123 and investigation of rational combination approaches of CD123-directed therapy with other therapies. [Read the Full Post]

LncRNA FER1L4 induces apoptosis and suppresses EMT and the activation of PI3K/AKT pathway in osteosarcoma cells via inhibiting miR-18a-5p to promote SOCS5

391 | Oct 03 2019

Ye F et al. indicated thatthe overexpression of FER1L4 promoted apoptosis and inhibited the EMT markers expression and PI3K/AKT signaling pathway activation in OS cells via downregulating miR-18a-5p to promote SOCS5. [Read the Full Post]

On the Mechanism of Cytoprotection by Ferrostatin-1 and Liproxstatin-1 and the Role of Lipid Peroxidation in Ferroptotic Cell Death

0 | Oct 02 2019

Zilka O et al. demonstrated that potent RTAs subvert ferroptosis and suggest that lipid peroxidation (autoxidation) may play a central role in the process. [Read the Full Post]

ABT-737 potentiates cisplatin-induced apoptosis in human osteosarcoma cells via the mitochondrial apoptotic pathway

550 | Sep 22 2019

Zhang F et al. demonstrated that ABT-737 alone has a nominal influence on human U-2OS cells when treated within the clinically administered range, but when combined with DDP, it can inhibit the proliferation of human U-2OS cells by inducing apoptosis via the mitochondrial apoptotic pathway. [Read the Full Post]

Fenretinide via NOXA induction, enhanced activity of the BCL-2 inhibitor venetoclax in high BCL-2-expressing neuroblastoma preclinical models

410 | Sep 06 2019

Reynolds CP et al. found that fenretinide + ventoclax is a synergistic combination that warrants clinical testing in high BCL-2 expressing neuroblastoma. [Read the Full Post]

An in vitro assay for biomarker discovery and dose prediction applied to ibrutinib plus venetoclax treatment of CLL

219 | Sep 06 2019

Skånland SS et al. suggested that phospho flow should be considered as a novel approach for dose and synergy prediction in a precision medicine setting for CLL. [Read the Full Post]

XPO1 inhibitor KPT-330 synergizes with Bcl-xL inhibitor to induce cancer cell apoptosis by perturbing rRNA processing and Mcl-1 protein synthesis

421 | Aug 28 2019

Zhu ZC et al. clarify the reason of apoptosis resistance of cancer cells to XPO1 inhibition and develop a potential strategy for treating solid tumors. [Read the Full Post]

Heme oxygenase-1 accelerates erastin-induced ferroptotic cell death

461 | Aug 06 2019

Kwon MY et al. showed that hemin and CORM accelerate the HO-1 expression in the presence of Erastin and increase membranous lipid peroxidation. Thus, HO-1 is an essential enzyme for iron-dependent lipid peroxidation during ferroptotic cell death. [Read the Full Post]

RSL3 and Erastin differentially regulate redox signaling to promote Smac mimetic-induced cell death

0 | Aug 06 2019

Dächert J et al. showed that RSL3/BV6 and Erastin/BV6 differentially regulate redox signaling and cell death in ALL cells. While RSL3/BV6 cotreatment induces ferroptotic cell death, Erastin/BV6 stimulates oxidative cell death independently of iron. These findings have important implications for the therapeutic targeting of redox signaling to enhance Smac mimetic-induced cell death in ALL. [Read the Full Post]

Inhibition of apoptosis by caspase inhibitor Z-VAD-FMK improves cryotolerance of in vitro derived bovine embryos

0 | Jul 22 2019

Pero ME et al. indicated the addition of 20 μM Z-VAD-FMK during vitrification/warming and post-warming culture partially inhibits cryopreservation-induced apoptosis by reducing the level of active caspase 3, suggesting a potential use as an additive to ameliorate the efficiency of embryo cryopreservation in cattle, critical for a further diffusion of IVEP technology in the field. Further studies are though needed to evaluate the effect of Z-VAD-FMK on post-transfer embryo development before considering a commercial application. [Read the Full Post]

Inhibition of Bcl-2/xl With ABT-263 Selectively Kills Senescent Type II Pneumocytes and Reverses Persistent Pulmonary Fibrosis Induced by Ionizing Radiation in Mice

465 | Jul 16 2019

Pan J et al. demonstrated that PF can be reversed by a senolytic drug such as ABT-263 after it becomes a progressive disease. Therefore, ABT-263 has the potential to be developed as a new treatment for PF. [Read the Full Post]

Identification of a novel senolytic agent, navitoclax, targeting the Bcl-2 family of anti-apoptotic factors

432 | Jul 15 2019

Zhu Y et al. showed the hypothesis-driven, bioinformatics-based approach we used to discover that dasatinib (D) and quercetin (Q) are senolytic can be extended to increase the repertoire of senolytic drugs, including additional cell type-specific senolytic agents. [Read the Full Post]

Flavopiridol enhances ABT-199 sensitivity in unfavourable-risk multiple myeloma cells in vitro and in vivo

414 | Jul 12 2019

Zhou L et al. argue that CDK9 inhibitors, for example, FP may increase the antimyeloma activity of ABT-199, including in unfavourable-risk MM minimally responsive to ABT-199 alone. [Read the Full Post]

Therapeutics targeting Bcl-2 in hematological malignancies

414 | Jul 12 2019

Ruefli-Brasse A et al. review recent progress in direct and selective targeting of Bcl-2 family proteins for cancer therapy and the search for rationale combinations. [Read the Full Post]

Structural States of Hdm2 and HdmX: X-ray Elucidation of Adaptations and Binding Interactions for Different Chemical Compound Classes

523 | Jun 26 2019

Kallen J et al. used the same numbering for Hdm2 (as in Q00987) and HdmX (as in O15151, but minus 1). Taken together, these structural insights should prove useful for the design and optimization of further selective and/or dual Hdm2/HdmX inhibitors. [Read the Full Post]

Direct Activation of BAX by BTSA1 Overcomes Apoptosis Resistance in Acute Myeloid Leukemia

472 | Jun 24 2019

Reyna DE et al. provides proof-of-concept for direct BAX activation as a treatment strategy in AML. [Read the Full Post]

Curaxin CBL0137 has the potential to reverse HIV-1 latency

822 | Jun 24 2019

Jean MJ et al. indicated that CBL0137 possesses capabilities as a LRA and could be considered for the "shock and kill" approach. [Read the Full Post]

Increased MCL-1 expression predicts poor prognosis and disease recurrence in acute myeloid leukemia

440 | Jun 13 2019

Li XX et al. suggested that higher expression of MCL-1 predicts poor prognosis and can be used for disease monitoring. [Read the Full Post]

Combination of Emricasan with Ponatinib Synergistically Reduces Ischemia/Reperfusion Injury in Rat Brain Through Simultaneous Prevention of Apoptosis and Necroptosis

638 | Jun 10 2019

Tian J et al. concluded that combination of emricasan with ponatinib could synergistically reduce I/R injury in rat brain through simultaneous prevention of apoptosis and necroptosis. Our findings might lay a basis on extension of the clinical indications for emricasan and ponatinib in treating ischemic stroke. [Read the Full Post]

Superior anti-tumor activity of the MDM2 antagonist idasanutlin and the Bcl-2 inhibitor venetoclax in p53 wild-type acute myeloid leukemia models

823 | Jun 08 2019

Lehmann C et al provided functional and molecular insight on the superior anti-tumor activity of combined idasanutlin and venetoclax treatment in AML and support its further exploration in clinical studies. [Read the Full Post]

Regulation of Skeletal Muscle DRP-1 and FIS-1 Protein Expression by IL-6 Signaling

898 | Jun 03 2019

Fix DK et al. elevated IL-6 can directly induce DRP-1 and FIS-1 expression through gp130 signaling in cultured myotubes and skeletal muscle. Furthermore, ERK 1/2 signaling is necessary for the IL-6 induction of DRP-1 and FIS-1 expression in myotubes. [Read the Full Post]

Hemin-induced platelet activation and ferroptosis is mediated through ROS-driven proteasomal activity and inflammasome activation: Protection by Melatonin

546 | May 26 2019

NaveenKumar SK et al. demonstrated an association of platelet activation/ferroptosis with proteasome activity and inflammasome activation. Although, high-throughput screening has recognized ferrostatin-1 (Fer-1) and liproxstatin-1 (Lip-1) as potent ferroptosis inhibitors, having an endogenous antioxidant such as MLT as ferroptosis inhibitor is of high interest. MLT is a well-known chronobiotic hormone that regulates the circadian rhythms in vertebrates. It is also known to exhibit potent antioxidant and ROS quenching capabilities. MLT can regulate fundamental cellular functions by exhibiting cytoprotective, oncostatic, antiaging, anti-venom, and immunomodulatory activities. The ROS scavenging capacity of MLT is key for its cytoprotective and anti-apoptotic properties. Considering the anti-ferroptotic and anti-apoptotic potentials MLT, it could be a promising clinical application to treat hemolytic, thrombotic and thrombocytopenic conditions. Therefore, we propose MLT as a pharmacological and therapeutic agent to inhibit ferroptosis and platelet activation. [Read the Full Post]

Bendamustine plus rituximab versus fludarabine plus rituximab for patients with relapsed indolent and mantle-cell lymphomas: a multicentre, randomised, open-label, non-inferiority phase 3 trial

1268 | May 21 2019

Rummel M et al. indicated that in combination with rituximab, bendamustine was more effective than fludarabine, suggesting that bendamustine plus rituximab may be the preferred treatment option for patients with relapsed indolent and mantle-cell lymphomas. [Read the Full Post]

Inhibition of apoptosis by caspase inhibitor Z-VAD-FMK improves cryotolerance of in vitro derived bovine embryos

1169 | May 17 2019

Pero ME et al. found that the addition of 20 μM Z-VAD-FMK during vitrification/warming and post-warming culture partially inhibits cryopreservation-induced apoptosis by reducing the level of active caspase 3, suggesting a potential use as an additive to ameliorate the efficiency of embryo cryopreservation in cattle, critical for a further diffusion of IVEP technology in the field. [Read the Full Post]

MPP+ induces necrostatin-1- and ferrostatin-1-sensitive necrotic death of neuronal SH-SY5Y cells

0 | May 06 2019

Ito K et al. found that MPP+ predominantly induced non-apoptotic death of neuronally differentiated SH-SY5Y cells. This cell death was strongly inhibited by necrostatin-1 (Nec-1), a necroptosis inhibitor, and by an indole-containing compound (3,3'-diindolylmethane: DIM). However, it occurred independently of receptor-interacting serine/threonine-protein kinase 1/3 (RIP1/RIP3), indicating that this form of cell death was not necroptosis. MPP+-induced cell death was also inhibited by several inhibitors of ferroptosis, including ferrostatin-1 (Fer-1). Although MPP+-induced death and ferroptosis shared some features, such as occurrence of lipid peroxidation and inhibition by Fer-1, MPP+-induced death seemed to be distinct from ferroptosis because MPP+-induced death (but not ferroptosis) was inhibited by Nec-1, was independent of p53, and was accompanied by ATP depletion and mitochondrial swelling. Further investigation of MPP+-induced non-apoptotic cell death may be useful for understanding the mechanisms of neuronal loss and for treatment of neurodegenerative diseases such as Parkinson's disease. [Read the Full Post]

Suppression of human T cell proliferation by the caspase inhibitors, z-VAD-FMK and z-IETD-FMK is independent of their caspase inhibition properties

791 | May 04 2019

Lawrence CP et al. demonstrated that both z-VAD-FMK and z-IETD-FMK are immunosuppressive in vitro and inhibit T cell proliferation without blocking the processing of caspase-8 and caspase-3. [Read the Full Post]

On the Mechanism of Cytoprotection by Ferrostatin-1 and Liproxstatin-1 and the Role of Lipid Peroxidation in Ferroptotic Cell Death

612 | Apr 30 2019

Zilka O et al. demonstrated that potent RTAs subvert ferroptosis and suggest that lipid peroxidation (autoxidation) may play a central role in the process. [Read the Full Post]

The Caspase 1 Inhibitor VX-765 Protects the Isolated Rat Heart via the RISK Pathway

847 | Apr 22 2019

Do Carmo H et al. indicated the caspase 1 inhibitor, VX-765, was able to reduce myocardial infarction in a model of IR injury. However, the addition of IPC did not demonstrate any further protection. [Read the Full Post]

Napabucasin: An Update on the First-in-Class Cancer Stemness Inhibitor

986 | Apr 11 2019

Hubbard JM et al. showed that napabucasin may prove useful in targeting cancer stem cells, with the potential to suppress metastasis and prevent relapse in patients with varying cancer types. [Read the Full Post]

Lipoxygenase-mediated generation of lipid peroxides enhances ferroptosis induced by erastin and RSL3

473 | Apr 08 2019

Shintoku R et al suggested that tumor ferroptosis is promoted by LOX-catalyzed lipid hydroperoxide generation in cellular membranes. [Read the Full Post]

Bcl-xL inhibition enhances Dinaciclib-induced cell death in soft-tissue sarcomas

551 | Apr 05 2019

Rello-Varona S et al showed that Bcl-xL inhibitor A-1331852 also synergized with conventional chemotherapy drugs as Gemcitabine. Thus, Bcl-xL targeted therapy arises as a major opportunity to the treatment of STS. [Read the Full Post]

Memantine and Q-VD-OPh Treatments in Experimental Spinal Cord Injury: Combined Inhibition of Necrosis and Apoptosis

723 | Apr 05 2019

Aydoseli A et al showed that combined use of memantine and Q-VD-OPh provides better histological and clinical results. The combined inhibition of the two major pathways, necrosis and apoptosis, needs to be further assessed with in-vivo or in-vitro studies. [Read the Full Post]

Pharmacological clearance of senescent cells improves survival and recovery in aged mice following acute myocardial infarction

433 | Apr 04 2019

Walaszczyk A et al. provided proof-of-concept evidence that senescent cells are major contributors to impaired function and increased mortality following MI and that senolytics are a potential new therapeutic avenue for MI. [Read the Full Post]

MCL-1 or BCL-xL-dependent resistance to the BCL-2 antagonist (ABT-199) can be overcome by specific inhibitor as single agents and in combination with ABT-199 in acute myeloid leukemia cells

400 | Apr 02 2019

Wang Q et al. showed that ABT-199 could synergize with A-1210477 in vitro or in vivo. [Read the Full Post]

Targeting Oxidative Stress With Auranofin or Prima-1Met to Circumvent p53 or Bax/Bak Deficiency in Myeloma Cells

455 | Mar 29 2019

Tessoulin B et al. showed that auranofin and Prima-1Metsimilarly overcome cell death resistance in myeloma cells due to either p53 deficiency or to mitochondrial dysfunction. [Read the Full Post]

Down-regulation of JMJD5 suppresses metastasis and induces apoptosis in oral squamous cell carcinoma by regulating p53/NF-κB pathway

1790 | Mar 19 2019

Yao Y et al. supplied mechanistic insights into the effects of JMJD5 on the modulation of OSCC development, illustrating that JMJD5 might be an essential prognostic indicator and therapeutic target against OSCC progression. [Read the Full Post]

Neuroprotection with the P53-Inhibitor Pifithrin-μ after Cardiac Arrest in a Rodent Model

1981 | Mar 18 2019

Glas M et al. indicated that temporarily inhibition of apoptosis with pifithrin-μ after cardiac arrest decreases the number of injured neurons in the CA1 segment of hippocampus in a cardiac arrest rat model, without clinical correlate. Further studies should elucidate the role of this neuroprotective agent in different settings and with longer cardiac arrest. [Read the Full Post]

Nutlin-3a selects for cells harbouring TP53 mutations

708 | Mar 04 2019

Kucab JE et al. suggested that including a Nutlin-3a counter-screen significantly improves the specificity and efficiency of the HIMA, whereby TP53-mutated clones are selected prior to sequencing and TP53-WT clones can be discarded. [Read the Full Post]

RSL3 and Erastin differentially regulate redox signaling to promote Smac mimetic-induced cell death

681 | Feb 25 2019

Dächert J et al. indicated that RSL3/BV6 and Erastin/BV6 differentially regulate redox signaling and cell death in ALL cells. While RSL3/BV6 cotreatment induces ferroptotic cell death, Erastin/BV6 stimulates oxidative cell death independently of iron. These findings have important implications for the therapeutic targeting of redox signaling to enhance Smac mimetic-induced cell death in ALL. [Read the Full Post]

Practice patterns and outcomes with the use of regorafenib in metastatic colorectal cancer: Results from the Regorafenib in Metastatic colorectal cancer - An Indian exploratory analysis study

1017 | Feb 19 2019

Ramaswamy A et al. indicated duration of treatment with regorafenib as an efficacy end point in this study is similar to available data from other regions as it is the side effect profile. [Read the Full Post]

Regorafenib for patients with hepatocellular carcinoma who progressed on sorafenib treatment (RESORCE): a randomised, double-blind, placebo-controlled, phase 3 trial

1248 | Feb 18 2019

Bruix J et al. indicated that regorafenib is the only systemic treatment shown to provide survival benefit in HCC patients progressing on sorafenib treatment. Future trials should explore combinations of regorafenib with other systemic agents and third-line treatments for patients who fail or who do not tolerate the sequence of sorafenib and regorafenib. [Read the Full Post]

Cooperation of IRAK1/4 inhibitor and ABT-737 in nanoparticles for synergistic therapy of T cell acute lymphoblastic leukemia

724 | Feb 13 2019

Wu X et al. indicated taht they conducted in vivo experiments in which IRAK/ABT-NP exhibited greater cytotoxicity toward T-ALL cells, the capacity to significantly restore white blood cell number in peripheral blood, and improved survival time of T-ALL mouse model compared to the IRAK1/4 and ABT-737 combined solution. [Read the Full Post]

Nutlin-3, A p53-Mdm2 Antagonist for Nasopharyngeal Carcinoma Treatment

969 | Feb 05 2019

Yee-Lin V et al. Nutlin-3, a small molecule inhibitor that specifically targets p53-Mdm2 interaction offers new therapeutic opportunities by enhancing cancer cell growth arrest and apoptosis through the restoration of the p53-mediated tumor suppression pathway while producing minimal cytotoxicity and side effects. [Read the Full Post]

The caspase-8 inhibitor emricasan combines with the SMAC mimetic birinapant to induce necroptosis and treat acute myeloid leukemia

598 | Feb 01 2019

Brumatti G et al. demonstrated antileukemic efficacy and safety of the birinapant/emricasan combination in vivo suggest that induction of necroptosis warrants clinical investigation as a therapeutic opportunity in AML. [Read the Full Post]

MDM2 is implicated in high-glucose-induced podocyte mitotic catastrophe via Notch1 signalling

716 | Jan 29 2019

Tang H, et al. found that high glucose up-regulates MDM2 expression and leads to podocyte MC. Notch1 signalling is an essential downstream pathway of MDM2 in mediating HG-induced MC in podocytes. [Read the Full Post]

Drp1 mediates compression-induced programmed necrosis of rat nucleus pulposus cells by promoting mitochondrial translocation of p53 and nuclear translocation of AIF

529 | Jan 28 2019

Lin H et al. indicated that Drp1 mediates compression-induced programmed necrosis of NP cells by promoting mitochondrial translocation of p53 and nuclear translocation of AIF. [Read the Full Post]

Targeting MCL-1 sensitizes human esophageal squamous cell carcinoma cells to cisplatin-induced apoptosis

452 | Jan 06 2019

Yu X et al. suggested that MCL-1 contributes to the development of ESCC and is a promising therapeutic target for chemosensitization of ESCC cells to cisplatin. This might provide a scientific basis for developing effective approaches to treat the subset of ESCCs patients with MCL-1 overexpression. [Read the Full Post]

RNA Polymerase I Inhibition with CX-5461 as a Novel Therapeutic Strategy to Target MYC in Multiple Myeloma

748 | Dec 24 2018

Lee HC et al. provided a rationale for the clinical translation of CX-5461 as a novel therapeutic approach to target MYC in myeloma. [Read the Full Post]

WIP1 modulates responsiveness to Sonic Hedgehog signaling in neuronal precursor cells and medulloblastoma

0 | Dec 23 2018

Wen J et al. found that Wip1 knockdown or treatment with a WIP1 inhibitor suppressed the effects of Shh stimulation and potentiated the growth inhibitory effects of SHH pathway-inhibiting drugs in Shh-activated MB cells in vitro. [Read the Full Post]

Regulation of XIAP Turnover Reveals a Role for USP11 in Promotion of Tumorigenesis

0 | Dec 22 2018

Zhou Z et al. proposed that aberrant USP11, via stabilization of XIAP, promotes tumor initiation and progression. [Read the Full Post]

Heme oxygenase-1 mitigates ferroptosis in renal proximal tubule cells

547 | Dec 13 2018

Adedoyin O et al. demonstrated an important antiferroptotic role of HO-1 in renal epithelial cells. [Read the Full Post]

Parthenolide inhibits the initiation of experimental autoimmune neuritis

1715 | Dec 09 2018

Zhang M et al. indicated that PAR plays dual roles in EAN and it is not proper to be applied in autoimmune diseases of nervous system. [Read the Full Post]

Inhibitors of ubiquitin E3 ligase as potential new antimalarial drug leads

978 | Dec 04 2018

Jain J et al. provided better understanding regarding the importance of E3 ligase functions in the malaria parasite as a potential new antimalarial drug target and a new class of antimalarial drug leads. [Read the Full Post]

RCN1 suppresses ER stress-induced apoptosis via calcium homeostasis and PERK-CHOP signaling

1249 | Nov 24 2018

Xu S et al. indicated that RCN1, a target of NF-κB, suppresses ER calcium release by binding to IP3R1 and decreases the UPR, thereby inhibiting ER stress-induced apoptosis. [Read the Full Post]

Circadian rhythm disruption impairs tissue homeostasis and exacerbates chronic inflammation in the intestine

679 | Nov 18 2018

Pagel R et al. suggested that circadian rhythm stability is pivotal for the maintenance of mucosal barrier function. CRD increases intestinal necroptosis, thus rendering the gut epithelium more susceptible to inflammatory processes.-Pagel, R., Bär, F., Schröder, T., Sünderhauf, A., Künstner, A., Ibrahim, S. M., Autenrieth, S. E., Kalies, K., König, P., Tsang, A. H., Bettenworth, D., Divanovic, S., Lehnert, H., Fellermann, K., Oster, H., Derer, S., Sina, C. Circadian rhythm disruption impairs tissue homeostasis and exacerbates chronic inflammation in the intestine. [Read the Full Post]

Stress-induced dynamic regulation of mitochondrial STAT3 and its association with cyclophilin D reduce mitochondrial ROS production

1052 | Nov 03 2018

Meier JA et al. outlined a role for mitochondrially localized STAT3 in sensing and responding to external stimuli. [Read the Full Post]

BIM mediates synergistic killing of B-cell acute lymphoblastic leukemia cells by BCL-2 and MEK inhibitors

0 | Oct 30 2018

Korfi K et al. observed in B-ALL cells driven by a range of genetic abnormalities and therefore has significant therapeutic potential. [Read the Full Post]

AT101 exerts a synergetic efficacy in gastric cancer patients with 5-FU based treatment through promoting apoptosis and autophagy

740 | Oct 29 2018

Wei X et al. showed APE1 is guided as a potential therapeutic target for gastric cancer. AT101 could be regarded as a potent inhibitor to promote chemotherapeutic sensitivity in patients with gastric cancer. [Read the Full Post]

Loss of XIAP facilitates switch to TNFα-induced necroptosis in mouse neutrophils

2181 | Oct 28 2018

Wicki S et al. may implicated an important role of neutrophils in the development of hyperinflammation and disease progression of patients diagnosed with X-linked lymphoproliferative syndrome type 2, which are deficient in XIAP. [Read the Full Post]

FANCD2 protects against bone marrow injury from ferroptosis

548 | Oct 27 2018

Song X et al. indicate that FANCD2 plays a novel role in the negative regulation of ferroptosis. [Read the Full Post]

Identification of mTOR as a primary resistance factor of the IAP antagonist AT406 in hepatocellular carcinoma cells

0 | Oct 24 2018

Zhen MC et al. concluded that mTOR could be a key resistance factor of AT406 in HCC cells. [Read the Full Post]

AT-101 inhibits hedgehog pathway activity and cancer growth

0 | Oct 02 2018

Wang J et al. revealed a novel molecular mechanism responsible for the anticancer action of AT-101 and contributes to the further development of AT-101 as an anticancer drug. [Read the Full Post]

JAK/STAT signaling pathway-mediated immune response in silkworm (Bombyx mori) challenged by Beauveria bassiana

1136 | Sep 09 2018

Geng T et al. suggested that BmCTL5 might be one pattern recognition receptors for JAK/STAT signaling pathway in silkworm. These findings yield insights for better understand the molecular mechanisms of JAK/STAT signaling pathway in antifungal immune response in silkworm. [Read the Full Post]

microRNA-200a silencing protects neural stem cells against cerebral ischemia/reperfusion injury

1127 | Sep 09 2018

Ma J et al. indicated miR-200a silencing protects NSCs from OGD/R-induced injury, possibly via regulating the STATs/c-Myc and MAPK/c-Myc signalings. [Read the Full Post]

Niclosamide inhibition of STAT3 synergizes with erlotinib in human colon cancer

0 | Sep 05 2018

Shi L et al. suggested that erlotinib and niclosamide combination provides an effective therapeutic approach to improving the prognosis of colon cancer. [Read the Full Post]

MicroRNA-17 regulates autophagy to promote hepatic ischemia/reperfusion injury via suppression of signal transductions and activation of transcription-3 expression

1004 | Sep 02 2018

Li S et al. showed that high levels of miR-17 expression can function to up-regulate autophagy to aggravate hepatic IRI by suppressing Stat3 expression. Liver Transplantation 22 1697-1709 2016 AASLD. [Read the Full Post]

A NOXA/MCL-1 Imbalance Underlies Chemoresistance of Malignant Rhabdoid Tumor Cells

751 | Aug 19 2018

Ouchi K et al. suggested that modulation of the NOXA/MCL-1 pathway may be a potential strategy for the treatment of patients with MRT. [Read the Full Post]

DRP-1 is required for BH3 mimetic-mediated mitochondrial fragmentation and apoptosis

697 | Aug 19 2018

Milani M et al. provided new insights into MCL-1 ligands, and the interplay between DRP-1 and the anti-apoptotic BCL-2 family members in the regulation of apoptosis. [Read the Full Post]

Combined treatment of carfilzomib and z-VAD-fmk inhibits skeletal proteolysis and apoptosis and ameliorates cancer cachexia

1008 | Aug 06 2018

Wang Q et al. found that Combined treatment with CFZ and z-VAD-fmk early in the development of cachexia was associated with signs of less proteolysis and apoptosis and less severe cachexia in a mouse model of cancer-induced cachexia. [Read the Full Post]

Inhibitor of apoptosis protein expression in glioblastomas and their in vitro and in vivo targeting by SMAC mimetic GDC-0152

756 | Jul 23 2018

Tchoghandjian A et al. revealed for the first time that ML-IAP protein expression correlates with GBM patient survival and that its antagonist GDC-0152 improves outcome in xenografted mouse. [Read the Full Post]

Anti-apoptotic Bcl-XL but not Mcl-1 contributes to protection against virus-induced apoptosis

681 | Jul 17 2018

Ohmer M et al. showed that Mcl-1 is dispensable for the regulation of apoptosis during infection with different large DNA viruses, either because the viruses replace its function (in fibroblasts and epithelial cells) or because the pro-apoptotic activity generated by the infection appears not to be blocked by it (in macrophages). [Read the Full Post]

Ferroptosis is an autophagic cell death process

921 | Jul 12 2018

Gao M et al. indicated that ferroptosis is an autophagic cell death process, and NCOA4-mediated ferritinophagy supports ferroptosis by controlling cellular iron homeostasis. [Read the Full Post]

BIM mediates synergistic killing of B-cell acute lymphoblastic leukemia cells by BCL-2 and MEK inhibitors

1146 | Jun 13 2018

Korfi K et al. observed in B-ALL cells driven by a range of genetic abnormalities and therefore has significant therapeutic potential. [Read the Full Post]

Calcineurin complex isolated from T-cell acute lymphoblastic leukemia (T-ALL) cells identifies new signaling pathways including mTOR/AKT/S6K whose inhibition synergize with calcineurin inhibition to promote T-ALL cell death

0 | May 31 2018

Tosello V et al. identified AKT inhibition as a novel promising drug combination to potentiate the pro-apoptotic effects of Cn inhibitors. [Read the Full Post]

Etoposide Induces Apoptosis in Activated Human Hepatic Stellate Cells via ER Stress

1631 | May 31 2018

Wang C et al. demonstrated that VP-16 exerts a proapoptotic effect on LX-2 cells and has an antifibrogenic effect on collagen deposition, suggesting a new strategy for the treatment of liver fibrosis. [Read the Full Post]

Glucocorticoids Prevent Enterovirus 71 Capsid Protein VP1 Induced Calreticulin Surface Exposure by Alleviating Neuronal ER Stress

1540 | May 29 2018

Hu DD et al. identified VP1-promoted Ecto-CRT upregulation as a novel mechanism of EV71-induced neuronal cell damage and highlight the potential of the use of glucocorticoids to treat severe HFMD patients with CNS complications. [Read the Full Post]

Niclosamide inhibition of STAT3 synergizes with erlotinib in human colon cancer

1718 | May 28 2018

Shi L et al. suggested that erlotinib and niclosamide combination provides an effective therapeutic approach to improving the prognosis of colon cancer. [Read the Full Post]

Pharmacological Inhibition of PERK Attenuates Early Brain Injury After Subarachnoid Hemorrhage in Rats Through the Activation of Akt

1474 | May 19 2018

Yan F et al. found that PERK might serve as a promising target for future therapeutic intervention. [Read the Full Post]

Melatonin alleviates inflammasome-induced pyroptosis through inhibiting NF-κB/GSDMD signal in mice adipose tissue

3274 | May 16 2018

Liu Z et al. revealed a novel function of melatonin on adipocyte pyroptosis, suggesting a new potential therapy for melatonin to prevent and treat obesity caused systemic inflammatory response. [Read the Full Post]

Myosin IIA-related Actomyosin Contractility Mediates Oxidative Stress-induced Neuronal Apoptosis

1153 | May 16 2018

Wang Y et al. unraveled the biochemical and mechanistic mechanisms during oxidative stress-induced neuronal apoptosis and may be applicable for the development of therapies for CNS diseases. [Read the Full Post]

Nutlin-3a: A Potential Therapeutic Opportunity for TP53 Wild-Type Ovarian Carcinomas

948 | May 15 2018

Crane EK et al. found that Nutlin-3a could be a potential therapeutic agent for ovarian carcinomas expressing wild-type TP53 and warrants further investigation. [Read the Full Post]

p53-related protein kinase confers poor prognosis and represents a novel therapeutic target in multiple myeloma

1390 | Apr 23 2018

Hideshima T et al. demonstrated that either genetic or pharmacological inhibition of TP53RK triggers MM cell apoptosis via both p53-Myc axis-dependent and axis-independent pathways, validating TP53RK as a novel therapeutic target in patients with poor-prognosis MM. [Read the Full Post]

Diabetes mellitus stimulates pancreatic cancer growth and epithelial-mesenchymal transition-mediated metastasis via a p38 MAPK pathway

0 | Apr 23 2018

Wang L et al. revealed that p38 MAPK inhibitors may provide a novel intervention strategy for diabetic pancreatic cancer treatment. [Read the Full Post]

4-Hydroxy-2-nonenal induces apoptosis by activating ERK1/2 signaling and depleting intracellular glutathione in intestinal epithelial cells

1758 | Apr 08 2018

Ji Y et al. provided new insights into a functional role of MKP-1 in oxidative stress-induced cell death by regulating ERK1/2 MAP kinase in intestinal epithelial cells. [Read the Full Post]

Cancer-associated fibroblasts attenuate Cisplatin-induced apoptosis in ovarian cancer cells by promoting STAT3 signaling

1248 | Apr 06 2018

Yan H et al. suggested that CAFs could activate the anti-apoptotic STAT3 signaling, thereby decrease the Cisplatin-induced apoptosis and promote chemoresistance in ovarian cancer. [Read the Full Post]

In situ electrochemical evaluation of dsDNA interaction with the anticancer drug danusertib nitrenium radical product using the DNA-electrochemical biosensor

3607 | Apr 05 2018

Diculescu VC et al. indicated the danusertib nitrenium cation radical redox metabolite was covalently attached to the C8 of guanine residues preventing their oxidation. An interaction mechanism of dsDNA-danusertib is proposed and the formation of the danusertib redox nitrenium radical metabolite-guanine adduct explained. [Read the Full Post]

Targeting Autophagy Sensitizes BRAF-Mutant Thyroid Cancer to Vemurafenib

1502 | Apr 05 2018

Wang W et al. demonstrated that vemurafenib induces ER stress response-mediated autophagy in thyroid cancer and autophagy inhibition may be a beneficial strategy to sensitize BRAF-mutant thyroid cancer to vemurafenib. [Read the Full Post]

Novel MDM2 inhibitor SAR405838 (MI-773) induces p53-mediated apoptosis in neuroblastoma

975 | Apr 03 2018

Lu J et al. suggested that MDM2-specific inhibitors like SAR405838 may serve not only as a stand-alone therapy, but also as an effective adjunct to current chemotherapeutic regimens for treating NB with an intact MDM2-p53 axis. [Read the Full Post]

Downregulation of B-myb promotes senescence via the ROS-mediated p53/p21 pathway, in vascular endothelial cells

1709 | Mar 24 2018

Zhou Z et al. suggested that B-myb may be a novel candidate for regulating cell senescence to protect against endothelial senescence-related cardiovascular diseases. [Read the Full Post]

Late-stage inhibition of autophagy enhances calreticulin surface exposure

1484 | Mar 07 2018

Li DD et al. highlight the potential of the combined use of ER stress inducers and autophagy late-stage inhibitors to reestablish and strengthen both the CRT exposure and immunogenicity of chemotherapeutic agents induced death cells. [Read the Full Post]

HSPA5 Regulates Ferroptotic Cell Death in Cancer Cells

0 | Mar 07 2018

Zhu S et al. identified a novel role of HSPA5 in ferroptosis and suggest a potential therapeutic strategy for overcoming gemcitabine resistance. [Read the Full Post]

UMI-77 primes glioma cells for TRAIL-induced apoptosis by unsequestering Bim and Bak from Mcl-1

871 | Mar 01 2018

Liu JW et al. showed that UMI-77 enhances TRAIL-induced apoptosis by unsequestering Bim and Bak, which provides a novel therapeutic strategy for the treatment of gliomas. [Read the Full Post]

Strain- and host species-specific inflammasome activation, IL-1β release, and cell death in macrophages infected with uropathogenic Escherichia coli

3262 | Feb 26 2018

Schaale K et al. indicated in mouse macrophages, CFT073-triggered inflammasome responses are completely NLRP3-dependent, and largely α-hemolysin-dependent. In contrast, UPEC activates an NLRP3-independent cell death pathway and an α-hemolysin-independent IL-1β secretion pathway in human macrophages. This has important implications for understanding UTI in [Read the Full Post]

Pharmacological inhibition of Bcl-xL sensitizes osteosarcoma to doxorubicin

813 | Feb 21 2018

Baranski Z et al. identified Bcl-xL as a candidate drug target for sensitization to chemotherapy in patients with osteosarcoma. [Read the Full Post]

Nanoparticle-Mediated Mitochondrial Damage Induces Apoptosis in Cancer

1225 | Jan 28 2018

Mallick A et al. presented here clearly stimulate the usage of multiple drugs to perturb simultaneously diverse targets, selectively in mitochondria, as next-generation cancer therapeutics. [Read the Full Post]

Ablation of ferroptosis regulator glutathione peroxidase 4 in forebrain neurons promotes cognitive impairment and neurodegeneration

962 | Jan 26 2018

Hambright WS et al. suggested that ferroptosis may be an important neurodegenerative mechanism in diseases such as AD. [Read the Full Post]

Chenodeoxycholic acid activates NLRP3 inflammasome and contributes to cholestatic liver fibrosis

1527 | Jan 12 2018

Gong Z et al. offered a mechanistic basis to ameliorate cholestatic liver fibrosis by targeting inflammasome activation. [Read the Full Post]

AKT is indispensable for coordinating Par-4/JNK cross talk in p21 downmodulation during ER stress

1531 | Jan 10 2018

Rasool RU et al. found that 3-AWA inhibits colorectal tumor growth and formation of colorectal polyps at a tolerable dose, similar to the first-line drug for colorectal cancer-5-fluorouracil. [Read the Full Post]

Biliary tract instillation of a SMAC mimetic induces TRAIL-dependent acute sclerosing cholangitis-like injury in mice

929 | Jan 08 2018

Guicciardi ME et al. contributed to the development of the disease. Our results also indicate that inhibition of TRAIL signaling pathways may be beneficial in the treatment of PSC. [Read the Full Post]

Human Papillomavirus Downregulates the Expression of IFITM1 and RIPK3 to Escape from IFNγ- and TNFα-Mediated Antiproliferative Effects and Necroptosis

2363 | Jan 07 2018

Ma W et al. revealed how hrHPV deregulates two pathways involved in cell death and growth regulation to withstand immune-mediated control of hrHPV-infected cells. [Read the Full Post]

Blocking EZH2 methylation transferase activity by GSK126 decreases stem cell-like myeloma cells

2183 | Jan 05 2018

Zeng D et al. suggested that EZH2 inactivation by GSK126 is effective in killing MM cells and CSCs as a single agent or in combination with bortezomib. Clinical trial of GSK126 in patients with MM may be warranted. [Read the Full Post]

Activation of oncogenic pathways in classical Hodgkin lymphoma by decitabine: A rationale for combination with small molecular weight inhibitors.

1564 | Dec 29 2017

Swerev TM et al. concluded that targeting of oncogenic pathways of cHL may improve efficacy of DNA-demethylating therapy in cHL. [Read the Full Post]

Matrine induces Akt/mTOR signalling inhibition-mediated autophagy and apoptosis in acute myeloid leukaemia cells

1377 | Dec 20 2017

Wu J et al. indicated that matrine exerts antitumour effect through apoptosis and autophagy, and the latter one might be a potential therapeutic strategy for AML. [Read the Full Post]

THZ1 targeting CDK7 suppresses STAT transcriptional activity and sensitizes T-cell lymphomas to BCL2 inhibitors

1503 | Dec 14 2017

Cayrol F et al. showed that the combination of THZ1 and the BH3 mimetic obatoclax improves lymphoma growth control in a primary PTCL ex vivo culture and in two STAT3-mutant PTCL xenografts, delineating a potential targeted agent-based therapeutic option for these patients. [Read the Full Post]

Interleukin-6 suppression reduces tumour self-seeding by circulating tumour cells in a human osteosarcoma nude mouse model

1474 | Dec 12 2017

Zhang Y et al. provided a novel strategy for future therapeutic interventions to prevent osteosarcoma progression and recurrence. [Read the Full Post]

E platinum, a newly synthesized platinum compound, induces apoptosis through ROS-triggered ER stress in gastric carcinoma cells

1576 | Dec 09 2017

Wang X et al. indicated that E Platinum may be a potential and effective treatment for gastric cancer in clinical. [Read the Full Post]

Histone Deacetylase Inhibitor Trichostatin a Promotes the Apoptosis of Osteosarcoma Cells through p53 Signaling Pathway Activation

1180 | Dec 07 2017

Deng Z et al. indicated class I HDACs play a central role in the pathogenesis of osteosarcoma, and HDAC inhibitors may thus have promise as new therapeutic agents against osteosarcoma. [Read the Full Post]

High efficacy of the BCL-2 inhibitor ABT199 (venetoclax) in BCL-2 high-expressing neuroblastoma cell lines and xenografts and rational for combination with MCL-1 inhibition

1074 | Dec 03 2017

Bate-Eya LT et al. suggested that neuroblastoma patients with high BCL-2 and BIM/BCL-2 complex levels might benefit from combination treatment with ABT199 and compounds that inhibit MCL-1 expression. [Read the Full Post]

HSPA5 Regulates Ferroptotic Cell Death in Cancer Cells

1038 | Oct 23 2017

Zhu S et al. identified a novel role of HSPA5 in ferroptosis and suggest a potential therapeutic strategy for overcoming gemcitabine resistance. [Read the Full Post]

Chemotherapy-induced Dkk-1 expression by primary human mesenchymal stem cells is p53 dependent

1740 | Oct 23 2017

Hare I et al. indicated that Dkk-1 has been shown to promote tumor growth in several models of malignancy, suggesting that MSC-derived Dkk-1 could counteract the intent of cytotoxic chemotherapy, and that pharmacologic inhibition of Dkk-1 in patients receiving chemotherapy treatment for certain malignancies may be warranted. [Read the Full Post]

Cytokine correlation analysis based on drug perturbation

0 | Oct 18 2017

Wallner FK et al. showed that cytokines are highly co-regulated, which provide valuable information for how a therapeutic drug might affect clusters of cytokines. In addition, a cytokine that is used as a therapeutic biomarker could be combined with its related cytokines into a biomarker panel to improve diagnostic accuracy. [Read the Full Post]

Protective effect of necrostatin-1 on myocardial tissue in rats with acute myocardial infarction

0 | Oct 13 2017

Liu YR et al. found that necrostatin-1 can inhibit myocardial tissue apoptosis and necrosis in acute myocardial infarct rats and has a protective effect on myocardial tissue. [Read the Full Post]

STAT1 as a downstream mediator of ERK signaling contributes to bone cancer pain by regulating MHC II expression in spinal microglia

2052 | Oct 04 2017

Song Z et al. suggested that STAT1 contributes to bone cancer pain as a downstream mediator of ERK signaling by regulating MHC II expression in spinal microglia. [Read the Full Post]

Ultrasound Enhances the Expression of Brain-Derived Neurotrophic Factor in Astrocyte Through Activation of TrkB-Akt and Calcium-CaMK Signaling Pathways

0 | Sep 29 2017

Liu SH et al. found that LIPUS stimulation might play a crucial and beneficial role in neurodegenerative diseases. [Read the Full Post]

Basic FGF and PDGF-BB synergistically stimulate hyaluronan and IL-6 production by orbital fibroblasts

0 | Sep 27 2017

Virakul S et al. found that multi-target therapy directed at the bFGF and PDGF pathways may potentially be of interest for the treatment of GO. [Read the Full Post]

K45A mutation of RIPK1 results in poor necroptosis and cytokine signaling in macrophages, which impacts inflammatory responses in vivo

0 | Sep 18 2017

Shutinoski B et al. indicated that K45 mediated kinase activity of RIPK1 is not only important for necroptosis but it also has a key role in promoting cytokine signaling and host response to inflammatory stimuli. [Read the Full Post]

Targeting of Survivin Pathways by YM155 Inhibits Cell Death and Invasion in Oral Squamous Cell Carcinoma Cells.

0 | Sep 07 2017

Zhang W et al. provided evidence showing that YM155 could act as a small molecule survivin inhibitor on survivin-rich expressed SCC9 cells in culture as well as when grown as tumor in a xenograft model. [Read the Full Post]

Embelin Reduces Systemic Inflammation and Ameliorates Organ Injuries in Septic Rats Through Downregulating STAT3 and NF-κB Pathways

2478 | Sep 05 2017

Zhou XL et al. indicated that embelin ameliorates sepsis in rats through suppressing STAT3 and NF-κB pathways. [Read the Full Post]

Regulation of TRPM7 Function by IL-6 through the JAK2-STAT3 Signaling Pathway

1454 | Sep 05 2017

Liu A et al. indicated IL-6 inhibits the inward TRPM7 current via the JAK2-STAT3 signaling pathway. [Read the Full Post]

Role of BmDredd during Apoptosis of Silk Gland in Silkworm, Bombyx mori

1607 | Sep 04 2017

Chen RT et al. suggested that BmDredd plays a critical role in SG apoptosis. [Read the Full Post]

Calcineurin and GSK-3 inhibition sensitizes T-cell acute lymphoblastic leukemia cells to apoptosis through X-linked inhibitor of apoptosis protein degradation

1150 | Sep 04 2017

Tosello V et al. showed that dual Cn and GSK-3 inhibitor treatment in vitro and in vivo is effective against available models of T-ALL, indicating an insofar untapped therapeutic opportunity. [Read the Full Post]

The Role of the Active Oxygen Produced from Gp91phox NADPH Oxidase on the Newborn Weight of Mouse Pups

1669 | Sep 03 2017

Keiichi Hiramoto et al. indicated that gp91phox NADPH oxidase produces ROS during graviditas. The ROS activate NLRP3, and NLRP3 leads to the production of caspase-1, which subsequently increases IL-1, thereby finally inducing IGF-1. Because the newborn weight is determined by IGF-1, gp91phox appears to be important for promoting fetal growth during graviditas. [Read the Full Post]

Targeting of Survivin Pathways by YM155 Inhibits Cell Death and Invasion in Oral Squamous Cell Carcinoma Cells

0 | Aug 30 2017

Zhang W et al. suggested that survivin could be further developed as a potential therapeutic agent for the treatment of survivin-rich expressed OSCC. [Read the Full Post]

Interleukin 6 induces cell proliferation of clear cell renal cell carcinoma by suppressing hepaCAM via the STAT3-dependent up-regulation of DNMT1 or DNMT3b

1854 | Aug 17 2017

Quan Z et al. provided a novel signal pathway regulating cell proliferation, potentially representing a therapeutic target for RCC. [Read the Full Post]

Cholesterol Synthetase DHCR24 Induced by Insulin Aggravates Cancer Invasion and Progesterone Resistance in Endometrial Carcinoma

2200 | Aug 17 2017

Dai M et al. demonstrated for the first time the crucial role of the insulin/STAT3/DHCR24/PGR axis in the progression of EC by modulating the metastasis and progesterone response, which could serve as potential therapeutic targets for the treatment of EC with progesterone receptor loss. [Read the Full Post]

Lipopolysaccharide increases IL-6 secretion via activation of the ERK1/2 signaling pathway to up-regulate RANKL gene expression in MLO-Y4 cells

1762 | Aug 16 2017

Yu K et al. indicated that LPS up-regulates osteocyte expression of RANKL and IL-6, and the increased RANKL is associated with the up-regulation of IL-6, which involves the ERK1/2 pathway. [Read the Full Post]

Assessment of the chemotherapeutic potential of a new camptothecin derivative, ZBH-1205

0 | Aug 11 2017

Wu D, et al. found that ZBH-1205 is a promising chemotherapeutic agent to be further assessed in large-scale clinical trials. [Read the Full Post]

BRG1 targeting STAT3/VEGFC signaling regulates lymphangiogenesis in colorectal cancer

1726 | Aug 09 2017

Zhu X et al. demonstration of the important roles of the BRG1/STAT3/VEGFC in tumor-associated lymphangiogenesis might lead to the discovery of novel therapeutic targets in the treatment of cancers with BRG1 loss of function. [Read the Full Post]

Bcl-2 phosphorylation confers resistance on chronic lymphocytic leukaemia cells to the BH3 mimetics ABT-737, ABT-263 and ABT-199 by impeding direct binding

1720 | Aug 03 2017

Song T et al. suggested that a structural alteration in the BH3-binding groove was induced by phosphorylation of Bcl-2. Our data also provided a framework to overcome resistance of CLL cells to the ABT compounds by combining pBcl-2 kinase inhibitors with the ABT compounds. [Read the Full Post]

Sorafenib potentiates ABT-737-induced apoptosis in human oral cancer cells

1658 | Aug 02 2017

Kim LH et al. suggest that sorafenib may effectively overcome ABT-737 resistance to apoptotic cell death, which can be a new potential chemotherapeutic strategy against human oral cancer. [Read the Full Post]

Profiling B cell chronic lymphocytic leukemia by reverse phase protein array: Focus on apoptotic proteins

0 | Jul 24 2017

Frezzato F et al. identified some molecules, particularly those involved in apoptosis control, which could be considered for further studies to design new therapeutic strategies in CLL. [Read the Full Post]

Inhibition of Bcl-2 potentiates AZD-2014-induced anti-head and neck squamous cell carcinoma cell activity

0 | Jun 26 2017

Li Y et al. suggested that AZD-2014 could be further tested as a valuable anti-HNSCC agent, either alone or in combination with Bcl-2 inhibitors. [Read the Full Post]

Overcoming resistance to TRAIL-induced apoptosis in solid tumor cells by simultaneously targeting death receptors, c-FLIP and IAPs

0 | Jun 03 2017

Huang Y et al. provided a rationale for the development of TRAIL-induced apoptosis-based cancer therapies. [Read the Full Post]

Erastin Disrupts Mitochondrial Permeability Transition Pore (mPTP) and Induces Apoptotic Death of Colorectal Cancer Cells

0 | May 25 2017

Huo H et al. found that erastin is cytotoxic and pro-apoptotic to colorectal cancer cells. [Read the Full Post]

Targeting survivin as a potential new treatment for chondrosarcoma of bone

0 | May 19 2017

de Jong Y et al. found that survivin is important for chondrosarcoma survival and chondrosarcoma patients might benefit from survivin inhibition using YM155, for which TP53 mutational status can serve as a predictive biomarker. [Read the Full Post]

The apoptotic members CD95, BclxL, and Bcl-2 cooperate to promote cell migration by inducing Ca(2+) flux from the endoplasmic reticulum to mitochondria.

1176 | May 04 2017

Fouqué A et al. revealed a novel molecular mechanism controlled by BclxL to promote cancer cell migration. [Read the Full Post]

The small-molecule IAP antagonist AT406 inhibits pancreatic cancer cells in vitro and in vivo

0 | May 02 2017

Jiang Y et al. suggested that AT406 could be further evaluated as a promising anti-pancreatic cancer agent. [Read the Full Post]

The apoptotic members CD95, BclxL, and Bcl-2 cooperate to promote cell migration by inducing Ca(2+) flux from the endoplasmic reticulum to mitochondria

1108 | Apr 27 2017

Fouqué A et al. revealed a novel molecular mechanism controlled by BclxL to promote cancer cell migration and supports the use of BH3 mimetics as therapeutic options not only to kill tumor cells but also to prevent metastatic dissemination in TNBCs. [Read the Full Post]

The small-molecule IAP antagonist AT406 inhibits pancreatic cancer cells in vitro and in vivo

1834 | Apr 25 2017

Jiang Y et al. suggested that AT406 could be further evaluated as a promising anti-pancreatic cancer agent. [Read the Full Post]

Developmental expression of STATs, nuclear factor-κB and inflammatory genes in the jejunum of piglets during weaning

2984 | Apr 18 2017

Yi H et al found weaning caused severe inflammation associated with activation of the NF-κB and STAT-3 pathways and suppression of STAT-1 and STAT-6 in the jejunum of piglets. [Read the Full Post]

Inhibition of Bcl-2 family members sensitises soft tissue leiomyosarcomas to chemotherapy

1932 | Apr 15 2017

In conclusion,de Graaff MA et al found Bcl-2 family proteins contribute to soft tissue leiomyosarcoma chemoresistance. Antiapoptotic proteins are highly expressed in leiomyosarcoma of soft tissue, and inhibition of these proteins using a BH3 mimetic increases leiomyosarcoma sensitivity to doxorubicin. [Read the Full Post]

BH3 mimetic ABT-737 sensitizes colorectal cancer cells to ixazomib through MCL-1 downregulation and autophagy inhibition

1909 | Apr 12 2017

Yang L et al. found that the combination of ABT-737 with MLN9708 is a promising therapeutic strategy for human colorectal cancer. [Read the Full Post]

Signaling factors and pathways of α-particle irradiation induced bilateral bystander responses between Beas-2B and U937 cells

0 | Apr 12 2017

Fu J et al disclosed novel signaling cascades of macrophage-mediated bilateral bystander responses that the release of TNF-α and IL-8 regulated by MAPK and NF-κB pathways synergistically increased cellular injury after α-particle irradiation. [Read the Full Post]

Resveratrol delays polycystic kidney disease progression through attenuation of nuclear factor κB-induced inflammation

0 | Apr 09 2017

Wu M et al found that the NF-κB signaling pathway is activated and partly responsible for inflammation in polycystic kidney tissues. Targeting inflammation through resveratrol could be a new strategy for PKD treatment in the future. [Read the Full Post]

A synthetic cell-penetrating dominant-negative ATF5 peptide exerts anti-cancer activity against a broad spectrum of treatment resistant cancers

1234 | Apr 02 2017

Karpel-Massler G et al found the idea that CP-d/n-ATF5-S1, administered as a single reagent or in combination with other drugs, holds promise as an innovative, safe, and efficient antineoplastic agent against treatment-resistant cancers. Clin Cancer Res; 22(18); 4698-711. ©2016 AACR. [Read the Full Post]

AT-101 inhibits hedgehog pathway activity and cancer growth

1379 | Mar 17 2017

Wang J et al. demonstrated that AT-101 significantly and selectively inhibits Hh pathway activity by potentially targeting Smo and consequently suppresses the growth of Hh-driven cancer. [Read the Full Post]

Metallothionein-1G facilitates sorafenib resistance through inhibition of ferroptosis

1979 | Mar 10 2017

Sun X et al. found that knockdown of MT-1G by RNA interference increases glutathione depletion and lipid peroxidation, which contributes to sorafenib-induced ferroptosis. [Read the Full Post]

Identification of baicalein as a ferroptosis inhibitor by natural product library screening

1364 | Mar 10 2017

Xie Y et al. found that baicalein enhances cellular anti-ferroptosis capacity and could be a potential therapeutic agent for ferroptosis-associated tissue injury. [Read the Full Post]

Lenalidomide, Thalidomide, and Pomalidomide Reactivate the Epstein-Barr Virus Lytic Cycle through Phosphoinositide 3-Kinase Signaling and Ikaros Expression

2140 | Mar 09 2017

Jones RJ et al. concluded LTP may reactivate EBV-positive resting memory B cells thereby enhancing EBV lytic cycle and host immune suppression. [Read the Full Post]

Assessment of the chemotherapeutic potential of a new camptothecin derivative, ZBH-1205

0 | Mar 04 2017

Wu D et al. found that ZBH-1205 is a promising chemotherapeutic agent to be further assessed in large-scale clinical trials. [Read the Full Post]

Host-based Prophylaxis Successfully Targets Liver Stage Malaria Parasites

2547 | Feb 19 2017

Douglass AN, et al.'s data demonstrate that host-based prophylaxis could be developed into an effective intervention strategy that eliminates LS parasites before the onset of clinical disease and thus opens a [Read the Full Post]

Palmitate increases musclin gene expression through activation of PERK signaling pathway in C2C12 myotubes

0 | Feb 14 2017

Gu N, et al.'s findings suggest that palmitate increases musclin gene expression via the activation of the PERK signaling pathway in C2C12 myotubes. [Read the Full Post]

Activation of the p62-Keap1-NRF2 Pathway Protects Against Ferroptosis in Hepatocellular Carcinoma Cells

0 | Feb 11 2017

Sun X, et al.'s findings demonstrate novel molecular mechanisms and signaling pathways of ferroptosis; the status of NRF2 is a key factor that determines the therapeutic response to ferroptosis-targeted therapies in HCC cells. [Read the Full Post]

Assessment of the chemotherapeutic potential of a new camptothecin derivative, ZBH-1205

0 | Jan 21 2017

Wu D et al. found that ZBH-1205 is a promising chemotherapeutic agent to be further assessed in large-scale clinical trials. [Read the Full Post]

Endothelial Cell Apoptosis Induces TGF-β Signaling-Dependent Host Endothelial-Mesenchymal Transition to Promote Transplant Arteriosclerosis

1956 | Jan 16 2017

Li J et al. suggested that allograft EC apoptosis induced recipient endothelial-mesenchymal (smooth muscle) transition via TGF-β signaling, resulting in recipient EC-derived SMC accumulation as a major mechanism of vascular remodeling during TA. [Read the Full Post]

Host-based Prophylaxis Successfully Targets Liver Stage Malaria Parasites

2893 | Jan 08 2017

Douglass AN, et al.‘’s data demonstrate that host-based prophylaxis could be developed into an effective intervention strategy that eliminates LS parasites before the onset of clinical disease and thus opens a new avenue to prevent malaria. [Read the Full Post]

Palmitate increases musclin gene expression through activation of PERK signaling pathway in C2C12 myotubes

2103 | Jan 07 2017

Gu N et al. suggested that palmitate increases musclin gene expression via the activation of the PERK signaling pathway in C2C12 myotubes. [Read the Full Post]

Targeting of Survivin Pathways by YM155 Inhibits Cell Death and Invasion in Oral Squamous Cell Carcinoma Cells

0 | Dec 24 2016

Zhang W et al. suggested that survivin could be further developed as a potential therapeutic agent for the treatment of survivin-rich expressed OSCC. [Read the Full Post]

Profiling B cell chronic lymphocytic leukemia by reverse phase protein array: Focus on apoptotic proteins

1445 | Dec 14 2016

Frezzato F, et al. identified some molecules, particularly those involved in apoptosis control, which could be considered for further studies to design new therapeutic strategies in CLL. [Read the Full Post]

Assessment of the chemotherapeutic potential of a new camptothecin derivative, ZBH-1205

2803 | Dec 10 2016

Wu D et al. found that ZBH-1205 is a promising chemotherapeutic agent to be further assessed in large-scale clinical trials. [Read the Full Post]

Acute Sensitivity of Ph-like Acute Lymphoblastic Leukemia to the SMAC-Mimetic Birinapant.

0 | Dec 09 2016

In combination therapy, birinapant enhanced the in vivo efficacy of an induction-type regimen of vincristine, dexamethasone, and L-asparaginase against Ph-like ALL xenografts, offering a preclinical rationale to further evaluate this SMAC mimetic for BCP-ALL treatment. [Read the Full Post]

Targeting of Survivin Pathways by YM155 Inhibits Cell Death and Invasion in Oral Squamous Cell Carcinoma Cells

1991 | Dec 03 2016

Zhang W et al. suggested that survivin could be further developed as a potential therapeutic agent for the treatment of survivin-rich expressed OSCC. [Read the Full Post]

K45A mutation of RIPK1 results in poor necroptosis and cytokine signaling in macrophages, which impacts inflammatory responses in vivo

1787 | Nov 27 2016

Shutinoski B et al.'s results indicated that K45 mediated kinase activity of RIPK1 is not only important for necroptosis but it also has a key role in promoting cytokine signaling and host response to inflammatory stimuli. [Read the Full Post]

Protective effect of necrostatin-1 on myocardial tissue in rats with acute myocardial infarction

1725 | Nov 15 2016

Liu YR et al. found that necrostatin-1 can inhibit myocardial tissue apoptosis and necrosis in acute myocardial infarct rats and has a protective effect on myocardial tissue. [Read the Full Post]

Overcoming resistance to TRAIL-induced apoptosis in solid tumor cells by simultaneously targeting death receptors, c-FLIP and IAPs

3024 | Nov 01 2016

Huang Y et al. provided a rationale for the development of TRAIL-induced apoptosis-based cancer therapies. [Read the Full Post]

Erastin Disrupts Mitochondrial Permeability Transition Pore (mPTP) and Induces Apoptotic Death of Colorectal Cancer Cells

1859 | Oct 24 2016

Huo H et al. demonstrated that erastin is cytotoxic and pro-apoptotic to colorectal cancer cells. [Read the Full Post]

Targeting survivin as a potential new treatment for chondrosarcoma of bone

1797 | Oct 17 2016

De Jong Y et al. found that survivin is important for chondrosarcoma survival and chondrosarcoma patients might benefit from survivin inhibition using YM155, for which TP53 mutational status can serve as a predictive biomarker. [Read the Full Post]

Inhibition of Bcl-2 potentiates AZD-2014-induced anti-head and neck squamous cell carcinoma cell activity

3239 | Sep 30 2016

Li Y et al. suggest that AZD-2014 could be further tested as a valuable anti-HNSCC agent, either alone or in combination with Bcl-2 inhibitors. [Read the Full Post]

Developmental expression of STATs, nuclear factor-κB and inflammatory genes in the jejunum of piglets during weaning

7106 | Sep 20 2016

Yi H et al. found that weaning caused severe inflammation associated with activation of the NF-κB and STAT-3 pathways and suppression of STAT-1 and STAT-6 in the jejunum of piglets. [Read the Full Post]

Inhibition of Bcl-2 family members sensitises soft tissue leiomyosarcomas to chemotherapy

2040 | Sep 18 2016

De Graaff MA, et al. found that Bcl-2 family proteins contribute to soft tissue leiomyosarcoma chemoresistance. [Read the Full Post]

Signaling factors and pathways of α-particle irradiation induced bilateral bystander responses between Beas-2B and U937 cells

10323 | Sep 14 2016

[Read the Full Post]

A Synthetic Cell-Penetrating Dominant-Negative ATF5 Peptide Exerts Anticancer Activity against a Broad Spectrum of Treatment-Resistant Cancers

1538 | Sep 07 2016

Karpel-Massler G, et al. found that CP-d/n-ATF5-S1, administered as a single reagent or in combination with other drugs, holds promise as an innovative, safe, and efficient antineoplastic agent against treatment-resistant cancers. [Read the Full Post]

Activation of the p62-Keap1-NRF2 pathway protects against ferroptosis in hepatocellular carcinoma cells

3405 | Aug 31 2016

Sun X, et al. demonstrated novel molecular mechanisms and signaling pathways of ferroptosis; the status of NRF2 is a key factor that determines the therapeutic response to ferroptosis-targeted therapies in HCC cells. [Read the Full Post]

CY190602, a novel DNA/HDAC dual-targeting drug with enhanced anti-cancer potency

9923 | Mar 19 2015

Liu et al. demonstrated a novel bendamustine-derived drug, CY190602, enhanced anticancer potency. [Read the Full Post]

The roles of Bim and Bmf in B-cell development and apoptosis in TACI-lg transgenic mice

4926 | Mar 11 2015

Woess et al. demonstrated B-cell lymphoma 2 (Bcl2) interacting mediator of cell death (Bim) and Bcl2 modifying factor (Bmf), the two pro-apoptotic members of Bcl2 family, mediate apoptosis in the context of lacking BAFF and APRIL. [Read the Full Post]

The role of heat shock protein beta-1 in erastin-induced ferroptosis

4764 | Mar 09 2015

Sun et al. found heat shock protein beta-1 (HSPB1) as a key negative mediator of ferroptotic cancer cell death. [Read the Full Post]

RIP1, a novel oncogenic driver in melanoma

5170 | Mar 06 2015

u et al. found that RIP1 plays a role as an oncogenic driver in human melanoma. [Read the Full Post]

The inhibition of JAK signaling promotes the conversion from white to brown adipocytes

8748 | Dec 17 2014

By using a screening platform of small molecules identification, Moisan et al. found two inhibitors of JAK signaling were able to convert white adipocytes to brown adipocytes. [Read the Full Post]

The Notch signaling controls maintenance of memory CD4+ T cells

10527 | Dec 16 2014

Recently, Maekawa et al. demonstrated Notch signaling is important for the survival of memory CD4+ T cells by regulating glucose uptake. [Read the Full Post]

The binding of mutant p53 and DAB2IP increase the invasion of inflammation induced cancer cells

5035 | Dec 08 2014

Minin et al. inflammatory cytokines can increase the invasive behavior of cancer cells with p53 missense mutants (mutp53). [Read the Full Post]

GP130/JAK/STAT3 signaling pathway induces multiple myeloma

11693 | Nov 24 2014

Dechow et al. determined GP130/JAK/STAT3 signaling pathway is sufficient to induce MM generation in mice retroviral murine BM transduction-transplantation model. [Read the Full Post]

Interactions between Slit-Robo and JAK-STAT signaling in regulation of stem cell-niche adhesion

9142 | Nov 10 2014

Rachel R. Stine et al. found Slit-Robo and JAK-STAT signaling pathways play key roles in stem cells competition within their niches. [Read the Full Post]

FGF21 is not required for CR-mediated IGF-1 reduction or cell proliferation inhibition

8351 | Nov 06 2014

Thompson et al. found that, in response to moderate CR, phosphorylated STAT5 may act as a key molecule, and FGF21 was not required for the down-regulation of IGF-1 expression level or cell proliferation rates. [Read the Full Post]

Neural stem cells "heal" target cells via extracellular vesicles

4530 | Oct 29 2014

Cossetti et al. found NPCs communicate to the host via extracellular vesicles (EVs) and also investigated the cytokine-regulated pathways involved in the communication. It comes to a novel view in the understanding the mechanisms of stem cell therapy. [Read the Full Post]

At101 was developed to put requirements in place for CPA

2622 | Mar 03 2014

AT-101 inhibits a panel of different lymphoproliferative malignancies with IC50 ranged from 1.2 μM to 7.4 μM. [Read the Full Post]

Lenalidomide is effective in induring complete response

2844 | Feb 28 2014

Lenalidomide (Revlimid, CC-5013) is a TNF-α secretion inhibitor with IC50 of 13 nM. [Read the Full Post]

BCL 2 inhibition with ABT 737 prolongs survival in an NRAS

2581 | Feb 26 2014

ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM [Read the Full Post]

Abt199 is designed to block the function of the protein Bcl2

2927 | Feb 14 2014

ABT-199 (GDC-0199) is a Bcl-2-selective inhibitor with Ki of <0.01 nM, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. [Read the Full Post]

Nutlin 3 is a cis imidazoline analog

4505 | Jan 26 2014

Nutlin-3 is a potent and selective Mdm2 (RING finger-dependent ubiquitin protein ligase for itself and p53) antagonist with IC50 of 90 nM; stabilizes p73 in p53-deficient cells. [Read the Full Post]

Abt 199 is designed to block the protein Bcl 2

3034 | Jan 16 2014

ABT-199 (GDC-0199) is a Bcl-2-selective inhibitor with Ki of <0.01 nM, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. [Read the Full Post]

ABT 737 is a small molecule that acts as a selective inhibitor of Bcl 2

2925 | Dec 23 2013

ABT-737 shows low activity to Bcl-B and no effects to Mcl-1 and BFL-1. [Read the Full Post]

Abt199 is designed to block the function of the protein Bcl 2

2650 | Dec 17 2013

ABT-199 (GDC-0199) is a Bcl-2-selective inhibitor with Ki of <0.01 nM, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. [Read the Full Post]

AT101 was developed to put requirements in place for CPAs

2746 | Dec 13 2013

AT-101 inhibits a panel of different lymphoproliferative malignancies with IC50 ranged from 1.2 μM to 7.4 μM. [Read the Full Post]

ABT 263 was formulated in 10 ethano

2989 | Dec 05 2013

ABT-263 is structurally related to ABT-737; it is a disruptor of Bcl-2/Bcl-xL interactions with pro-apoptotic proteins. [Read the Full Post]

Nutlin 3 inhibits the interaction between the proteins p53 and MDM2

4348 | Nov 29 2013

Nutlin-3 is a potent and selective Mdm2 (RING finger-dependent ubiquitin protein ligase for itself and p53) antagonist with IC50 of 90 nM; stabilizes p73 in p53-deficient cells. [Read the Full Post]

ABT 199 is designed to block the function of the protein Bcl 2

3355 | Nov 18 2013

ABT-199 (GDC-0199) is a Bcl-2-selective inhibitor with Ki of <0.01 nM, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. [Read the Full Post]

Nutlin3 inhibits the MDM2 p53 interaction and activates p5

4159 | Sep 26 2013

Nutlin-3 is a potent and selective Mdm2 (RING finger-dependent ubiquitin protein ligase for itself and p53) antagonist with IC50 of 90 nM; stabilizes p73 in p53-deficient cells. [Read the Full Post]

TW37 is a Bcl2 inhibitor that has been shown to inhibit the angiogenic potential of endothelial cells

2738 | Jun 24 2013

TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.29 μM, 1.11 μM and 0.26 μM, respectively. [Read the Full Post]

BCL-2 INHIBITORS HARMONIZING APOPTOSIS

3134 | Sep 18 2012

IMPROPER REGULATION OF BCL-2 PATHWAY IN TUMORS: Bcl-2 protein is abbreviated on basis of chromosomal translocations for the B-cell lymphoma 2 is a major apoptosis regulatory protein and is seen to be associated with it in the follicular lymphoma. Bcl-2 protein along with its other family members keeps a tight check on balancing the cell growth and apoptosis of the cells by keeping an interaction with each other. Any disturbance in the homeostatic balance between apoptosis and growth of cells usually results in the aberrations associated with various types of cancers. Hence using the Bcl-2 inhibitors to achieve Bcl-2 inhibition seems to be an attractive and promising strategy for the treatment of many types of cancers. Different Bcl-2 antagonists are designed on the basis of this strategy among them some are showing promising results at the pre-clinical and clinical levels. As the decrease in apoptosis is a key feature of the development of some sort of cancer, so it was not very surprising to find an association between the Bcl-2 gene, breast cancer, melanoma, prostate cancer and lung carcinomas along with the neurodegenerative problems like autoimmune disorders and schizophrenia. [Read the Full Post]

LENALIDOMIDE – AN ANTI-INFLAMMATORY DRUG

4104 | Sep 05 2012

LENALIDOMIDE: INTRODUCTION Tumor Necrosis factor (TNF) is a pro-inflammatory cytokine, the high levels of which signify inflammation in several disease conditions like autoimmune disorders (e.g. - rheumatoid arthritis, Crohn's disease and ankylosing spondylitis etc.), numerous cancers, skin diseases like psoriasis and refractory asthma. This is often the rationale that TNF-alpha inhibitors are given such importance in medical literature. Starting from natural compounds like curcumin, cannabis and green tea to xanthine derivatives, hallucination inducing compounds and also the best of all monoclonal antibodies, several TNF inhibitors are being studied in several and physiological conditions.As a result of its significance, TNF-alpha inhibition in cancers researchers got abundant attention. [Read the Full Post]

LENALIDOMIDE – AN INHIBITOR OF INFLAMMATION

5686 | Aug 29 2012

LENALIDOMIDE Tumor necrosis factor or TNF is amongst the pro-inflammatory cytokines, in varied forms of diseases associated with cancer, autoimmune diseases (like ankylosing spondylitis and Crohn's disease etc.) and skin diseases e: g refractory asthma and psoriasis high levels of TNF are being observed. From medical point of view due to this reality inhibitors of TNF-alpha are being given lots of value. Different inhibitors of tumor necrosis factor are being studied from numerous physiological and medical point of view these inhibitors include illusion inducing compounds, natural compounds comprising cannabis, curcumin and green tea whereas artificial include xanthine derivatives and most significantly monoclonal antibodies. Lots of emphasize is being placed on these inhibitors for cancer therapy. [Read the Full Post]

LENALIDOMIDE – AN ANTI-INFLAMMATORY DRUG

5082 | Jul 10 2012

LENALIDOMIDE: INTRODUCTION Tumor Necrosis factor (TNF) is a pro-inflammatory cytokine, the high levels of which signify inflammation in several disease conditions like autoimmune disorders (e.g. - rheumatoid arthritis, Crohn's disease and ankylosing spondylitis etc.), numerous cancers, skin diseases like psoriasis and refractory asthma. This is often the rationale that TNF inhibitors are given such importance in medical literature. Starting from natural compounds like curcumin, cannabis and green tea to xanthine derivatives, hallucination inducing compounds and also the best of all monoclonal antibodies, several TNF inhibitors are being studied in several and physiological conditions.As a result of its significance, TNF inhibition in cancers researchers got abundant attention. [Read the Full Post]

LENALIDOMIDE AND INFALAMATION

3571 | Apr 12 2012

ROLE OF TUMOR NECROSIS FACTOR Different types of molecules are there in the body for the purpose of communication between cells. Cytokines are one of such molecules that can induce a change such as growth, differentiation, movement or cell death. Tumor Necrosis factor abbreviated as TNF is one of such cytokines that plays a role in the development of inflammation at the site of disease or microbial attack. Its high levels are associated with the development of inflammation in many types of diseased conditions e.g., different types of cancers, autoimmune disorders (rheumatoid arthritis, ankylosing spondylitis and Crohn's disease etc.), and skin diseases e.g., refractory asthma and psoriasis. Due to its relatedness to many diseases, TNF-alpha is given importance in medical research as well as literature. [Read the Full Post]

OBATOCLAX AGAINST BCL-2 PATHWAYS IN CANCER

3750 | Mar 13 2012

Importance of Bcl-2 Pathway in Cancer: The pro-survival protein Bcl-2 and its related family members activate pro-survival pathways in cancer that are often associated with uncontrolled proliferation of cancer cells. Apart from this direct effect, stress pathways are also reported to be converging with Bcl-2 signaling pathways which makes the development of various Bcl-2 inhibitors an attractive approach to target cancer by inducing mitochondrial apoptotic pathways. [Read the Full Post]

ABT-263: THE BH-3 MIMETIC

5081 | Mar 13 2012

ABT-263 – Introduction: ABT-263 is a small molecule Bcl-2/Bcl-XL inhibitor marketed by Abbott laboratories under the generic name of Navitoclax. Similar in nature to ABT-737, also marketed by Abbott laboratories, ABT-263 inhibits the anti – intrinsic apoptotic pathway via the BH3 domain. Bcl-2/Bcl-XL bind with pro-apoptotic proteins (BID) with the single BH3 domain and thereby regulate the apoptotic process. However, it has been observed in numerous cancer types that Bcl-2 is over expressed which leads to the survival of cells that would normally be removed via apoptosis. ABT-263 Bcl-2 inhibitor have been demonstrated to be effective against small cell lung cancer xenographs, acute lymphoblastic leukemia and hematologic tumors. [Read the Full Post]

BCL-2 INHIBITOR – SMALL YET EFFECTIVE

4016 | Mar 13 2012

INHIBITION OF BCL-2 PROTEINS: Apoptosis is the natural system for the removal of cellular material from the body. This could be due to damage by invasion, age or injury. There are two mechanisms which regulate this process, the Intrinsic and the Extrinsic pathways. The extrinsic pathway is a cascade of signal originating from outside the cell via death receptors on the cellular membrane. The intrinsic pathway is initiated within the cell whereby pro-apoptotic proteins are released to activate the caspase cascade from the mitochondria. Part of the caspase cascade is the family of Bcl-2 proteins which regulate the process towards apoptosis or survival. Bcl-2 family consists of anti-apoptotic members such as Bcl-2, Mcl-1, Bcl-XL and Bcl2a1, other members are the pro-apoptotic proteins such as BAX, BAK, BAD, BIM, PUMA, BID, BIK, NOXA and BMF. In many forms of cancer it has been demonstrated that Bcl-2 is over expressed such as lung, breast, prostate, renal, ovarian and glioblastoma cancer, melanoma and leukemia are the highest report over expressers of Bcl-2. [Read the Full Post]

ABT-737: THE SMALL BCL-2 INHIBITOR

4422 | Mar 13 2012

BCL-2 INHIBITION AND ITS IMPLICATIONS: Bcl-2 family of proteins are a series of regulator proteins governing the pro-survival pathway. Characteristically Bcl-2 has been discovered to be over expressed in a variety of tumor types such small cell lung cancer, melanoma, prostate and breast cancer. The concept of targeted chemotherapy is to focus drug inhibition against a target that is over expressed in the cancer cell in comparison to normal cellular material; Bcl-2 is a clear target for inhibition. Over expression of this protein disrupts the regulation of the intrinsic apoptotic pathway, creating chemotherapeutic resistance. By inhibiting the sequestering of pro-apoptotic proteins by the Bcl-2 family (anti-apoptotic proteins) normal apoptotic processes can be utilized to trigger tumor cell death. Significantly there have been several now molecules introduced into the clinic in recent years which target Bcl-2 and have demonstrated clear benefits in chemotherapeutic action. One of these small molecules is ABT-737, while others are Navitoclax (ABT-263), Obatoclax (GX15-070) and TW-37. [Read the Full Post]

Survivin, the novel target for the treatment of fibrotic disease

5984 | Nov 06 2011

A fibroblast is a type of mesenchymal cells that synthesize the extracellular matrix(ECM) and collagen, and plays a key role in wound healing by differentiating into alpha-smooth muscle actin expressing myofibroblasts. At last, the normal wound repair progress following injury requires the elimination of myofibroblasts by apoptosis. However, in abnormal state, this excessive ECM can result in the progressive destruction of tissue architecture and lead to impaired organ function. Idiopathic pulmonary fibrosis (IPF) is a chronic, progressive form of lung disease caused by fibrosis of the lungs. [Read the Full Post]

The roles of p53 in hematopoietic stem cell rate

3711 | Nov 03 2011

At present, p53 is the star gene of the cancer studies, since more than half of cancer development and progression are reported to be related to the p53 mutation. p53 is a tumor suppressor protein, and is originally isolated as a cellular partner of simian virus 40(SV-40)-derived tumor antigens[1]. p53 has regulated several signaling pathways involved in the cell’s response to stress, and plays a role in apoptosis, genomic stability, senescence, inducing cell-cycle arrest and inhibition of angiogenesis. [Read the Full Post]

Chipuk, J. E., T. Moldoveanu, et al. (2010). "The BCL-2 family reunion." Mol Cell 37(3): 299-310.

3226 | Jul 9 2011

The newest review which give a overview of the BCL-2 family proteins including detail data of bcl-2 proteins, the signal transduction related to the bcl-2 and Pharmacological Regulation of the Bcl-2 Proteins [Read the Full Post]

Altieri, D. C. (2008). "Survivin, cancer networks and pathway-directed drug discovery." Nat Rev Cancer 8(1): 61-70.

3964 | Jun 11 2011

A fantastic review about survivin which was published in NATURE REVIEW CANCER. It concludes nearly all the important pathways which survivin is involved in. We can find wonderful pictures of pathways in this review [Read the Full Post]

Kruse, J. P. and W. Gu (2009). "Modes of p53 regulation." Cell 137(4): 609-622.

3855 | Jun 4 2011

This article which was published in CELL gives us a overview of p53 regulation. It give a introduction of the Classical Model of p53 regulation, Mdm2 Regulation, promoter-Specific Activation, p53 Transcriptional Activation. We can get detail information for p53 regulation from this article. [Read the Full Post]

He, L., X. He, et al. (2007). "A microRNA component of the p53 tumour suppressor network." Nature 447(7148): 1130-1134.

3474 | May 15 2011

The article which was published in NATURE uses miRNA to study p53 network. The article which was citied by 562 provides a new way to study target. [Read the Full Post]

Wheatley, S. P. and I. A. McNeish (2005). "Survivin: a protein with dual roles in mitosis and apoptosis." Int Rev Cytol 247: 35-88.

3849 | Apr 22 2011

a review give us a detail information of survivin’s role in mitosis and apoptosis.54 pages content include main information and data about survivin. [Read the Full Post]

Bouwmeester, T., A. Bauch, et al. (2004). "A physical and functional map of the human TNF-alpha/NF-kappa B signal transduction pathway." Nat Cell Biol 6(2): 97-105.

3681 | Apr 20 2011

How the TNF-α triggers the NF-KB ? [Read the Full Post]

Chen, G. and D. V. Goeddel (2002). "TNF-R1 signaling: a beautiful pathway." Science 296(5573): 1634-1635.

3919 | Mar 26 2011

This short article introduce TNF-R1 signaling pathway and the targets which are regulated by TNF-R1 signaling pathway. [Read the Full Post]

Lane, D. P. and T. R. Hupp (2003). "Drug discovery and p53." Drug Discov Today 8(8): 347-355.

3479 | Mar 19 2011

The article try to explain the relationship between p53 structure and drug discovery of p53. [Read the Full Post]

Coultas, L. and A. Strasser (2003). "The role of the Bcl-2 protein family in cancer." Semin Cancer Biol 13(2): 115-123.

2775 | Mar 11 2011

A review which gives a systematic description of the relationship between bcl-2 and cancer. [Read the Full Post]

Adams, J. M. and S. Cory (1998). "The Bcl-2 protein family: arbiters of cell survival." Science 281(5381): 1322-1326.

2589 | Mar 2 2011

A article about bcl-2 family proteins which is citied more than 3500.One of the most classical articles about bcl-2 family proteins which is published in science. [Read the Full Post]