Others

Development and Characterization of Thiolated Cyclodextrin-Based Nanoparticles for Topical Delivery of Minoxidil

149 | Feb 16 2024

This study demonstrates the potential of thiolated β-CD-based nanoparticles loaded with Minoxidil as an effective and non-irritating drug delivery system for treating scalp diseases topically. [Read the Full Post]

Comparing the Reliability of the Glomerular Filtration Rate Estimated with 99m-Technetium Diethylene-Triamine-Pentaacetate versus the Effective Renal Plasma Flow Obtained with 99m-Technetium Ethylene Dicysteine: A Prospective Observational Study

133 | Feb 16 2024

The study compared different methods of estimating glomerular filtration rate (GFR) in patients with varying renal function, concluding that in individuals with renal dysfunction, calculating GFR from effective renal plasma flow (ERPF) obtained via 99m-technetium ethylene dicysteine (99mTc-EC) was more accurate than other techniques, particularly in contrast to Gates' method using a gamma camera, which tended to overestimate GFR. [Read the Full Post]

Mitochondria-Targeted Lipid Nanoparticles Loaded with Rotenone as a New Approach for the Treatment of Oncological Diseases

99 | Feb 15 2024

This research demonstrates that modifying liposomes to carry a mitochondrial poison selectively targets and diminishes the mitochondrial function of specific cancer cells, showcasing promising advancements in targeted anticancer therapy. [Read the Full Post]

In silico design of novel bioactive molecules to treat breast cancer with chlorogenic acid derivatives: a computational and SAR approach

138 | Feb 15 2024

The comprehensive computational analysis conducted on chlorogenic acid derivatives strongly indicates their potential as powerful inhibitors for the treatment of breast cancer, outperforming certain standard drugs in docking scores and demonstrating promising interactions and favorable ADME profiles. [Read the Full Post]

Effects of Plant Regulators on the Seed Germination and Antioxidant Enzyme Activity of Cotton under Compound Salt Stress

101 | Feb 14 2024

Soaking treatments employing compound sodium nitrophenolate (CSN) and 24-epibrassinolide (EBR) effectively enhance cotton germination under high-salt conditions by bolstering antioxidant enzyme activities, showcasing promising potential to improve cotton's salt tolerance. [Read the Full Post]

Enantioselectivity in the enzymatic dehydration of malate and tartrate: Mirror image specificities of structurally similar dehydratases

110 | Feb 12 2024

The switch in substrate stereospecificity between fumarate hydratase and L-tartrate dehydratase may be attributed to subtle conformational adjustments and amino acid flexibility in the active site, potentially facilitated by the enantiomer superposition model. [Read the Full Post]

CD74-ROS1 L2026M mutant enhances autophagy through the MEK/ERK pathway to promote invasion, metastasis and crizotinib resistance in non-small cell lung cancer cells

103 | Feb 12 2024

The CD74-ROS1 L2026M mutation in NSCLC cells induces increased invasion, metastasis, and crizotinib resistance via the MEK/ERK pathway-mediated autophagy, highlighting MEK as a potential target for reversing these processes and enhancing treatment efficacy. [Read the Full Post]

Immunotactoid hepatopathy: A novel entity with histologically proven recurrence post liver transplantation

124 | Feb 12 2024

This case of hepatic immunotactoid deposition following liver transplantation, managed with a Daratumumab-based regimen targeting underlying plasma-cell dyscrasia, exhibited encouraging outcomes in reducing serum paraproteins, resolving ascites, and improving kidney function without inducing rejection, showing promise for treating this rare complication. [Read the Full Post]

Diallyl disulfide synergizes with melphalan to increase apoptosis and DNA damage through elevation of reactive oxygen species in multiple myeloma cells

103 | Feb 12 2024

The study underscores the potential of combining DADS, a compound found in garlic, with melphalan as a promising strategy for enhancing the efficacy of multiple myeloma treatment through induced apoptosis and increased DNA damage in MM cells. [Read the Full Post]

Heterostructured BiVO4/CoPi nanoarrays as high-efficiency photoanode and AuPt nanodendrites as nanozyme for sensitive sensing of miRNA 141

115 | Feb 11 2024

A highly sensitive BiVO4/CoPi heterostructured PEC biosensor utilizing AuPt nanodendrites as a nanozyme has been developed, exhibiting a wide linear range from 5 fM to 1 pM and an ultra-low detection limit of 0.17 fM for miRNA 141, offering valuable prospects for precise tumor biomarker analysis in clinical applications. [Read the Full Post]

Targeting lncRNA NEAT1 Hampers Alzheimer's Disease Progression

71 | Feb 10 2024

Knocking down lnc-NEAT1 in Alzheimer's disease models demonstrated reduced neuronal damage, inflammation, and oxidative stress through the mediation of microRNA-193a and activation of protective neuronal pathways. [Read the Full Post]

Targeting of HBP1/TIMP3 axis as a novel strategy against breast cancer

91 | Feb 10 2024

The study elucidates the pivotal role of the HBP1/TIMP3 axis in suppressing breast cancer tumorigenesis and progression while enhancing sensitivity to radiation and hormone therapies, unveiling promising prospects for novel treatment modalities and improved prognostic approaches. [Read the Full Post]

Engineering the cofactor binding site of 7α-hydroxysteroid dehydrogenase for improvement of catalytic activity, thermostability, and alteration of substrate preference

62 | Feb 09 2024

The targeted mutations at the cofactor binding site of Hydroxysteroid dehydrogenase (HSDH) St-2-2 not only significantly enhanced catalytic activity, altered substrate preference, and increased thermostability but also provided valuable insights into modifying enzymatic properties, offering potential applications in disease treatment through engineered bacteria. [Read the Full Post]

Establishment of a Rapid and Effective Agrobacterium-Mediated Genetic Transformation System of Oxalis triangularis 'Purpurea'

53 | Feb 09 2024

Your study's refined transformation protocol for Oxalis triangularis 'Purpurea' opens new avenues for comprehensive gene function studies and enhances the potential for genetic manipulation in ornamental plants. [Read the Full Post]

Preparation and Characterization of Modified ZrO2/SiO2/Silicone-Modified Acrylic Emulsion Superhydrophobic Coating

88 | Feb 08 2024

Using an innovative spraying technique and a meticulously selected combination of γ-Methacryloyloxypropyltrimethoxysilane-modified ZrO2/SiO2/silicone-modified acrylic emulsion, our superhydrophobic coating showcased exceptional properties, including high contact angle, low rolling angle, wear resistance, and self-cleaning efficiency, making it ideal for critical industrial applications. [Read the Full Post]

Selective Shielding of the (002) Plane Enabling Vertically Oriented Zinc Plating for Dendrite-Free Zinc Anode

77 | Feb 07 2024

The innovative use of disodium lauryl phosphate as an electrolyte additive enables controlled, dendrite-free Zn plating with preferential growth on the (100) crystal plane, unlocking exceptional stability and high-performance capabilities in aqueous Zn-ion batteries. [Read the Full Post]

Inhibition of protein tyrosine phosphatases unmasks vasoconstriction and potentiates calcium signaling in rat aorta smooth muscle cells in response to an agonist of 5-HT2B receptors BW723C86

88 | Feb 07 2024

Oxidative stress-induced inhibition of protein tyrosine phosphatases unmasks the vasoconstrictive potential of serotonin 5-HT2B receptors, elucidating the intricate interplay between oxidative stress, receptor activity, and vascular dysfunction. [Read the Full Post]

Identification and application of a novel deoxynivalenol-degrading enzyme from Youhaiella tibetensis

67 | Feb 06 2024

YoDDH, an enzyme from Youhaiella tibetensis, exhibits potent DON-degrading capabilities under optimal conditions, making it a promising solution for combating DON contamination in food and feed industries. [Read the Full Post]

Detection of Reverse Transcriptase LAMP-Amplified Nucleic Acid from Oropharyngeal Viral Swab Samples Using Biotinylated DNA Probes through a Lateral Flow Assay

100 | Feb 06 2024

This study presents a rapid, sensitive, and specific nucleic acid testing-point of care technique using crude throat swab samples, RT-LAMP-LFA readouts with biotinylated DNA probes, and digital semi-quantification, showcasing its potential as a versatile biosensor platform for efficient pathogen detection without the need for extensive sample processing. [Read the Full Post]

Consuming artificial sweeteners may alter the structure and function of duodenal microbial communities

89 | Feb 06 2024

Consuming non-sugar sweeteners appears to significantly alter both the composition and metabolic function of the microbiome in the metabolically active small bowel and stool, demonstrating distinct effects on different regions of the gut. [Read the Full Post]

Local perfusion of capillaries reveals disrupted beta-amyloid homeostasis at the blood-brain barrier in Tg2576 murine Alzheimer's model

137 | Feb 04 2024

This study reveals disrupted tight junction integrity, impaired transporter functionality, and decreased Aβ-receptor binding at the blood-brain barrier in Alzheimer's disease, prompting potential therapeutic strategies targeting these specific alterations. [Read the Full Post]

Adelmidrol ameliorates liver ischemia-reperfusion injury through activating Nrf2 signaling pathway

143 | Feb 04 2024

Adelmidrol demonstrates promise in ameliorating liver ischemia/reperfusion injury by activating the Nrf2 signaling pathway, as evidenced by its reduction of inflammatory response, oxidative stress, and apoptosis in both mouse liver I/R injury models and AML12 cell hypoxia-reoxygenation experiments. [Read the Full Post]

Functional groups matter: metabolomics analysis of Escherichia coli exposed to trans-cinnamic acid and its derivatives unveils common and unique targets

73 | Feb 04 2024

This study employing a metabolomics approach revealed distinctive metabolic responses in Escherichia coli to trans-cinnamic acid, p-coumaric acid, and ferulic acid, indicating diverse impacts on bacterial metabolism and cellular processes. [Read the Full Post]

Highly Potent Peptide Therapeutics To Prevent Protein Aggregation in Huntington's Disease

108 | Feb 03 2024

Peptide-based therapies exhibiting inhibition of mHtt fibril formation present a promising avenue for halting the progression of Huntington's disease by targeting the misfolded proteins associated with the condition. [Read the Full Post]

Characterization of a (p)ppApp Synthetase Belonging to a New Family of Poly

75 | Feb 03 2024

This study characterizes the MuF-RelA_SpoT polymorphic toxin in Streptococcus pneumoniae SPNA45, revealing its (p)ppApp synthetase activity and the downstream genes encoding immunity proteins, while proposing a distinguishing signature for (p)ppApp synthetases. [Read the Full Post]

Overcoming multi drug resistance mediated by ABC transporters by a novel acetogenin- annonacin from Annona muricata L

145 | Feb 03 2024

The study's findings suggest that annonacin from Annona muricata has the potential to counteract drug resistance in colorectal cancer cells by inhibiting P-glycoprotein-mediated drug efflux, highlighting a promising avenue for future therapeutic developments. [Read the Full Post]

Pluronic F-127 Enhances the Antifungal Activity of Fluconazole against Resistant Candida Strains

126 | Feb 02 2024

The study investigates how Pluronic F-127 (PLX) formulations loaded with fluconazole (FLU) potentially increase susceptibility in drug-resistant Candida strains, revealing a significant inhibitory effect on yeast growth, particularly at concentrations of 5.0% and 10.0% w/v of PLX, while detecting upregulation of CDR1/CDR2 genes, indicative of drug efflux as the primary resistance mechanism. [Read the Full Post]

The Equilibria of Triterpene Sapogenins-Phosphatidylcholine in Monolayers at the Air/Water Interface

93 | Feb 02 2024

The study investigating the interaction of asiatic acid and oleanolic acid with phosphatidylcholine (DPPC) in monolayers using the Langmuir method with Brewster angle microscopy revealed stable 1:1 complexes, shedding light on their potential applications and phase transitions within these systems. [Read the Full Post]

Antibody-decorated chitosan-iodoacetamide-coated nanocarriers for the potential delivery of doxorubicin to breast cancer cells

69 | Feb 01 2024

Trastuzumab-conjugated chitosan iodoacetamide-coated nanocarriers loaded with doxorubicin demonstrate promising potential as a targeted and effective delivery system for HER-2-positive breast cancer, exhibiting superior antitumor activity and high cellular accumulation compared to unconjugated nanocarriers and drug solutions. [Read the Full Post]

Role of MAPKs in TGF-β1-induced maturation and mineralization in human osteoblast-like cells

99 | Feb 01 2024

"TGF-β1 induces mineralization in human osteoblast-like MG63 cells primarily through the activation of JNK within the MAPK signaling pathway." [Read the Full Post]

Unilateral hypoglossal nerve palsy following orthognathic surgery: A case report and literature review

69 | Feb 01 2024

Unilateral hypoglossal nerve palsy following orthognathic surgery in a 56-year-old woman highlighted potential triggers like intubation, anesthesia-related factors, and viral infection, emphasizing the importance of clinicians' vigilance in recognizing and managing such postoperative complications. [Read the Full Post]

Apparent and true digestibility of macro and micro nutrients in adult maintenance dog foods containing either a majority of animal or vegetable proteins1

70 | Jan 31 2024

This study investigates mineral digestibility in canines fed different diets, revealing significant differences in apparent and true digestibility values and suggesting a need for refined models to comprehensively understand nutrient absorption in dogs. [Read the Full Post]

Brain uptake pharmacokinetics of albiglutide, dulaglutide, tirzepatide, and DA5-CH in the search for new treatments of Alzheimer's and Parkinson's diseases

76 | Jan 30 2024

The distinction between fast and slow blood-brain barrier transport mechanisms for peptide incretin receptor agonists underscores their potential as rapid-acting therapeutics for Alzheimer's and Parkinson's diseases. [Read the Full Post]

Assessing safety concerns of interstitial lung disease associated with antibody-drug conjugates: a real-world pharmacovigilance evaluation of the FDA adverse event reporting system

415 | Jan 29 2024

The identification of significant safety signals for interstitial lung disease associated with several FDA-approved antibody-drug conjugates underscores the critical need for heightened clinician awareness and early patient monitoring, prompting further research and potential adjustments in clinical practice guidelines. [Read the Full Post]

Axillary Nodal Response to Neoadjuvant T-DM1 Combined with Pertuzumab in a Prospective Phase II Multi-Institution Clinical Trial

362 | Jan 29 2024

In HER2-positive breast cancer patients undergoing neoadjuvant dual HER2-targeted therapy, achieving a pathologic complete response or residual cancer burden I in the breast strongly correlates with a high probability of having no residual disease in the axillary lymph nodes, suggesting a potential consideration for omitting axillary surgical staging in future trials for those demonstrating these favorable responses. [Read the Full Post]

18F-FDG and 18F-AIF-NOTA-Octreotide PET/CT Confirmed a Rare Case of Cutaneous Merkel Cell Carcinoma With a Solitary Local Nodal Metastasis

79 | Jan 29 2024

A 56-year-old man with cutaneous Merkel cell carcinoma and nodal metastasis underwent radical treatment following a specialized 18F-AIF-NOTA-octreotide PET/CT confirmation of a solitary somatostatin receptor-positive left inguinal mass, guiding a more targeted therapeutic approach. [Read the Full Post]

Recurrent bilateral idiopathic chylothorax: a therapeutic challenge

92 | Jan 29 2024

The multidisciplinary management involving total parenteral nutrition, octreotide, thoracic duct embolisation, and ultimately thoracic duct ligation with talc pleurodesis proved effective in resolving the persistent bilateral idiopathic chylothorax, showcasing the intricate yet successful approach to this challenging condition. [Read the Full Post]

Management of chronic HBV-HDV patients chronic HBV-HDV infection: A review on new management options

85 | Jan 29 2024

Despite its discovery almost 50 years ago by Mario Rizzetto, Hepatitis D remains a challenge due to limited progress in diagnosis and treatment, with the recent approval of bulevirtide marking a significant but incomplete advancement in addressing this chronic viral hepatitis. [Read the Full Post]

Response-guided neoadjuvant sacituzumab govitecan for localized triple negative breast cancer: results from the NeoSTAR trial

130 | Jan 28 2024

The neoadjuvant trial of sacituzumab govitecan in early-stage triple-negative breast cancer demonstrated a 30% pathological complete response rate with manageable adverse events, emphasizing the potential of SG as a single agent and the need for further research into optimal treatment duration and combination strategies. [Read the Full Post]

Design and Discovery of MRTX0902, a Potent, Selective, Brain-Penetrant, and Orally Bioavailable Inhibitor of the SOS1:KRAS Protein-Protein Interaction

96 | Jan 27 2024

The discovery of MRTX0902, a potent SOS1 binder disrupting the SOS1:KRASG12C interaction and its synergistic effect with MRTX849, targeting GDP-loaded KRASG12C, presents a promising combined strategy for enhanced antitumor activity in KRAS-driven cancers. [Read the Full Post]

Discovery and characterization of a selective IKZF2 glue degrader for cancer immunotherapy

90 | Jan 27 2024

NVP-DKY709, a selective molecular glue degrader of IKZF2, shows promise as an immune-enhancing agent for cancer immunotherapy by specifically targeting regulatory T cells and T-effector cells, potentially altering tumor growth and improving immune responses in preclinical models. [Read the Full Post]

A novel class of TMPRSS2 inhibitors potently block SARS-CoV-2 and MERS-CoV viral entry and protect human epithelial lung cells

99 | Jan 26 2024

The discovery of MM3122, a covalent ketobenzothiazole inhibitor with potent activity against TMPRSS2 and various coronaviruses, showcasing exceptional efficacy, metabolic stability, and favorable pharmacokinetics in mice, stands as a promising breakthrough for COVID-19 treatment. [Read the Full Post]

Structural and energetic insights into the selective inhibition of PKMYT1 against WEE1

91 | Jan 26 2024

This comprehensive study utilizing molecular simulations and free energy calculations unveils the molecular basis behind RP-6306's binding selectivity towards PKMYT1 over WEE1, offering critical insights for the design of more effective and specific inhibitors in cancer therapy. [Read the Full Post]

Combinatorial design of ionizable lipid nanoparticles for muscle-selective mRNA delivery with minimized off-target effects

74 | Jan 24 2024

The discovery of iso-A11B5C1 as a muscle-specific ionizable lipid for mRNA delivery, challenging traditional immune cell transfection paradigms, redefines the criteria for effective mRNA vaccines and expands the horizon for tissue-targeted therapies. [Read the Full Post]

Chemical Inhibition of ENL/AF9 YEATS Domains in Acute Leukemia

77 | Jan 23 2024

The research underscores the potential of inhibiting the ENL YEATS domain with SR-0813 as a targeted approach to disrupt the pathogenic function of ENL in acute leukemia while providing the first thoroughly characterized chemical probe for this domain. [Read the Full Post]

Trastuzumab Deruxtecan in Previously Treated Patients With HER2-Positive Metastatic Breast Cancer: Updated Survival Results From a Phase 2 Trial (DESTINY-Breast01)

218 | Jan 23 2024

The updated analysis of the DESTINY-Breast01 trial underscores the sustained efficacy and generally consistent safety profile of trastuzumab deruxtecan in heavily pretreated patients with HER2-positive metastatic breast cancer, revealing a 62.0% objective response rate, a median overall survival of 29.1 months, and notable treatment-emergent adverse events such as drug-related interstitial lung disease/pneumonitis in 15.8% of patients. [Read the Full Post]

Tetrahydrocannabinol (THC)-containing e-cigarette, or vaping, product use behaviors among adults after the onset of the 2019 outbreak of e-cigarette, or vaping, product use-associated lung injury (EVALI)

87 | Jan 18 2024

This study reveals continued significant THC-EVP usage post-EVALI, emphasizing the need for ongoing monitoring and education to mitigate potential health risks associated with these products. [Read the Full Post]

Management of erythropoietic protoporphyria with cholestatic liver disease: A case report

115 | Jan 17 2024

Managing the complexities of Erythropoietic Protoporphyria (EPP), exacerbated by progressive cholestatic liver disease and further complicated by the coexistence of factor VII deficiency, necessitated a multifaceted approach culminating in successful allogeneic hematopoietic stem cell transplantation in this documented 3-year follow-up case. [Read the Full Post]

Reversible translocation of acyl-CoA:cholesterol acyltransferase (ACAT) between the endoplasmic reticulum and vesicular structures

139 | Jan 16 2024

The dynamic translocation of ACAT from the endoplasmic reticulum to vesicular structures, triggered by diverse stimuli and inhibitors while maintaining its enzymatic activity, underscores the intricate regulatory mechanisms governing lipid metabolism in response to cellular cues. [Read the Full Post]

Effects of a novel direct-fed microbial on growth performance, carcass characteristics, nutrient digestibility, and ruminal morphology of beef feedlot steers

124 | Jan 16 2024

The inclusion of L. salivarius L28 and monensin in finishing diets for steers did not significantly impact growth performance or ruminal fermentation but led to reduced feed intake and altered carcass quality, while also showing potential to positively influence ruminal morphology. [Read the Full Post]

pH-dependent structural transitions in cationic ionizable lipid mesophases are critical for lipid nanoparticle function

78 | Jan 14 2024

The study investigates the pH-dependent behavior of distinct ionizable lipids within lipid nanoparticles used for mRNA delivery, revealing structural transitions in CIL/cholesterol bulk phases that correlate with differences in mRNA delivery efficacy, shedding light on their varying effectiveness in gene expression. [Read the Full Post]

The Combination of Methioninase and Ethionine Exploits Methionine Addiction to Selectively Eradicate Osteosarcoma Cells and Not Normal Cells and Synergistically Down-regulates the Expression of C-MYC

114 | Jan 13 2024

The study demonstrates the synergistic potential of combining recombinant methioninase (rMETase) and ethionine to selectively eradicate osteosarcoma cells while down-regulating c-MYC expression, highlighting a promising avenue for future clinical strategies against this form of cancer. [Read the Full Post]

Loss of ORP3 induces aneuploidy and promotes bladder cancer cell invasion through deregulated microtubule and actin dynamics

65 | Jan 13 2024

The study demonstrates that ORP3, highly expressed in healthy bladder epithelium but downregulated in invasive bladder cancer, serves as a crucial tumor suppressor by influencing aneuploidy, genomic stability, and metastatic characteristics through its interactions with cytoskeletal components, elucidating a pivotal molecular link between aneuploidy and the invasive properties of metastatic cells. [Read the Full Post]

Granule Dendrobii suppresses chronic atrophic gastritis induced by N-methyl-N'-nitro-N-nitrosoguanidine by modulating the gastrointestinal bacteria in rats

82 | Jan 12 2024

Granule Dendrobii (GD) demonstrated efficacy in ameliorating chronic atrophic gastritis (CAG) in rats by improving gastric mucosal pathology and modulating the abundance of specific bacteria like Lactobacillus and Turicibacter, suggesting its potential as a treatment and offering new insights into CAG-associated microbiota. [Read the Full Post]

Active natural compounds perturb the melanoma risk-gene network

376 | Jan 07 2024

The study ingeniously employs network modeling of melanoma-associated genes, revealing crucial pathways and potential therapeutic targets while showcasing the predictive potential of this model in evaluating the efficacy of anti-melanoma phytochemicals. [Read the Full Post]

TH-302-loaded nanodrug reshapes the hypoxic tumour microenvironment and enhances PD-1 blockade efficacy in gastric cancer

79 | Jan 03 2024

TH-302 nanoparticles show promise in alleviating the hypoxic tumor microenvironment and enhancing the efficacy of PD-1 blockade, presenting a safe and effective combined immunotherapy approach for gastric cancer treatment. [Read the Full Post]

GSNOR deficiency attenuates MPTP-induced neurotoxicity and autophagy by facilitating CDK5 S-nitrosation in a mouse model of Parkinson's disease

68 | Jan 01 2024

The study revealed that increased S-nitrosoglutathione reductase (GSNOR) expression in an MPTP-induced Parkinson's disease mouse model heightened CDK5-mediated autophagy and neurotoxicity, while GSNOR deficiency or inhibition alleviated PD-like pathology by inhibiting CDK5 activity through increased S-nitrosation at Cys83. [Read the Full Post]

Prenatal Nicotine Exposure Raises Male Blood Pressure via FTO-Mediated NOX2/ROS Signaling

98 | Dec 30 2023

Nicotine exposure during pregnancy appears to increase the risk of hypertension in male offspring by influencing the epigenetic regulation of vascular NOX2 via the m6A demethylase FTO, revealing a potential target for preventing developmental hypertension programming. [Read the Full Post]

Treating Autoimmune Diseases With LANCL2 Therapeutics: A Novel Immunoregulatory Mechanism for Patients With Ulcerative Colitis and Crohn's Disease

88 | Dec 29 2023

Activation of LANCL2 through therapeutics like Omilancor shows promise in addressing autoimmune diseases by enhancing regulatory T cell responses and suppressing inflammatory reactions in the gut, presenting a potential breakthrough in treating conditions like ulcerative colitis and Crohn's disease. [Read the Full Post]

Circ_0020014 mediates CTSB expression and participates in IL-1β-prompted chondrocyte injury via interacting with miR-24-3p

79 | Dec 26 2023

This study elucidates the involvement of circ_0020014 in osteoarthritis by revealing its role as a regulator in IL-1β-induced chondrocyte injury through the circ_0020014/miR-24-3p/CTSB axis. [Read the Full Post]

Degradation of Cyclin-Dependent Kinase 9/Cyclin T1 by Optimized Microtubule-Associated Protein 1 Light Chain 3 Beta-Recruiting Coumarin Analogs

291 | Dec 24 2023

Researchers systematically optimized coumarin analogs linked with the CDK9 inhibitor SNS-032, potentially enabling simultaneous binding to CDK9 and LC3B, initiating selective autophagic degradation and demonstrating potential for treating diseases associated with intracellular pathogenic proteins. [Read the Full Post]

Advances in the treatment of metastatic prostate cancer

138 | Dec 20 2023

The unprecedented therapeutic advances in metastatic prostate cancer, including recent approvals of triplet therapy regimens and novel agents, pose challenges in treatment selection and sequencing, emphasizing the need for a multidisciplinary approach informed by ongoing clinical trials and personalized medicine principles. [Read the Full Post]

Thioredoxin domain-containing protein 12 (TXNDC12) in red spotted grouper (Epinephelus akaara): Molecular characteristics, disulfide reductase activities, and immune responses

93 | Dec 18 2023

The study on the thioredoxin domain-containing protein 12 (EaTXNDC12) in red spotted grouper reveals its crucial role in cellular redox homeostasis, immune regulation, and antioxidant activities, providing valuable insights into the molecular mechanisms governing these processes in fish species. [Read the Full Post]

An overview of the past decade of bufalin in the treatment of refractory and drug-resistant cancers: current status, challenges, and future perspectives

158 | Dec 15 2023

The research on bufalin, a compound found in toad venom, demonstrates significant potential in overcoming drug resistance in cancer cells through its diverse mechanisms of action, chemo-sensitizing properties, derivative development, and proactive consideration of obstacles, emphasizing the need for further in-depth studies and clinical trials. [Read the Full Post]

RAGE inhibitor TTP488 (Azeliragon) suppresses metastasis in triple-negative breast cancer

74 | Dec 12 2023

The study demonstrates that the RAGE inhibitor TTP488 (Azeliragon) significantly impairs metastasis of triple-negative breast cancer by disrupting key metastatic pathways, suggesting its potential as a targeted therapy in clinical trials. [Read the Full Post]

Cyclin-dependent kinase 6 (CDK6) as a potent regulator of the ovarian primordial-to-primary follicle transition

163 | Dec 11 2023

The study reveals that CDK6 inhibition using BSJ disrupts the primordial-to-primary follicle transition, emphasizing the crucial role of precise cell cycle regulation in ovarian follicle development and suggesting potential implications for fertility-related interventions. [Read the Full Post]

Retinoic acid delays murine palatal shelf elevation by inhibiting Wnt5a-mediated noncanonical Wnt signaling and downstream Cdc-42/F-actin remodeling in mesenchymal cells

243 | Dec 10 2023

This study elucidates the mechanism by which retinoic acid disrupts palate development, causing cleft palate in mice, revealing the crucial role of Wnt5a-mediated noncanonical Wnt signaling downstream of Rho GTPase Cdc42 in regulating cytoskeletal remodeling and cell migration during the process. [Read the Full Post]

Optimization of a Glucagon-Like Peptide 1 Receptor Antagonist Antibody for Treatment of Hyperinsulinism

53 | Dec 02 2023

A highly potent GLP-1R antagonist antibody, TB-222-023, derived from a combinatorial variant antibody library, effectively decreases insulin secretion in hyperinsulinism mouse models and human islets, offering a promising therapeutic strategy for congenital hyperinsulinism. [Read the Full Post]

Targeting SWI/SNF ATPases in H3.3K27M diffuse intrinsic pontine gliomas

71 | Dec 02 2023

H3K27M mutations in diffuse midline gliomas reprogram the SWI/SNF complex, leading to upregulated SMARCA4 levels, and therapeutic targeting of SMARCA4, SMARCA2, and PBRM1 using AU-15330 selectively induces cytotoxicity in H3.3K27M-mutant cells, suggesting a potent and specific therapeutic strategy for these deadly childhood brain tumors. [Read the Full Post]

The Subtilisin-Like Protease Furin Regulates Hemin-Dependent Ectodomain Shedding of Glycoprotein VI

59 | Nov 28 2023

This study reveals a previously unrecognized mechanism where hemin induces shedding of the GPVI ectodomain through furin-mediated pathways, enhancing platelet activation and thrombus formation, thus providing crucial insights into hemin-induced thrombotic disorders. [Read the Full Post]

Microglia trigger the structural plasticity of GABAergic neurons in the hippocampal CA1 region of a lipopolysaccharide-induced neuroinflammation model

164 | Nov 26 2023

The study demonstrates that LPS-induced microglial activation in the hippocampal CA1 region leads to cognitive impairment through the upregulation of GABAergic inhibitory synapses, and this effect can be reversed by blocking GABA receptor activity or depleting microglia, highlighting the critical role of neuroinflammatory responses and synaptic plasticity in cognitive dysfunction. [Read the Full Post]

Promoting TFEB nuclear localization with curcumin analog C1 attenuates sensory hair cell injury and delays age-related hearing loss in C57BL/6 mice

55 | Nov 25 2023

The study reveals that the curcumin analog C1 promotes nuclear localization of TFEB, restores impaired autophagy, alleviates hair cell injury, and delays age-related hearing loss, highlighting TFEB as a promising therapeutic target for AHL. [Read the Full Post]

Retinal transcriptome profiling identifies novel candidate genes associated with visual impairment in a mouse model of multiple sclerosis

45 | Nov 24 2023

This study identifies immune-related gene expression changes in the retinas of mice with experimental autoimmune encephalomyelitis (EAE), providing molecular insights into the visual impairments observed in EAE and implicating potential targets for understanding and treating similar conditions in multiple sclerosis. [Read the Full Post]

A nanocellulose molecularly imprinted membrane: Preparation, characterization and application in targeted separation of taxane 10-deacetylbaccatin III

51 | Nov 23 2023

The study introduces a nanocellulose-based molecular imprinted membrane (NC-MIM) with high specificity and stability, enabling the efficient and selective separation of 10-deacetylbaccatin III (10-DAB), a crucial phytochemical in paclitaxel synthesis, offering a promising and green approach for natural medicine applications. [Read the Full Post]

Endotyping of IgE-Mediated Polyethylene Glycol and/or Polysorbate 80 Allergy

82 | Nov 16 2023

The study found that patients with allergies to polyethylene glycol (PEG) and polysorbate 80 (PS80) can safely receive the PEGylated lipid nanoparticle (LNP) COVID-19 vaccine BNT162b2, with cross-reactivity between PEG and PS80 being mediated by IgE recognizing short PEG motifs. [Read the Full Post]

Homogentisate 1,2-dioxygenase (HGD) gene variants in young Egyptian patients with alkaptonuria

57 | Nov 11 2023

In this study, the clinical and genetic spectrum of Alkaptonuria in Egypt was characterized, revealing four pathogenic missense variants, including a novel variant, in the HGD gene, and emphasizing the importance of early genetic confirmation for timely intervention with nitisinone therapy to prevent serious complications. [Read the Full Post]

The therapeutic effect of the BRD4-degrading PROTAC A1874 in human colon cancer cells

0 | Nov 10 2023

A1874, a novel BRD4-degrading PROTAC, demonstrates potent anti-colon cancer activity through both BRD4-dependent and -independent mechanisms, inhibiting cell growth, inducing apoptosis, and showing efficacy in in vivo models. [Read the Full Post]

Flavonoid compound from Agrimonia pilosa Ledeb improves adipose insulin resistance by alleviating oxidative stress and inflammation

62 | Nov 09 2023

The study demonstrates that the flavonoid component (FC) extracted from Agrimonia pilosa Ledeb improves insulin resistance and glucose metabolism by regulating insulin signaling pathways, reducing oxidative stress, and attenuating inflammation, suggesting its potential as a therapeutic agent for type 2 diabetes. [Read the Full Post]

EAT-2 attenuates C. elegans development via metabolic remodeling in a chemically defined food environment

49 | Nov 06 2023

This study revealed that specific fatty acids, including C17ISO, palmitic acid, and stearic acid, as well as metabolites such as S-adenosylmethionine and methionine sulfoxide, can counteract the developmental attenuation caused by tmc-1 and eat-2 mutations in C. elegans by promoting metabolic remodeling and adaptation to the nutritional environment. [Read the Full Post]

Single-Nucleotide Polymorphism of the MLX Gene Is Associated With Takayasu Arteritis

103 | Nov 06 2023

The MLX-Q139R mutation in the MLX gene plays a crucial role in the pathogenesis of Takayasu arteritis by promoting inflammasome formation, increased oxidative stress, and impaired autophagy. [Read the Full Post]

The regeneration-responsive element careg monitors activation of Müller glia after MNU-induced damage of photoreceptors in the zebrafish retina

21 | Oct 31 2023

Zebrafish can regenerate damaged photoreceptors, and a study identified that the careg reporter gene marks activated Müller glia cells involved in regeneration, revealing distinct molecular signatures and the involvement of TOR signaling in the regenerative process. [Read the Full Post]

Digeda-4 decoction and its disassembled prescriptions improve dyslipidemia and apoptosis by regulating AMPK/SIRT1 pathway on tyloxapol-induced nonalcoholic fatty liver disease in mice

80 | Oct 28 2023

This study demonstrated that DGD-4, a Mongolian herbal formulation, showed protective effects against NAFLD by improving dyslipidemia, inhibiting apoptosis, and regulating the AMPK/SIRT1 pathway. [Read the Full Post]

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

367 | 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]

Lipid Peroxidation and Antioxidative Capacity Are Unaltered in Transitional Breast Milk Exposed to Light from Women Giving Birth to Preterm Infants before 32 Weeks of Gestation

142 | Oct 23 2023

The study found that light exposure of expressed transitional breast milk did not significantly affect lipid peroxidation or the levels of malondialdehyde, 4-hydroxynonenal, or total antioxidant capacity. [Read the Full Post]

Dehydrocorydaline Protects Against Sepsis-Induced Myocardial Injury Through Modulating the TRAF6/NF-κB Pathway

149 | Oct 23 2023

Dehydrocorydaline (Deh) treatment effectively mitigates sepsis-induced myocardial injury by inhibiting the TRAF6/NF-κB pathway, demonstrating its potential as a therapeutic intervention. [Read the Full Post]

Mapping of Tilapia Lake Virus entry pathways with inhibitors reveals dependence on dynamin activity and cholesterol but not endosomal acidification

60 | Oct 20 2023

Tilapia Lake Virus (TiLV) enters tilapia cells through a dynamin-mediated endocytic pathway that depends on cholesterol and the cytoskeleton, but is independent of clathrin and pH. [Read the Full Post]

Arum palaestinum delays hepatocellular carcinoma proliferation through the PI3K-AKT-mTOR signaling pathway and exhibits anticoagulant effects with antimicrobial properties

106 | Oct 18 2023

The study revealed that the aqueous extract of Arum palaestinum Boiss (AP) flowers exhibited potent antimicrobial activity, anticoagulant properties, and potential as an anticancer agent by impacting cell cycle, HCC biomarkers, and the PI3K-AKT-mTOR signaling pathway. [Read the Full Post]

Knockdown screening of chromatin binding and regulatory proteins in zebrafish identified Suz12b as a regulator of tfpia and an antithrombotic drug target

289 | Oct 15 2023

This study identified novel epigenetic regulators of the tfpia gene and demonstrated the potential of UNC6852 as an antithrombotic drug by enhancing tfpia mRNA levels and prolonging the time to occlude the caudal vessel after laser injury in zebrafish larvae and adults. [Read the Full Post]

Docking-Based Evidence for the Potential of ImmunoDefender: A Novel Formulated Essential Oil Blend Incorporating Synergistic Antiviral Bioactive Compounds as Promising Mpro Inhibitors against SARS-CoV-2

78 | Oct 09 2023

In silico studies demonstrated that certain components of the "ImmunoDefender" antiviral compound, derived from essential oils, showed strong affinity and binding energies to the main protease of SARS-CoV-2, suggesting their potential in inhibiting the virus's pathogenesis and transmission, but further research is needed to confirm these findings. [Read the Full Post]

Antibiotic Susceptibility Profile of Bacteria Causing Aerobic Vaginitis in Women in Iraq

193 | Oct 06 2023

The study revealed high rates of antimicrobial resistance among bacterial isolates from women with aerobic vaginitis, with Gram-positive bacteria showing resistance to penicillins and cephalosporins and Gram-negative bacteria displaying resistance to multiple antibiotic classes. [Read the Full Post]

The ensured proliferative capacity of myoblast in serum-reduced conditions with Methyl-β-cyclodextrin

49 | Oct 04 2023

This study demonstrates that Methyl-β-cyclodextrin (MβCD) can effectively inhibit the differentiation of myoblasts into myotubes and maintain their proliferative capacity in a serum-reduced medium, providing valuable insights for the large-scale production of muscle fibers for cultured meat. [Read the Full Post]

NR4A1 Aggravates Myocardial Ischaemia-Reperfusion Injury by Inhibiting OPA1-Mediated Mitochondrial Fusion

55 | Oct 04 2023

NR4A1 inhibits OPA1 expression, disrupts mitochondrial dynamics, and activates the STING and NF-κB pathways, exacerbating myocardial ischemia-reperfusion injury (IR) and leading to mitochondrial damage, increased apoptosis, and inflammatory reactions in cardiomyocytes. [Read the Full Post]

5-Fluorouracil-Loaded PLGA Nanoparticles: Formulation, Physicochemical Characterisation, and In Vitro Anti-Cancer Activity

52 | Oct 03 2023

The study aimed to develop polymeric nanoparticles loaded with 5-fluorouracil (FU) using the interfacial deposition method, resulting in spherical and homogenous nanoparticles with a nanometric size of 200 nm suitable for intravenous delivery, and showed improved cytotoxic effect compared to the marketed formulation Fluracil. [Read the Full Post]

C5aR1 is a master regulator in Colorectal Tumorigenesis via Immune modulation

65 | Oct 01 2023

Activation of the complement system, specifically C5a/C5aR1 signaling, plays a crucial role in colorectal tumorigenesis by recruiting myeloid-derived suppressor cells, impairing CD8+ T cell function, and modulating cytokine and chemokine production. [Read the Full Post]

α-Synuclein induces Th17 differentiation and impairs the function and stability of Tregs by promoting RORC transcription in Parkinson's disease

72 | Sep 28 2023

Alpha-synuclein promotes the imbalance between regulatory T cells and Th17 cells in Parkinson's disease by upregulating the transcription of retinoid-related orphan nuclear receptor γt, leading to impaired Treg stability and increased Th17 differentiation. [Read the Full Post]

Human Epidermal Growth Factor Receptor 2 Testing in Breast Cancer: American Society of Clinical Oncology-College of American Pathologists Guideline Update

158 | Sep 23 2023

The American Society of Clinical Oncology-College of American Pathologists (ASCO-CAP) affirms the 2018 recommendations for HER2 testing in breast cancer but highlights the importance of distinguishing between immunohistochemistry (IHC) 0 and 1+ results and provides best practice recommendations for this distinction. [Read the Full Post]

Sulfopin is a covalent inhibitor of Pin1 that blocks Myc-driven tumors in vivo

62 | Sep 22 2023

The study successfully developed Sulfopin, a nanomolar Pin1 inhibitor, which demonstrated potent target engagement, downregulation of c-Myc target genes, and therapeutic benefits in preclinical models of neuroblastoma and pancreatic cancer, highlighting Pin1 as a potential drug target for cancer treatment. [Read the Full Post]

Modeling the Effect of Cooperativity in Ternary Complex Formation and Targeted Protein Degradation Mediated by Heterobifunctional Degraders

168 | Sep 16 2023

This study develops a pharmacodynamic model and statistical inference model to investigate the role of cooperativity in ternary complex formation and degradation efficiency, providing insights for the rational design of effective HBF degraders in targeted protein degradation. [Read the Full Post]

Anti-Klebsiella pneumoniae activity of secondary metabolism of Achromobacter from the intestine of Periplaneta americana

250 | Sep 13 2023

This study identifies a strain of Achromobacter from the intestinal tract of Periplaneta americana that exhibits strong antibacterial activity against Klebsiella pneumoniae, highlighting the potential for the development of novel antimicrobial compounds from insect intestinal microorganisms. [Read the Full Post]

Ursolic acid-downregulated long noncoding RNA ASMTL-AS1 inhibits renal cell carcinoma growth via binding to HuR and reducing vascular endothelial growth factor expression

185 | Sep 12 2023

The study found that ursolic acid (UA) inhibits renal cell carcinoma (RCC) growth and tumorigenesis by downregulating ASMTL-AS1, which destabilizes VEGF mRNA and suppresses RCC cell migration, invasion, and angiogenesis. [Read the Full Post]

Effects of the inclusion of coffee pulp silage in the diet on the performance and profitability of crossbred milk cows in the middle tropics

155 | Sep 06 2023

The inclusion of coffee pulp silage in the diet of crossbred dairy cows in the middle tropics improved their productive efficiency and nutritional characteristics without affecting milk production. [Read the Full Post]

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

210 | 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

220 | 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]

MUC1-C is a master regulator of MICA/B NKG2D ligand and exosome secretion in human cancer cells

51 | Aug 20 2023

Targeting the MUC1-C protein in cancer cells enhances the expression of MICA/B ligands, inhibits their cleavage, reduces exosome secretion, and promotes NK cell-mediated killing, uncovering mechanisms by which MUC1-C confers immune evasion to cancer cells. [Read the Full Post]

Glutathione-Scavenging Nanoparticle-Mediated PROTACs Delivery for Targeted Protein Degradation and Amplified Antitumor Effects

88 | Aug 09 2023

The development of Nano-PROTACs, which involve encapsulating PROTACs in GSH-responsive polymeric nanoparticles, demonstrates improved bioavailability, enhanced protein degradation, and superior anti-tumor efficacy, showing promise for the targeted treatment of diseases. [Read the Full Post]

VH298-loaded extracellular vesicles released from gelatin methacryloyl hydrogel facilitate diabetic wound healing by HIF-1α-mediated enhancement of angiogenesis

299 | Aug 03 2023

This study demonstrates the potential of VH298-loaded extracellular vesicles (EVs) and GelMA hydrogel as a promising therapeutic strategy for diabetic wound treatment, promoting angiogenesis and enhancing wound healing. [Read the Full Post]

BRD4: New hope in the battle against glioblastoma

119 | Jul 28 2023

This review provides a comprehensive overview of the roles and mechanisms of BRD4 in glioblastoma pathogenesis, as well as evaluates the potential of BRD4 inhibitors and degraders as novel treatment strategies against GBM. [Read the Full Post]

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

250 | 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]

Charting the Chemical Reaction Space around a Multicomponent Combination: Controlled Access to a Diverse Set of Biologically Relevant Scaffolds

82 | Jun 28 2023

Researchers have developed general protocols to selectively access desired chemotypes by combining carbonyls, amines, and isocyanoacetates, leading to the synthesis of unsaturated imidazolone scaffolds with the chromophore of the green fluorescent protein and the core structure of the natural product coelenterazine, as well as unprecedented reactivity at the C-2 position to obtain diverse derivatives featuring natural products, kinase inhibitors, and fluorescent probes. [Read the Full Post]

Results of a Phase II Trial Testing the Resensitization With Trabectedin in Platinum-resistant Ovarian Cancer

92 | Jun 26 2023

The study found that while trabectedin did not result in widespread resensitization to platinum-based chemotherapy in heavily pretreated patients with platinum-resistant ovarian cancer, a significant proportion of patients achieved disease control with the treatment. [Read the Full Post]

Short-term follow-up pilot study of sole middle meningeal artery embolization for chronic subdural hematoma: influence of internal architecture on the radiological outcomes

178 | Jun 24 2023

The study found that patients with separated chronic subdural hematoma (CSDH) architecture had a lower rate of achieving the radiological endpoint and a slower rate of volume reduction compared to other CSDH types when treated with middle meningeal artery embolization (MMAE). [Read the Full Post]

SLC26A3 (DRA) is stimulated in a synergistic, intracellular Ca2+ dependent manner by cAMP and ATP in intestinal epithelial cells

51 | Jun 14 2023

The study demonstrated that the combined presence of subthreshold concentrations of forskolin and ATP synergistically stimulated DRA activity and intracellular calcium levels, potentially contributing to increased anion secretion in diarrheal diseases with elevated cAMP and Ca2+ levels. [Read the Full Post]

Mediation of PKM2-dependent glycolytic and non-glycolytic pathways by ENO2 in head and neck cancer development

144 | Jun 10 2023

ENO2 plays a crucial role in head and neck squamous cell carcinoma (HNSCC) by promoting cell proliferation and glycolysis through regulation of PKM2 stability and nuclear translocation, and targeting ENO2 shows potential as a therapeutic strategy for HNSCC treatment. [Read the Full Post]

Icariin promotes osteogenic differentiation by upregulating alpha-enolase expression

58 | Jun 10 2023

Icariin promotes osteogenic differentiation by upregulating alpha-enolase (Eno1) and activating the BMP/Smad4 signaling pathway, indicating Eno1 as a promising drug target for regulating bone formation. [Read the Full Post]

Aberrant m5C hypermethylation mediates intrinsic resistance to gefitinib through NSUN2/YBX1/QSOX1 axis in EGFR-mutant non-small-cell lung cancer

166 | Jun 07 2023

This study demonstrates that aberrant RNA m5C modification via the NSUN2-YBX1-QSOX1 axis plays a critical role in mediating intrinsic resistance to gefitinib in EGFR-mutant NSCLC. [Read the Full Post]

Incorporating valsartan in sesame oil enriched self-nanoemulsifying system-loaded liquisolid tablets to improve its bioavailability

106 | May 12 2023

This study developed liquisolid tablets containing a self-nanoemulsifying drug delivery system to improve the solubility and dissolution rate of Valsartan, resulting in increased bioavailability compared to the marketed product. [Read the Full Post]

Subchronic toxicity study of ferric oxide nanoparticles through intragastric administration: A 94-d, repeated dose study in Sprague Dawley rats

89 | May 12 2023

The study found that Fe2O3 NPs administered through gavage to SD rats for 94 days did not show significant toxicity or adverse effects up to a dose of 500 mg/kg, followed by recovery after Fe2O3 NPs withdrawal for 30 days. [Read the Full Post]

Optimization of the Solvent and In Vivo Administration Route of Auranofin in a Syngeneic Non-Small Cell Lung Cancer and Glioblastoma Mouse Model

94 | May 12 2023

The study provides important information on the optimal administration route and solvent of auranofin in two syngeneic cancer mouse models, which could contribute to its further development as a potential cancer therapy. [Read the Full Post]

Preferential Solvation Study of Rosuvastatin in the {PEG400 (1) + Water (2)} Cosolvent Mixture and GastroPlus Software-Based In Vivo Predictions

76 | May 12 2023

The study investigates the solubility and preferential solvation of rosuvastatin in PEG400 + water binary mixtures and predicts that the RST-loaded mixture can enhance the drug's oral absorption and be a promising strategy to control systemic dyslipidemia. [Read the Full Post]

DLin-MC3-Containing mRNA Lipid Nanoparticles Induce an Antibody Th2-Biased Immune Response Polarization in a Delivery Route-Dependent Manner in Mice

48 | May 11 2023

The study investigated the influence of lipid components and immunization route on the humoral immune responses induced by mRNA-based vaccines in mice, highlighting the importance of considering the delivery route when designing and optimizing vaccination strategies. [Read the Full Post]

Intracellular trafficking kinetics of nucleic acid escape from lipid nanoparticles via fluorescence imaging

192 | May 11 2023

The study investigates the intracellular fate of different lipid nanoparticles for delivering nucleic acids to target cell populations using fluorescence microscopy to determine their localization to endosomes and lysosomes, and demonstrated the technique across different nucleic acid types to aid in the formulation optimization for in vivo studies. [Read the Full Post]

Hematological parameters, antioxidant status, and gene expression of γ-INF and IL-1β in vaccinated lambs fed different type of lipids

78 | May 11 2023

The study suggests that flaxseed oil had more beneficial effects on the immune response than other vegetable oils in vaccinated lambs. [Read the Full Post]

Non-Nucleoside Inhibitors Decrease Foot-and-Mouth Disease Virus Replication by Blocking the Viral 3Dpol

202 | May 10 2023

The study used virtual screening and cell-based assays to identify potential inhibitors targeting the RNA-dependent RNA polymerase of Foot-and-mouth disease virus, and identified four compounds with antiviral activity. [Read the Full Post]

In vivo bioluminescence imaging of natural bacteria within deep tissues via ATP-binding cassette sugar transporter

52 | May 08 2023

A novel bioluminescence imaging method utilizing bacteria-specific ATP-binding cassette sugar transporters to internalize probes and differentiate bacterial and non-bacterial infections in vivo was developed. [Read the Full Post]

COVID-19 Vaccine Response in People with Multiple Sclerosis Treated with Dimethyl Fumarate, Diroximel Fumarate, Natalizumab, Ocrelizumab, or Interferon Beta Therapy

55 | May 07 2023

This study evaluated the immune response to the mRNA-1273 COVID-19 vaccine in people with MS receiving different DMTs and found that the humoral response was preserved and similar in participants treated with natalizumab, fumarates, and interferon beta, but muted with ocrelizumab, with all DMTs having preserved T cell response but the ocrelizumab cohort having a greater risk of vaccine-related side effects. [Read the Full Post]

The anorectic and thermogenic effects of pharmacological lactate in male mice are confounded by treatment osmolarity and co-administered counterions

126 | May 06 2023

The passage highlights the importance of controlling for injection osmolarity and counterions in metabolite research, as the hypertonicity of injected solutions and co-injected ions can confound the results of studies investigating lactate's effects. [Read the Full Post]

Ligand-Controlled Growth of Different Morphological Bimetallic Metal-Organic Frameworks for Enhanced Charge-Storage Performance and Quasi-Solid-State Hybrid Supercapacitors

166 | May 06 2023

This research work demonstrates a ligand-mediated approach to obtain different morphological surface structures of bimetallic metal-organic frameworks, which can offer a new pathway for synthesizing MOF materials for energy storage applications. [Read the Full Post]

Nitric Oxide Precursors and Dimethylarginines as Risk Markers for Accelerated Measured GFR Decline in the General Population

203 | May 05 2023

This prospective cohort study found that higher levels of asymmetric dimethylarginine were associated with a slower decline in glomerular filtration rate, while higher levels of citrulline and ornithine were associated with accelerated GFR decline and an increased risk of new-onset chronic kidney disease, suggesting a significant role of NO metabolism in the pathogenesis of CKD in middle-aged people. [Read the Full Post]

High level expression of nicotinamide nucleoside kinase from Saccharomyces cerevisiae and its purification and immobilization by one-step method

74 | May 02 2023

This study optimized the expression and immobilization of ScNRK1 to improve the enzyme activity and stability for the enzymatic synthesis of NMN, which has important implications for human health and potential applications in commercial production. [Read the Full Post]

Identification of the stable and reactive metabolites of tetrahydropiperine using ultrahigh-performance liquid chromatography combined with diode-array detection and high-resolution mass spectrometry

39 | May 01 2023

The study aimed to investigate the metabolic profiles of tetrahydropiperine in various species of hepatocytes, and the results showed that it was bioactivated through ortho-quinone, Michael receptor, and aldehyde intermediates, with major metabolic pathways being hydroxylation, dehydrogenation, methylation, GSH conjugation, and glucuronidation. [Read the Full Post]

A large-scale functional analysis of genes expressed differentially in insulin secreting MIN6 sublines with high versus mildly reduced glucose-responsiveness

227 | May 01 2023

This study identified 18 genes that altered glucose-stimulated insulin secretion (GSIS) in pancreatic β-cells, and confirmed Sox11 as a negative regulator of insulin secretion and its role in glucose metabolism. [Read the Full Post]

Nrf2 transcriptional activity in the mouse affects the physiological response to tribromoethanol

66 | Apr 26 2023

The study found that Avertin causes prolonged anesthesia in tNrf2-/- mice without acute toxicity, inflammatory reaction, or enhanced oxidative stress, and can normalize enhanced fibrosis without impairing intestine morphology in tNrf2-/- mice. [Read the Full Post]

Safety and efficacy of WC2031 versus vibramycin for the treatment of uncomplicated urogenital Chlamydia trachomatis infection: a randomized, double-blind, double-dummy, active-controlled, multicenter trial

128 | Apr 23 2023

The study found that a once-daily, delayed-release formulation of doxycycline hyclate (WC2031) was noninferior to twice-daily Vibramycin for the treatment of uncomplicated urogenital chlamydia and was better tolerated, with comparable safety. [Read the Full Post]

Multifunctional porous poly (L-lactic acid) nanofiber membranes with enhanced anti-inflammation, angiogenesis and antibacterial properties for diabetic wound healing

257 | Apr 22 2023

The study developed porous PLA/SCS/PDA-GS nanofiber membranes with enhanced antibacterial, anti-inflammatory, and angiogenic properties, demonstrating promising potential in diabetic wound healing processes. [Read the Full Post]

Imaging the TGFβ type I receptor in pulmonary arterial hypertension

62 | Apr 21 2023

This study evaluated the efficacy of two ALK5-targeting PET tracers for imaging ALK5 in pulmonary arterial hypertension, with [18F]EW-7197 showing superior in vivo imaging results compared to [11C]LR111. [Read the Full Post]

Prebiotic Galacto-Oligosaccharides and Fructo-Oligosaccharides, but Not Acacia Gum, Increase Iron Absorption from a Single High-Dose Ferrous Fumarate Supplement in Iron-Depleted Women

77 | Apr 20 2023

The study found that co-administration of prebiotic fibers such as GOS and FOS with FeFum increased iron absorption by approximately 50% in iron-depleted women, suggesting their potential as enhancers of supplemental iron absorption. [Read the Full Post]

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

451 | 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

483 | 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]

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

345 | 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]

An efficient transformation method for tannin-containing sorghum

232 | Apr 14 2023

The successful establishment of an efficient microprojectile transformation system for tannin-containing sorghum using immature embryos of Hongyingzi as explants offers the possibility of breaking the restriction imposed by tannins in plants and improving the nutritional value and potential of sorghum as a food and feed crop. [Read the Full Post]

A Versatile Toolset for Genetic Manipulation of the Wine Yeast Hanseniaspora uvarum

141 | Apr 14 2023

The passage describes the development of a toolset for efficient and targeted genetic manipulation of the yeast species Hanseniaspora uvarum, which includes the creation of homozygous auxotrophic deletion markers, self-replicating cloning vectors, and a chemical transformation procedure. [Read the Full Post]

A highly efficient genetic transformation system for broccoli and subcellular localization

168 | Apr 12 2023

This study provides new insights into the improvement of the genetic transformation and molecular breeding of broccoli, which could lead to the development of improved crop varieties with enhanced traits. [Read the Full Post]

Preclinical pharmacologic evaluation of geldanamycin as an antitumor agent

299 | Mar 31 2023

The passage describes the pharmacokinetics of geldanamycin in mice and a dog and highlights the potential for acute hepatotoxic reactions, indicating a need for further pharmacological and therapeutic information before considering the drug for clinical development. [Read the Full Post]

Identification of significant gene expression changes in multiple perturbation experiments using knockoffs

360 | Mar 30 2023

The approach described uses the model-X knockoffs framework and Deep Neural Networks to identify significant gene expression changes in multiple perturbation experiments, allowing for better understanding of underlying mechanisms of disease and identification of new drug targets. [Read the Full Post]

The outcome of ibrutinib-based regimens in relapsed/refractory central nervous system lymphoma and the potential impact of genomic variants

152 | Mar 28 2023

This study suggests that ibrutinib-based therapy is effective and safe for treating r/r CNSL patients, and patients with less genomic complexity, especially with regard to TMB, may benefit more from ibrutinib regimens. [Read the Full Post]

A nitric-oxide driven chemotactic nanomotor for enhanced immunotherapy of glioblastoma

163 | Mar 26 2023

The proposed chemotactic nanomotor loaded with brain endothelial cell targeting agent angiopep-2 and anti-tumor drug TLND, which uses ROS/iNOS as chemoattractants to induce the chemotactic behavior, has the potential to overcome major challenges of immunotherapy for glioblastoma and enhance the immune response against the tumor while preventing recurrence. [Read the Full Post]

Directly targeting ASC by lonidamine alleviates inflammasome-driven diseases

152 | Mar 26 2023

The study found that LND is a broad-spectrum inflammasome inhibitor that directly targets ASC and may have potential as a therapeutic agent for inflammasome-driven diseases in clinic. [Read the Full Post]

Clonal hematopoiesis involving DNA damage response genes in patients undergoing lung transplantation is increased

97 | Mar 23 2023

The study found that clonal hematopoiesis (CH) in DNA damage response genes TP53, PPM1D, and ATM is highly prevalent in patients with severe lung disease undergoing lung transplantation and is associated with post-transplant outcomes including cytomegalovirus activation and mycophenolate intolerance. [Read the Full Post]

Interplay of Breast Cancer Resistance Protein (Bcrp/Abcg2), Sex, and Fed State in Oral Pharmacokinetic Variability of Furosemide in Rats

118 | Mar 23 2023

The study investigated the effect of Bcrp-mediated transport, sex, and fed state on the pharmacokinetics of FUR in rats and found that Bcrp inhibition increased FUR exposure and that sex differences in Bcrp and Oat abundance in the kidney could influence PK. [Read the Full Post]

The European guideline on management of major bleeding and coagulopathy following trauma: sixth edition

94 | Mar 23 2023

The sixth edition of the European guideline on the management of major bleeding and coagulopathy following traumatic injury provides concise, evidence-based recommendations for the management of bleeding trauma patients, emphasizing the importance of a systematic approach to reduce preventable deaths. [Read the Full Post]

Unusual Square Pyramidal Chalcogenide Mo5 Cluster with Bridging Pyrazolate-Ligands

53 | Mar 21 2023

New chalcogenide molybdenum clusters with square pyramidal complexes [{Mo5(μ3-Se)i4(μ4-Se)i(μ-pz)i4}(pzH)t5]1+/2+ have been synthesized and characterized, showing promise for use in superconducting, magnetic, and catalytic systems. [Read the Full Post]

Metabolomic Analysis Reveals the Metabolic Diversity of Wild and Cultivated Stellaria Radix ( Stellaria dichotoma L. var. lanceolata Bge.)

216 | Mar 21 2023

The study compared the metabolites of wild and cultivated Yinchaihu, showing that the contents of total sterols and total flavonoids were significantly higher in wild Yinchaihu, while identifying 97 significant differences in metabolites between the two sources. [Read the Full Post]

Attenuation of initial pilocarpine-induced electrographic seizures by methionine sulfoximine pretreatment tightly correlates with the reduction of the extracellular taurine in the hippocampus

40 | Mar 13 2023

The study showed that the beneficial effect of MSO in mitigating the intensity of initial pilocarpine-induced seizures in juvenile rats is due to the prevention of cell volume increase concurrent with the onset of seizures, as indicated by the strong correlation between the attenuation of seizures and extracellular accumulation of taurine. [Read the Full Post]

Alginate oligosaccharides enhance the antifungal activity of nystatin against candidal biofilms

236 | Mar 11 2023

The study demonstrates the potential clinical utility of OligoG in conjunction with nystatin against Candida spp. in the prevention and topical treatment of candidal biofilm infections. [Read the Full Post]

Surface-Functionalized Metal-Organic Frameworks for Binding Coronavirus Proteins

153 | Mar 11 2023

The research proposes using metal-organic frameworks (MOFs) functionalized with repurposed antiviral agents to selectively bind and deactivate respiratory coronaviruses, highlighting their potential in combating future pandemics. [Read the Full Post]

HLA-haploidentical hematopoietic stem cells transplantation with regulatory and conventional T-cell adoptive immunotherapy in pediatric patients with very high-risk acute leukemia

175 | Mar 07 2023

The study reports promising outcomes of a novel HLA-haploidentical hematopoietic stem cell transplantation strategy with adoptive immunotherapy in pediatric patients with high-risk acute leukemia who lack an HLA-matched donor. [Read the Full Post]

Antifibrinolytics use during surgery for oncological spine diseases: A systematic review

65 | Mar 03 2023

The use of tranexamic acid in patients undergoing surgery for oncological spine disease may reduce intraoperative blood loss, transfusion requirements, and postoperative drainage while not significantly increasing the incidence of deep venous thrombosis or pulmonary embolism. [Read the Full Post]

First report of rot disease in Prunus salicina var. taoxingli fruit caused by Fusarium lateritium in China

0 | Mar 03 2023

A study reports on Fusarium lateritium causing rot on Shengzhou nane fruits in Zhejiang province, China, and highlights the need for effective control strategies to reduce its incidence. [Read the Full Post]

The Gradual Release of Alendronate for the Treatment of Critical Bone Defects in Osteoporotic and Control Rats

63 | Mar 01 2023

This study demonstrates the potential of emulsion/dispersion scaffolds containing ALN and HA nanoparticles for local delivery of ALN in the treatment of osteoporosis, with positive effects on bone formation observed both in vitro and in vivo. [Read the Full Post]

Exploring drug repositioning for leishmaniasis treatment: Ivermectin plus polymeric micelles induce immunological response and protection against tegumentary leishmaniasis

79 | Mar 01 2023

The study found that ivermectin has the potential to be a candidate for the treatment of leishmaniasis caused by different species of Leishmania, as it showed efficacy in reducing parasite load and lesion size in infected mice, with low toxicity, and maintained efficacy 30 days after therapy. [Read the Full Post]

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

184 | 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]

Staurosporine analogues from microbial and synthetic sources and their biological activities

452 | Feb 20 2023

Staurosporine and its analogues have strong inhibitory effects against a variety of kinases and have various biological properties such as antifungal, antibacterial, and immunosuppressive activities, but have limited clinical effectiveness due to cross-reactivity and poor selectivity. [Read the Full Post]

Critical Role of Position 10 Residue in the Polymyxin Antimicrobial Activity

212 | Feb 19 2023

The study synthesized 30 novel analogues of polymyxin B1 modified at position 10 to examine their antimicrobial activity against Gram-negative bacteria and toxicity, revealing the role of the β-hydroxy side chain in promoting the correctly folded conformation of the polymyxin that drives outer membrane penetration and antibacterial activity, providing important information for developing new-generation polymyxin antibiotics. [Read the Full Post]

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

204 | 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

295 | 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]

Camptothecin analogs in malignant gliomas: comparative analysis and characterization

259 | 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

414 | 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]

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

519 | 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

700 | 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

217 | 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

219 | 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]

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

154 | 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

290 | 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]

Loss of tRNA methyltransferase 9 and DNA damage response genes in yeast confers sensitivity to aminoglycosides

278 | Feb 08 2023

The study showed that Trm9-catalyzed tRNA modifications enhance the DNA damage response and that cells with tRNA modification dysregulation and DNA repair gene defects can be selectively sensitized using a combination of translation inhibitors and DNA damaging agents. [Read the Full Post]

DNA radiosensitization by terpyridine-platinum: damage induced by 5 and 10 eV transient anions

135 | Feb 08 2023

Tpy-Pt enhances DNA damage induced by monoenergetic electrons in CRT, with the highest enhancement for base damage-related crosslinks, potentially causing roadblocks to replication and transcription in genomic DNA, particularly within telomeres where it binds preferentially to G-quadruplexes. [Read the Full Post]

Phase II Trials of Iniparib (BSI-201) in Combination with Gemcitabine and Carboplatin in Patients with Recurrent Ovarian Cancer

249 | Feb 08 2023

In two parallel phase II studies of iniparib (BSI-201) combined with gemcitabine and carboplatin in ovarian cancer patients, the overall response rate was 66% in platinum-sensitive disease and 26% in platinum-resistant disease, with higher response rates in patients with BRCA mutations and the combination was generally well tolerated with no new toxicities. [Read the Full Post]

Gancao Nourishing-Yin decoction combined with methotrexate in treatment of aging CIA mice: a study based on DIA proteomic analysis

393 | Feb 07 2023

Gancao Nourishing-Yin decoction (GCNY) added to methotrexate (MTX) showed better effects in treating elderly rheumatoid arthritis (ERA) mice model compared to either treatment alone, as seen through improved joint damage, decreased inflammation, and regulation of metabolism-related pathways, and ELISAs confirmed improved folic acid levels and anti-folate resistance pathways. [Read the Full Post]

Five-year cardiovascular event risk in early rheumatoid arthritis patients who received treat-to-target management: a case-control study

343 | Feb 07 2023

The study found that ERA patients managed using a treat-to-target strategy had a similar incidence of cardiovascular events compared to a CV risk factor-matched non-RA population, while a historical RA cohort receiving routine care had a significantly higher incidence. [Read the Full Post]

CXCL9 links skin inflammation and fibrosis via CXCR3-dependent upregulation of collagen 1a1 in fibroblasts

164 | Feb 07 2023

The study provides evidence that CXCL9 and its receptor CXCR3 play a key role in the development of inflammation and fibrosis in morphea through the induction of collagen 1a1 expression. [Read the Full Post]

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

355 | 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]

Neoadjuvant chemotherapy with weekly cisplatin and paclitaxel followed by chemoradiation for locally advanced cervical cancer

390 | Feb 01 2023

The study found that neoadjuvant chemotherapy with weekly cisplatin and paclitaxel followed by concurrent chemoradiation was a feasible, safe and effective treatment for cervical cancer, with a high response rate and good overall survival. [Read the Full Post]

Preparation and evaluation of paclitaxel-loaded reactive oxygen species and glutathione redox-responsive poly(lactic-co-glycolic acid) nanoparticles for controlled release in tumor cells

284 | Feb 01 2023

The study found that PLGA copolymer with thioether and disulfide groups can effectively deliver paclitaxel to tumors, leading to increased drug accumulation at the site and offering a promising approach for intelligent and responsive drug delivery. [Read the Full Post]

Identification of Potential Treatments for Acute Lymphoblastic Leukemia through Integrated Genomic Network Analysis

135 | Jan 03 2023

Zulfan Zazuli et al. thought that chlorprothixene, sirolimus, dihydroergocristine, papaverine, and tamoxifen were the top five drug repositioning candidates for ALL according to the CMap score with dasatinib as a comparator. [Read the Full Post]

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

301 | 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

408 | Dec 29 2022

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

Novel biallelic mutations in TTC29 cause asthenoteratospermia and male infertility

139 | Dec 10 2022

Siyu Dai et al. found the novel biallelic mutations in TTC29 in a MMAF patient, which findings expand the mutational spectrum of TTC29. [Read the Full Post]

Unearthing the Janus-face cholesterogenesis pathways in cancer

82 | Dec 10 2022

Babita Madan et al. suggested a potential role of disrupted cholesterol biosynthesis, in coordination with imported cholesterol, as a factor in cancer development. [Read the Full Post]

Proteolysis Targeting Chimeras (PROTACs) of Anaplastic Lymphoma Kinase (ALK)

280 | Dec 07 2022

Chengwei Zhang et al. found that MS4077 (5) and MS4078 (6) potently decreased cellular levels of oncogenic active ALK fusion proteins in a concentration- and time-dependent manner in SU-DHL-1 lymphoma and NCI-H2228 lung cancer cells. [Read the Full Post]

Drug Stability and Minimized Acid-/Drug-Catalyzed Phospholipid Degradation in Liposomal Irinotecan

263 | Dec 06 2022

Dmitri B Kirpotin et al. demonstrated that a narrow set of conditions related to the external pH, temperature, intraliposomal concentration, identity of the drug-trapping agent, physical form of the drug inside the liposomes. [Read the Full Post]

OXPHOS deficiency induces mitochondrial DNA synthesis through non-canonical AMPK-dependent mRNA compartmentalization

98 | Nov 24 2022

Milon Banik et al. inferred that AMPK was locally activated by inhibition of the F1F0 ATP synthase to stimulate association of mtDNA replication factor mRNAs, leading to stimulation of mtDNA synthesis. [Read the Full Post]

Dual Delivery of Cyclosporin A and Etodolac Using Polymeric Nanocapsules in a Rabbit Eye Model: Ocular Biodistribution and Pharmacokinetic Study

158 | Nov 11 2022

Syed Nazrin Ruhina Rahman et al. thought that the biodistribution and pharmacokinetic data might help and strengthen their understanding of synergetic anti-inflammatory activity of CsA and Edc from nanocapsules after its ocular topical application for managing keratoconjunctivitis sicca. [Read the Full Post]

Oil-free eye drops containing Cyclosporine A/cyclodextrin/PVA supramolecular complex as a treatment modality for dry eye disease

219 | Oct 06 2022

Pinal Chaudhari et al. demonstrated the potential of the supramolecular complex as an alternative to the oil-based formulation of eye drops for drugs that showed low solubility and poor corneal permeation. [Read the Full Post]

Radical S-Adenosyl Methionine Enzyme BlsE Catalyzes a Radical-Mediated 1,2-Diol Dehydration during the Biosynthesis of Blasticidin S

188 | Aug 26 2022

Yu-Hsuan Lee et al. suggested that BlsE catalysis likely proceeded via direct elimination of water from the CGA C4' α-hydroxyalkyl radical as opposed to 1,2-migration of the C3'-hydroxyl prior to dehydration. [Read the Full Post]

Small Molecule Inhibitors of MERTK and FLT3 Induce Cell Cycle Arrest in Human CD8 + T Cells

152 | 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

152 | 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]

Synthesis, structural characterization, DFT calculations, molecular docking, and molecular dynamics simulations of a novel ferrocene derivative to unravel its potential antitumor activity

742 | Jun 12 2022

Mohamed M Hammoud et al. revealed the antitumor potential of ferrocene derivative (10) through targeting and inhibiting mitogen-activated protein (MAP) kinases interacting kinase (Mnk) 1.Communicated by Ramaswamy H. Sarma. [Read the Full Post]

Three Birds, One Excipient: Development of an Improved pH, Isotonic, and Buffered Ketamine Formulation for Subcutaneous Injection

343 | Jun 03 2022

Jason Wallach et al. found that this strategy has the potential to be readily adapted to other amine-based APIs. [Read the Full Post]

Stability of Captisol-enabled versus propylene glycol-based melphalan at room temperature and after refrigeration

260 | Jun 03 2022

Jitesh D Kawedia et al. found that CE-melphalan at 2 mg/mL has 24-hour stability at RT and can be used for extended infusion times or may be compounded ahead of time. Reconstituted CE-melphalan vials are stable for 48 hours at both RT and 4 °C. [Read the Full Post]

Physicochemical Characterization, Molecular Docking, and In Vitro Dissolution of Glimepiride-Captisol Inclusion Complexes

376 | Jun 01 2022

Arpita Pal et al. found that complexation with Captisol enhanced the water solubility of glimepiride. [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

577 | 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]

Long Noncoding RNA MALAT1 Promotes Laryngocarcinoma Development by Targeting miR-708-5p/BRD4 Axis to Regulate YAP1-Mediated Epithelial-Mesenchymal Transition

505 | May 25 2022

Xiaoqin Wu et al. thought that targeting MALAT1/miR-708-5p/BRD4 axis might provide a promising therapeutic strategy for laryngocarcinoma. [Read the Full Post]

Intron retention coupled with nonsense-mediated decay is involved in cellulase biosynthesis in cellulolytic fungi

304 | May 20 2022

Yichen Gao et al. provided better understanding on intron retention, the NMD pathway, and cellulase production mechanism in filamentous fungi. [Read the Full Post]

The BCL2 Inhibitor Venetoclax Plus Rituximab Is Active in MYD88 Wild-Type Polyneuropathy With Anti-MAG Antibodies

266 | May 18 2022

Chiara Briani et al. found that Class IV evidence that for a patient with relapsed anti-MAG antibody polyneuropathy, MYD88 wild-type, venetoclax plus rituximab was effective. [Read the Full Post]

Impact of optimal vaccination and social distancing on COVID-19 pandemic

412 | May 10 2022

Sangeeta Saha et al. observed that maintaining physical distancing and taking vaccines at an early stage decreases the infection level significantly in the environment by reducing the probability of becoming infected. [Read the Full Post]

Phase II Clinical and Translational Study of Everolimus ± Paclitaxel as First-Line Therapy in Cisplatin-Ineligible Advanced Urothelial Carcinoma

459 | Apr 25 2022

Tomi Jun et al. thought that everolimus plus paclitaxel demonstrated clinical activity in cisplatin-ineligible patients with metastatic UC, although the specific contribution of everolimus could not be delineated. [Read the Full Post]

First-line therapy in non-small cell lung cancer patients with EGFR activating mutations: a consideration of the clinical position of osimertinib based on the subset of Japanese patients in the FLAURA study

334 | Apr 22 2022

Yoko Tsukita et al. reviewed data from the randomized clinical trials of first-line EGFR-TKIs including a subset of Japanese patients and discussed first-line therapies for patients with NSCLC harbouring EGFR mutations. [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

762 | 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]

CDK4/6 inhibitor enhances the radiosensitization of esophageal squamous cell carcinoma (ESCC) by activating autophagy signaling via the suppression of mTOR

285 | Apr 17 2022

Wen-Jun Qin et al. found that palbociclib improved the radiosensitivity of ESCC in vivo and in vitro, and thus it might be a promising radiosensitization agent for the treatment of ESCC. [Read the Full Post]

Degradation and inhibition of epigenetic regulatory protein BRD4 exacerbate Alzheimer's disease-related neuropathology in cell models

204 | Apr 12 2022

Siyi Zhang et al. not only showed that BRD4 was a novel epigenetic component that regulated BACE1 and Aβ levels, but also provided novel and translational insighted into the targeting of BRD4 for potential clinical applications. [Read the Full Post]

AI-Radiomics Can Improve Inclusion Criteria and Clinical Trial Performance

247 | Feb 28 2022

Michal R Tomaszewski et al. showed that had an appropriate model been used for selective patient inclusion, SARC021 trial could have met its primary survival objective for patients with metastatic STS. [Read the Full Post]

Sunitinib and Evofosfamide (TH-302) in Systemic Treatment-Naïve Patients with Grade 1/2 Metastatic Pancreatic Neuroendocrine Tumors: The GETNE-1408 Trial

422 | Feb 28 2022

Enrique Grande et al. found that the high systemic toxicity, with 88.2% of patients discontinuing the treatment, made this therapeutic approach unfeasible and encourages future research to overcome panNETs' resistance to antiangiogenic agents with other therapies with a safer profile. [Read the Full Post]

Effect of Divalent Metal Ion on the Structure, Stability and Function of Klebsiella pneumoniae Nicotinate-Nucleotide Adenylyltransferase: Empirical and Computational Studies

181 | Feb 14 2022

Olamide Jeje et al. thought that ATP binding affected KpNNAT dynamics, and the dynamics of ATP binding depended on the presence and type of divalent cation. [Read the Full Post]

Screening of the ubiquitin-proteasome system activators for anti-Alzheimer's disease by the high-content fluorescence imaging system

0 | Feb 03 2022

Yi-Ling Wang found that a novel insight into the discovery and development of anti-AD drugs. [Read the Full Post]

A standard knockout procedure alters expression of adjacent loci at the translational level

372 | Feb 02 2022

Artyom A Egorov et al. estimated that in as much as ∼1/5 of knockout strains the expression of neighboring genes might be substantially (>2-fold) deregulated at the level of translation. [Read the Full Post]

Establishment of gastric signet ring cell carcinoma organoid for the therapeutic drug testing

402 | Jan 13 2022

Guoliang Li et al. thought that gastric organoid drug models, including SRCC, were highly similar to the original tumors in phenotypic and genotypic profiling and could be as living biomarkers for drug response testing. [Read the Full Post]

Cannabidiol Inhibits In Vitro Human Liver Microsomal Metabolism of Remdesivir: A Promising Adjuvant for COVID-19 Treatment

555 | Dec 19 2021

Aishwarya Saraswat et al. suggested that CBD significantly inhibited human liver microsomal metabolism of RDV and extended its in vitro half-life. [Read the Full Post]

A nephroprotective iodinated contrast agent with cardioprotective properties: A pilot study

465 | Nov 13 2021

Elizabeth S Rowe et.al suggested that SBECD-iohexol is superior to iohexol alone, for both the preservation of cardiomyocyte integrity and preservation of myocardial function in myocardial ischemia. [Read the Full Post]

A [3Fe-4S] cluster and tRNA-dependent aminoacyltransferase BlsK in the biosynthesis of Blasticidin S

787 | Oct 03 2021

Xiankun Wang et al. provided an example of an iron-sulfur protein that catalyzed an aminoacyl-tRNA (aa-tRNA)-dependent amide bond formation in a natural product biosynthetic pathway. [Read the Full Post]

Neoantigen-Specific T-Cell Immune Responses: The Paradigm of NPM1-Mutated Acute Myeloid Leukemia

647 | 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

599 | Sep 20 2021

Xiyuan Lu et al. identified a novel drug combination, AC220 and IACS-010759. [Read the Full Post]

Angiokinase inhibition of VEGFR-2, PDGFR and FGFR and cell growth inhibition in lung cancer: Design, synthesis, biological evaluation and molecular docking of novel azaheterocyclic coumarin derivatives

1612 | Jul 21 2021

Eman Y Ahmed et al. found that 4a was capable of arresting the cell cycle at pre-G1 phase and S phase and inducing apoptosis. [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

1437 | 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]

The bromodomain inhibitor JQ1+ reduces calcium-sensing receptor activity in pituitary cell-lines

790 | Jul 06 2021

Kate E Lines et al. thought that reducing CaSR expression might be a viable option in the treatment of pituitary tumours. [Read the Full Post]

Evolution of β-catenin-independent Wnt-GSK3-mTOR signalling in regulation of energy metabolism in isoproterenol-induced cardiotoxicity model

566 | Jun 30 2021

Shriyansh Srivastava et al. discussed a novel therapeutic role of the β-catenin independent, Wnt-GSK3-mTOR axis in attenuation of Iso-induced cardiotoxicity in rodents. [Read the Full Post]

Natural history of Waldenström macroglobulinemia following acquired resistance to ibrutinib monotherapy

1243 | Jun 27 2021

Joshua N Gustine et al. revealed that continuation of ibrutinib until subsequent treatment was associated with improved disease control and clinical outcomes. [Read the Full Post]

Binding Insights into Quadruplex Selective Carbazole Ligands

691 | Jun 18 2021

Diana Müller et al. thought that carbazole was a very promising scaffold for assembling G4 ligands with a range of novel functional applications. [Read the Full Post]

Efficacy and safety of 177 Lu-DOTATATE in lung neuroendocrine tumors: a bi-center study

832 | May 31 2021

Lamiaa Zidan et al. found that in patients with advanced progressive lung NET and satisfactory SSR expression, 177Lu-DOTATATE was effective and safe with a high disease control rate and encouraging PFS and OS. [Read the Full Post]

Efficacy and Safety of Combination Treatment With Apatinib and Osimertinib After Osimertinib Resistance in Epidermal Growth Factor Receptor-Mutant Non-small Cell Lung Carcinoma-A Retrospective Analysis of a Multicenter Clinical Study

539 | May 26 2021

Xue Yang et al. found that the combination of apatinib and osimertinib improved the ORR and the DCR of patients with osimertinib-refractory EGFR-positive NSCLC, thus making it a reasonable treatment choice after the development of osimertinib resistance. [Read the Full Post]

Treatment of Luminal Metastatic Breast Cancer beyond CDK4/6 Inhibition: Is There a Standard of Care in Clinical Practice?

1527 | 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]

Lasofoxifene as a potential treatment for therapy-resistant ER-positive metastatic breast cancer

545 | May 14 2021

Muriel Lainé et al. reported for the first time the anti-tumor activity of lasofoxifene in mouse models of endocrine therapy-resistant breast cancer. [Read the Full Post]

BRD4 PROTAC degrader ARV-825 inhibits T-cell acute lymphoblastic leukemia by targeting 'Undruggable' Myc-pathway genes

640 | May 06 2021

Shuiyan Wu et al. thought that the BRD4 degrader ARV-825 could effectively suppress the proliferation and promote apoptosis of T-ALL cells via BET protein depletion and c-Myc inhibition, thus providing a new strategy for the treatment of T-ALL. [Read the Full Post]

Hypoxic targeting and activating TH-302 loaded transcatheter arterial embolization microsphere

447 | Mar 11 2021

Pengkai Ma et al. found that TH-302 microspheres showed to be feasible and effective for TACE and hold promise in the clinical for HCC chemoembolization therapy. [Read the Full Post]

Hypoxia-induced CREB cooperates MMSET to modify chromatin and promote DKK1 expression in multiple myeloma

362 | Mar 10 2021

Yinyin Xu et al. found that hypoxia and a cytogenetic abnormality regulated DKK1 expression in myeloma cells, and provided an additional rationale for the development of therapeutic strategies that interrupted DKK1 to cure MM. [Read the Full Post]

Safety evaluation after acute and sub-chronic oral administration of high purity nicotinamide mononucleotide (NMN-C®) in Sprague-Dawley rats

478 | Feb 26 2021

Cecile Cros et al. provided the first data highlighting the safety of short to intermediate term (sub-chronic) oral administration of NMN. [Read the Full Post]

The yeast platform engineered for synthetic gRNA-landing pads enables multiple gene integrations by a single gRNA/Cas9 system

778 | Feb 09 2021

Sihyun Baek et al. demonstrated the effectiveness of a single gRNA-mediated CRISPR platform to build complex metabolic pathways in yeast. [Read the Full Post]

[Altered Splicing in Stable Cell Strains Expressing Mini-hF9 Gene with Nonsense Mutation]

777 | Feb 09 2021

Gang Wang et al. found that the nonsense associated altered splicing (NAS) pathway, which generated alternately spliced transcripts, might be triggered in coagulation factor IX gene with nonsense mutation. [Read the Full Post]

Downregulation of breast cancer resistance protein by long-term fractionated radiotherapy sensitizes lung adenocarcinoma to SN-38

620 | Jan 23 2021

Yuqing Wang et al. suggested that irinotecan (the prodrug of SN-38) might be a promising drug candidate for lung adenocarcinoma patients with acquired radioresistance. [Read the Full Post]

Repurposing FDA approved drugs inhibiting mitochondrial function for targeting glioma-stem like cells

498 | Jan 11 2021

Sandipan Datta et al. demonstrated that FDA-approved mitochondrial inhibitors induced GSC-selective cytotoxicity, and targeting mitochondrial function could present a potential therapeutic option for GBM treatment. [Read the Full Post]

Potent and Specific Inhibition of NTCP-Mediated HBV/HDV Infection and Substrate Transporting by a Novel, Oral-Available Cyclosporine A Analogue

573 | Dec 29 2020

Yang Liu et al. found that 27A served as a promising lead for the development of novel anti-HDV/HBV agents. [Read the Full Post]

Effect of mechanochemical inclusion of triamterene into sulfobutylether-β-cyclodextrin and its improved dissolution behavior

602 | Nov 23 2020

Hideko Maeda et al. found that the water apparent solubility of TT could be improved by simple mechanical mixing without organic solvents, and improved bioavailability after oral administration was expected. [Read the Full Post]

CTELS: A Cell-Free System for the Analysis of Translation Termination Rate

823 | Sep 28 2020

Kseniya A Lashkevich et al. revealed a transient stalling event at a "leaky" stop codon context, which likely defined the basis of nonsense suppression. [Read the Full Post]

FLT3 inhibition upregulates HDAC8 via FOXO to inactivate p53 and promote maintenance of FLT3-ITD+ acute myeloid leukemia

644 | 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

647 | 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]

Overexpression of Fibroblast Growth factor-21 (FGF-21) Protects Mesenchymal Stem Cells Against Caspase-Dependent Apoptosis Induced by Oxidative Stress and Inflammation

1541 | Jun 22 2020

Gabriel R Linares et al. provided compelling evidence that FGF-21 played a crucial role in protecting MSCs from apoptosis induced by oxidative stress and inflammation, and merited further investigation as a strategy for enhancing the therapeutic efficacy of stem cell-based therapies. [Read the Full Post]

Staurosporine and NEM Mainly Impair WNK-SPAK/OSR1 Mediated Phosphorylation of KCC2 and NKCC1

1496 | Jun 18 2020

Jinwei Zhang et al. identified phospho-sites that are responsive to staurosporine or NEM application. [Read the Full Post]

Sulfobutylether-β-cyclodextrin /5,10,15,20-tetrakis(1-methylpyridinium-4-yl)porphine Nanoassemblies With Sustained Antimicrobial Phototherapeutic Action

697 | Jun 08 2020

Roberto Zagami et al. proposed the design and characterization of a novel nanophototherapeutic based on the trade cyclodextrin CAPTISOL® (sulfobutylether-beta-cyclodextrin, SBE-βCD) and 5,10,15,20-tetrakis(1-methylpyridinium-4-yl)porphine tetrakis(p-toluenesulfonate) (TMPyP) to fabricate efficient biocompatible systems for aPDT. [Read the Full Post]

Cell Cycle Arrest and Apoptosis Are Not Dependent on p53 Prior to p53-dependent Embryonic Stem Cell Differentiation

1578 | 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]

Small Molecule JQ1 Promotes Prostate Cancer Invasion via BET-independent Inactivation of FOXA1

654 | May 31 2020

Leiming Wang et al. indicated that JQ1 has an unexpected effect of promoting invasion in prostate cancer. [Read the Full Post]

Rapamycin: An InhibiTOR of Aging Emerges From the Soil of Easter Island

0 | May 24 2020

Sebastian I Arriola Apelo et al. discussed recent advances in understanding the molecular and physiological effects of rapamycin treatment, and they discussed how the use of alternative rapamycin treatment regimens or rapamycin analogs had the potential to mitigate the deleterious side effects of rapamycin treatment by more specifically targeting mTORC1. [Read the Full Post]

Treatment of γ-Hydroxybutyric Acid (GHB) and γ-Butyrolactone (GBL) Overdose with Two Potent Monocarboxylate Transporter 1 (MCT1) Inhibitors, AZD3965 and AR-C155858

1148 | Apr 29 2019

Follman KE et al. indicated that inhibition of MCT1 is an effective treatment for GHB/GBL overdose. SIGNIFICANCE STATEMENT: This research demonstrates the efficacy of a potent MCT1 inhibitor, AZD2965, as a treatment for GHB overdose. AZD3965 was shown to reduce the brain exposure of GHB, and therefore reduce the toxic impact of GHB. This compound may have the potential to be developed to treat GHB overdose clinically. [Read the Full Post]

MicroRNA-24-1 suppresses mouse hepatoma cell invasion and metastasis via directly targeting O-GlcNAc transferase

0 | Jan 14 2019

Liu Y et al. suggested that as a tumor suppressor, miR-24-1 may regulate mouse hepatocarcinoma cells migration and invasion, at least partially through targeting OGT, which could regulate the O-GlcNAcylation and the stability of this oncoprotein c-Myc. This may give insight into a novel mechanism and therapy of tumor lymphatic metastasis. [Read the Full Post]

MicroRNA-24-1 suppresses mouse hepatoma cell invasion and metastasis via directly targeting O-GlcNAc transferase

778 | Jan 14 2019

Liu Y et al. suggested that as a tumor suppressor, miR-24-1 may regulate mouse hepatocarcinoma cells migration and invasion, at least partially through targeting OGT, which could regulate the O-GlcNAcylation and the stability of this oncoprotein c-Myc. This may give insight into a novel mechanism and therapy of tumor lymphatic metastasis. [Read the Full Post]

MicroRNA-24-1 suppresses mouse hepatoma cell invasion and metastasis via directly targeting O-GlcNAc transferase

631 | Dec 17 2018

Liu Y et al. suggested that as a tumor suppressor, miR-24-1 may regulate mouse hepatocarcinoma cells migration and invasion, at least partially through targeting OGT, which could regulate the O-GlcNAcylation and the stability of this oncoprotein c-Myc. This may give insight into a novel mechanism and therapy of tumor lymphatic metastasis. [Read the Full Post]

SIRT1 prevents hyperuricemia via the PGC-1α/PPARγ-ABCG2 pathway

1464 | Dec 17 2018

Wang J et al. demonstrated that SIRT1 and its activator, RSV, have clear anti-hyperuricemia functions in this mouse model. One possible mechanism is the activation of ABCG2 in the ileum through the PGC-1α/PPARγ pathway. [Read the Full Post]

Cytokine correlation analysis based on drug perturbation

0 | Dec 09 2018

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]

Cell-based assay system for high-throughput screening of anti-photo-aging agents in fibroblast transfectants

0 | Dec 07 2018

Lee S et al. revealed that CCN1-GFs treated with sclareol showed decreased levels of UVB-induced CCN1 expression. Sclareol attenuated UVB-induced photo-aging by an increase in collagen synthesis and decrease in MMP-1 activity. [Read the Full Post]

Dihydroartemisinin inhibits TCTP-dependent metastasis in gallbladder cancer

762 | Nov 05 2018

Zhang F et al. provided new insights into the therapeutic activity of Dihydroartemisinin as a treatment for gallbladder cancer metastasis. [Read the Full Post]

Dichloroacetate induces regulatory T-cell differentiation and suppresses Th17-cell differentiation by pyruvate dehydrogenase kinase-independent mechanism

886 | Sep 12 2018

Makita N et al. indicated that Dichloroacetate possesses Treg induction and Th17 suppression, which is independent of PDHK and dependent on ROS production. [Read the Full Post]

Combined treatment with silibinin and either sorafenib or gefitinib enhances their growth-inhibiting effects in hepatocellular carcinoma cells

810 | Sep 07 2018

Gu HR et al. found that the combination of silibinin with either sorafenib or gefitinib could be a useful treatment approach for HCC in the future. [Read the Full Post]

Targeting the Spleen Tyrosine Kinase with Fostamatinib as a Strategy against Waldenström Macroglobulinemia

1788 | Aug 17 2018

Kuiatse I et al. supported the translation of approaches targeting Syk with fostamatinib to the clinic for patients with relapsed and possibly even newly diagnosed WMG. [Read the Full Post]

Cytokine correlation analysis based on drug perturbation

0 | Jul 14 2018

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. [Read the Full Post]

Hepatitis B Virus Middle Protein Enhances IL-6 Production via p38 MAPK/NF-κB Pathways in an ER Stress-Dependent Manner

790 | Jun 05 2018

Li YX et al. provided a possibility that MHBs could be involved in liver disease progression. [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

1665 | May 26 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]

Advanced glycation end products regulate anabolic and catabolic activities via NLRP3-inflammasome activation in human nucleus pulposus cells

0 | May 26 2018

Song Y et al. revealed that accumulation of AGEs in NP tissue may initiate inflammation-related degeneration of the intervertebral disc via activation of the NLRP3 inflammasome. [Read the Full Post]

Knockdown of eIF4E suppresses cell proliferation, invasion and enhances cisplatin cytotoxicity in human ovarian cancer cells

746 | May 25 2018

Wan J, et al. found that knockdown eIF4E gene can be used as a potential therapeutic target for the treatment of human ovarian cancer. [Read the Full Post]

Regulation of glutamate transporter trafficking by Nedd4-2 in a Parkinson's disease model

0 | May 24 2018

Zhang Y et al. indicated that Nedd4-2 may serve as a potential therapeutic target for the treatment of PD. [Read the Full Post]

The neuroprotection of Sinomenine against ischemic stroke in mice by suppressing NLRP3 inflammasome via AMPK signaling

710 | Apr 12 2018

Qiu J et al. demonstrated that SINO exerts a neuroprotective effect in ischemic stroke by inhibiting NLRP3 inflammasomes via the AMPK pathway, which also provides evidence of a novel treatment for clinical stroke therapy. [Read the Full Post]

Induction of p53-independent apoptosis by ectopic expression of HOXA5 in human liposarcomas

811 | Apr 04 2018

Lee DH et al. demonstrated for the first time that the downregulation of HOXA5 in LPS cells, partly by overexpression of miR-26a-2 in DDLPS, confers LPS cells resistance to apoptotic death. [Read the Full Post]

Sensitivity of Human Intrahepatic Cholangiocarcinoma Subtypes to Chemotherapeutics and Molecular Targeted Agents: A Study on Primary Cell Cultures

843 | Mar 21 2018

Fraveto A et al. identified a dual PI3-kinase/mTOR inhibitor that both in vitro and in vivo, exerts dramatic antiproliferative effects against both mucin- and mixed-IHCCA. [Read the Full Post]

tRNA modification profiles of the fast-proliferating cancer cells

0 | Oct 06 2017

Dong C et al. indicated that tRNA is a actively regulated RNA species in the fast-proliferating cancer cells, and suggest that they may play a more active role in biological process than expected. [Read the Full Post]

The serum and glucocorticoid-regulated protein kinases (SGK) stimulate bovine herpesvirus 1 and herpes simplex virus 1 productive infection

0 | Jul 29 2017

Kook I et al. suggest SGK may stimulate viral replication following stressful stimuli. [Read the Full Post]

Endoplasmic reticulum stress in mouse decidua during early pregnancy

0 | Apr 01 2017

Xiao Wei Gu et al showed that ER stress induces DNA damage and polyploidization in stromal cells. In conclusion, our data suggest that the GRP78/Ire1/Xbp1 signaling pathway of ER stress-UPR is activated and involved in mouse decidualization. [Read the Full Post]

Silymarin improved diet-induced liver damage and insulin resistance by decreasing inflammation in mice

1282 | Mar 24 2017

Guo Y et al. suggested that silymarin-induced alleviation of inflammatory response could be a mechanism responsible for its benefits against liver damage and insulin resistance. [Read the Full Post]

Autophagy dysfunction upregulates beta-amyloid peptides via enhancing the activity of γ-secretase complex

1796 | Mar 08 2017

Cai Z et al. found that autophagy inhibitor may activate γ-secretase and promote Aβ production and accumulation, but has no influence on Aβ clearance. [Read the Full Post]

Antiviral activity of micafungin against enterovirus 71

0 | Mar 04 2017

Kim C et al. revealed a new indication of micafungin as an effective inhibitor of EV71, which is the first case reporting antiviral activity of micafungin, an antifungal drug. [Read the Full Post]

Metformin regulates differentiation of bone marrow-derived endothelial progenitor cells via multiple mechanisms

1408 | Feb 23 2017

Li WD, et al.'s results here showed that metformin could regulate the differentiation of EPCs. Autophagy related pathway and AMPK-eNOS-NO pathway were involved in the mechanisms. [Read the Full Post]

Exploring simvastatin, an antihyperlipidemic drug, as a potential topical antibacterial agent

0 | Feb 22 2017

Thangamani S, et al.'s study lays the foundation for further investigation of repurposing simvastatin as a topical antibacterial agent to treat skin infections. [Read the Full Post]

Repurposing celecoxib as a topical antimicrobial agent

0 | Feb 21 2017

Thangamani S, et al.'s results demonstrate that celecoxib alone, or in combination with traditional antimicrobials, has a potential to use as a topical drug for the treatment of bacterial skin infections. [Read the Full Post]

Anidulafungin-Induced Suicidal Erythrocyte Death

0 | Feb 18 2017

Anidulafungin triggers hemolysis and eryptosis with cell shrinkage and phospholipid scrambling of the erythrocyte cell membrane, an effect in part due to Ca2+ entry and activation of p38 kinase. [Read the Full Post]

Antiviral activity of micafungin against enterovirus 71

0 | Jan 21 2017

The research of Kim C et al. revealed a new indication of micafungin as an effective inhibitor of EV71, which is the first case reporting antiviral activity of micafungin, an antifungal drug. [Read the Full Post]

Exploring simvastatin, an antihyperlipidemic drug, as a potential topical antibacterial agent

1729 | Jan 12 2017

The study of Thangamani S et al. lays the foundation for further investigation of repurposing simvastatin as a topical antibacterial agent to treat skin infections. [Read the Full Post]

Metformin regulates differentiation of bone marrow-derived endothelial progenitor cells via multiple mechanisms

1295 | Jan 12 2017

Li WD, et al.'s results here showed that metformin could regulate the differentiation of EPCs. Autophagy related pathway and AMPK-eNOS-NO pathway were involved in the mechanisms [Read the Full Post]

Repurposing celecoxib as a topical antimicrobial agent

2160 | Jan 11 2017

Thangamani S, et al.'s results demonstrate that celecoxib alone, or in combination with traditional antimicrobials, has a potential to use as a topical drug for the treatment of bacterial skin infections. [Read the Full Post]

Glucose Metabolism and AMPK Signaling Regulate Dopaminergic Cell Death Induced by Gene (α-Synuclein)-Environment (Paraquat) Interactions

1480 | Dec 26 2016

Anandhan A et al. demonstrated that glucose metabolism and AMPK regulate dopaminergic cell death induced by gene (α-synuclein)-environment (PQ) interactions. [Read the Full Post]

The serum and glucocorticoid-regulated protein kinases (SGK) stimulate bovine herpesvirus 1 and herpes simplex virus 1 productive infection

1632 | Dec 13 2016

Kook I et al.’s studies suggested that SGK may stimulate viral replication following stressful stimuli. [Read the Full Post]

Antiviral activity of micafungin against enterovirus 71

3302 | Dec 10 2016

The research of Kim C et al. revealed a new indication of micafungin as an effective inhibitor of EV71, which is the first case reporting antiviral activity of micafungin, an antifungal drug. [Read the Full Post]

Cannabinoid receptor-2 stimulation suppresses neuroinflammation by regulating microglial M1/M2 polarization through the cAMP/PKA pathway in an experimental GMH rat model

2124 | Nov 23 2016

The results of Tao Y et al. will help to further understand the mechanisms that underlie neuroprotection by CB2R in GMH and promote clinical translational research for CB2R agonists. [Read the Full Post]

tRNA modification profiles of the fast-proliferating cancer cells

2131 | Nov 22 2016

Dong C et al.'s results indicated that tRNA is a actively regulated RNA species in the fast-proliferating cancer cells, and suggest that they may play a more active role in biological process than expected. [Read the Full Post]

Anidulafungin-Induced Suicidal Erythrocyte Death

3175 | Nov 09 2016

Anidulafungin triggers hemolysis and eryptosis with cell shrinkage and phospholipid scrambling of the erythrocyte cell membrane, an effect in part due to Ca2+ entry and activation of p38 kinase. [Read the Full Post]

Nitric oxide generation by the organic nitrate NDBP attenuates oxidative stress and angiotensin II-mediated hypertension

2483 | Oct 26 2016

Porpino SK et al. suggested that NDBP treatment is associated with sustained NO release and attenuated activity of NADPH oxidase, which to some extent requires functional xanthine oxidase. [Read the Full Post]

The effect of hyperlipidemia on the pharmacokinetics, hepatic and pulmonary uptake of posaconazole in rat

2036 | Oct 18 2016

Khalil HA et al. found that poloxamer induced lipoprotein level elevation caused alterations in the PSZ pharmacokinetics and decreased its hepatic and pulmonary uptake. [Read the Full Post]

Endoplasmic reticulum stress in mouse decidua during early pregnancy

1786 | Sep 06 2016

Xiao Wei Gu, et al. suggested that the GRP78/Ire1/Xbp1 signaling pathway of ER stress-UPR is activated and involved in mouse decidualization. [Read the Full Post]

The role of heat shock protein beta-1 in erastin-induced ferroptosis

4737 | 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]

STIM2 promotes store-operated calcium entry via enhancing recruitment of STIM1 to the ER-PM junctions

2556 | Jan 26 2015

Ong et al. found STIM2 promotes STIM1 recruitment in endoplasmic reticulum- plasma membrane junctions at low stimulus intensities, results in the enhancement of store-operated calcium entry. [Read the Full Post]

Snail also acts as a transactivator for the expression of tumor-associated cytokines

7024 | Jan 16 2015

Hsu et al. demonstrated the underlying mechanism of Snail-mediated target gene transactivation, and also identified several target genes. [Read the Full Post]

An unusual mechanism of ERBB4 in regulating tumor related gene expression

9833 | Jan 06 2015

Haskins et al. found ERBB4 activated the transcriptional coactivator YAP by binding to its ligand neuregulin 1 (NRG1), to regulate gene expression of cancer cells. [Read the Full Post]

Resvertrol targets a human tRNA synthetase for activation of NAD+-dependent PARP1

5689 | Jan 05 2015

Mathew Sajish and Paul Schimmel found resvertrol interacts with tyrosyl transfer-RNA (tRNA) synthetase (TyrRS), which translocates to the nucleus in response to stress, to initiating its effect in nuclear. [Read the Full Post]

Retinoic acid and Wnt signaling are key regulators in development of hematopoietic stem cells

6679 | Dec 02 2014

Chanda et al. identified retinoic acid (RA) and Wnt signaling pathways as key mediators of HSC development. [Read the Full Post]

Docetaxel is a clinically well established anti mitotic chemotherapy medication

2666 | Dec 25 2013

Docetaxel, an analog of taxol, is an inhibitor of depolymerisation of microtubules through binding to stabilized microtubules. [Read the Full Post]

Salubrinal is a drug which acts as a specific inhibitor of eIF2a

3411 | Dec 11 2013

Salubrinal is a selective inhibitor of cellular complexes that dephosphorylate eukaryotic translation initiation factor 2 subunit α (eIF2α). [Read the Full Post]

AM803 is under development as an oral controller for the treatment

2639 | Oct 25 2013

GSK2190915 (AM803), a potent FLAP inhibitor, prevents the synthesis of leukotrienes and 5-oxo-ETE, with IC50 of 76 nM for inhibition of LTB4 in human blood, provides treatment for asthma. [Read the Full Post]

LY2886721 is used to treat Alzheimers Disease in preclinical experiments

2723 | Aug 23 2013

LY2886721 is an BACE inhibitor used for the treatment of Alzheimer's Disease. [Read the Full Post]

AMG517 is a potent and selective transient receptor potential TRPV1 antagonist

2633 | Jul 31 2013

Oral administration of AMG 517 produces a dose-dependent increase in plasma concentrations, it also produces a dose-dependent decrease in the number of flinches induced by capsaicin treatment. [Read the Full Post]

HIGH THROUGHPUT SCREENING HELPING THE DRUG DISCOVERY

3982 | Oct 14 2012

HIGH THROUGHPUT SCREENING: INTRODUCTION: In pharmaceutical industries different techniques are important and used for the novel drug discovery. Among these techniques the most effective one in this area is high throughput chemical screening. It is also named as HTS assays or high throughput assays which are being used for the biological, pharmacological assessment or the assessment of biochemical activities of a large number of drugs by the help of the latest automatic technology. Such technology is not only helpful in discovery of appropriate receptors, enzymes, ligands for different ion channels and the other pharmacologically important targets but also used in the extensive studies of various desired biochemical or cellular pathways by the aid of unknown and novel chemical agents. Regarding this an important example is of the screening of kinase inhibitor library for screening that is much easier than various other traditional methodologies. Reviews of high throughput screening are an efficient source of acknowledging the importance of HTS. These reviews reveal the speed and accuracy of high throughput screening in the pharmaceutical industries in improving the scientific approaches and business structures. [Read the Full Post]

KINASE INHIBITORS IN CANCER THERAPY

3634 | Oct 10 2012

KINASES IN CELL SIGNALLING: Kinases can rightly be called as the gateways of the cells due to their role in signal transduction in the cell. They function by activating or stimulating the critical pathway by phosphorylating the protein molecules. After getting stimulated enzymes allow the cells to perform some specific functions necessary for its proliferation, survival and growth etc. kinases are of many types which are Receptor tyrosine kinases (RTKs), non-receptor tyrosine kinases (NRTKs) and serine/threonine kinases. Mixed kinases and histidine kinases are also some of the examples of kinases. Basically kinases themselves get activated by a signaling molecule like a ligand from the extracellular environment or some other kinases and further activate subsequent molecule by phosphorylating or dephosphorylating them. Aurora kinase is an important example of kinase enzymes. Different types of agonist and antagonist molecules are used to study and unveil different functions of kinases in the cells. Kinase inhibitor is one of the examples of outcomes of such research on kinases and their inhibition. Different types of kinase assays are also there to study and analyze some specific kinds of kinases. [Read the Full Post]

DRUG DISCOVERY AND COMPOUND LIBRARIES

3961 | Sep 29 2012

INTRODUCTION: A large number of compounds stored for the purpose of discovering something beneficial and more efficient we are looking for is known as compound library screening. A compound library is constructed for the purpose of drug discovery and is screened for the best drug by high through put screening techniques of recent era. Compounds included in the library are fully organized by a specific database system containing information about the compounds and their related properties like purity, chemical structure, physical, chemical and pharmacological properties, and the preparation of that compound . Lots of libraries of different compounds are available commercially that contain different common or unique type of biochemical compounds. Description of these compounds and complete information is available in a file named research chemical library which can be bought from the suppliers of relevant compound libraries. [Read the Full Post]

COMPOUND LIBRARIES AND THEIR USAGE

3654 | Sep 25 2012

COMPOUND LIBRARY: A compound library is like a library of books where different titles and different content is available at a single place. Storage of compounds and their related data makes a compound library where different compounds are collected and arranged for some specific purposes. The compound screening of the library are placed, maintained and stored in a very scientific way. Drug discovery is one of the major purposes of making compound libraries. Recent technologies to organize and design chemical compound library have made the process of drug discovery a more interesting and attractive research area for the scientists and remarkable successes have been seen after the fast growing technologies have made its research easier. The most important thing after construction of compound library is its screening that is looking for the best suited compound relevant to question we are seeking the answer for and the compound that is biologically more active. [Read the Full Post]

KINASES INHIBITION FOR CANCER THERAPY

3499 | Sep 24 2012

SIGNALING THROUGH KINASES: Kinase enzymes are the protein phosphorylating enzymes which act as gateways for the transmission of metabolic signals from the extracellular to intracellular environment of the cell. Kinases stimulate the cells to perform the processes which are necessary for the cell survival, proliferation and cell growth etc. Many types of kinase enzymes exist in the cells like serine/threonine kinases, receptor tyrosine kinases and non-receptor tyrosine kinases, Histidine kinases and the mixed kinases. Basic mechanism of action of kinase proteins is to aquire activated state by some sort of signaling compound that can be a special ligand or some other kind of kinase and send the stimulus to the subsequent molecule in form of its dephosphorylation or phosphorylation. One of the important examples of such kinases is p38 MAP kinase. [Read the Full Post]

HIGH THROUGHPUT SCREENING AND DRUG DISCOVERIES

0 | Sep 19 2012

INTRODUCTION: Various techniques are important in pharmaceutical industries which are used for the discovery of novel drugs, one of the most effective technique in this field is high throughput screening. This is also known as high throughput assay or HTS assays which are utilized for the assessment of pharmacological, biological or biochemical activities of a huge number of drugs by the aid of latest and automatic technology. This technique is not only useful for the discovery of appropriate ligands for ion channels, receptors, enzymes and other important pharmaceutical targets but also used for extensive studies of biochemical or desired cellular pathways by the help of novel and unknown chemical molecules. In this regard an example is of screening of kinase inhibitor library which is quiet easier than many traditional methodologies. High throughput screening reviews are an efficient source of understanding the importance of HTS screening, these reviews describe the accuracy and speed of the HTS screening in pharmaceutical industries in terms of business improvement structures and scientific approaches. [Read the Full Post]

KINASE INHIBITORS AND CANCER THERAPY

3425 | Aug 23 2012

KINASE-DOWNSTREAM SIGNALING: Kinases act as windows for cells to the outer world, these enzymes are triggered by the signals coming from other cells, stimuli from the environment and as a result these kinases carry out phosphorylaiton of various molecules to transmit downstream signals. There are many types of kinase enzymes such as pim kinase and out of these most common are protein kinases. These protein kinases can also be further subdivided into various categories like receptor tyrosine kinase enzyme, threonine/serine protein kinases, mixed kinases and histidine protein kinases. Many of the kinase agonists and kinase antagonists have been employed for the understanding of multiple cellular pathways during research under physiological environment. Reviews on kinase inhibitors can prove the importance of these small compounds. There are various kinase assays are available which can be used for the activity assessment of a kinase enzyme in a given state. [Read the Full Post]

COMPOUND LIBRARY AND ITS BENIFITS

3510 | Aug 21 2012

THE BASIC CONCEPT OF COMPOUND LIBRARY: The collection of data about different compounds at a place where all these compounds can be analyzed by the good worth of their storage is known as a compound library. Hence compound library is basically a collection or arrangement of different compounds. The maintenance, storage and placing of these screening compounds is actually a proper scientific way. The development of different new and emerging technologies in designing and managing of a chemical screening library has brought very remarkable success and changes in the procedure of drug discovery and these new changes have a great and positive impact on the ongoing research on drug discovery [1]. The most determining and crucial step in this procedure of compound library screening is the selection of biologically relevant and useful compounds and molecules that is usually guided by some experts of this area who would must devise some detailed protocols and schemes to make this process of selection faster, more efficient and better than ever in generating a resourceful research chemicals library. State-of-the-art methodologies that include both the fragment-based library designing and the structure-based small molecule library designing procedure is supported by the latest and efficient software tools which ensure a promising implementation of a small molecule drug screening library. [Read the Full Post]

COMPOUND LIBRARIES AND THEIR ADVANTAGES

4403 | Aug 19 2012

COMPOUND LIBRARIES: INTRODUCTION AND FUNCTIONS A fair to a big group of the stored compounds which can be used for industrial manufacturing of drugs or the high-throughput screening assay based drug discovery, is defined as a compound library. This collection or group of compounds is supported by the specific kind of database that contains the relevant information and knowledge about the included compounds and that information includes the compound’s purity, preparation, chemical structure, chemical, physical and pharmacological properties [1]. A lot of compound libraries are commercially available and they might contain a mixture of some common or some unique biochemical compounds. A detailed file containing the complete information regarding the compounds is presented in the research chemical library and this file is purchasable from the relevant suppliers. These compound libraries are most advantageous in the high throughput screening assays in which the target of a drug is screened against a number of different compounds that are taking space in the library. More the number of compounds in a compound library more are the chances of getting a ‘hit’ in screening compound procedure. [Read the Full Post]

INHIBITION OF KINASES IN CANCER THERAPY

2680 | Aug 08 2012

SIGNALING VIA KINASES: Kinases are protein phosphorylating enzymes that function as gateways for the transmission of signals from extracellular to intracellular world of the cell. They stimulate the cells to carry out processes necessary for their survival, growth and proliferation etc. Different types of kinases are there in the cell for example; receptor tyrosine kinases, non-receptor tyrosine kinases, serine/threonine kinases, Histidine kinases and mixed kinases. The basic mode of action of kinases is to get activated by a signaling compound that may be a ligand or any other kinase and transmit the message to the next molecule in the form of its phosphorylation or dephosphorylation. MAP kinase is also one of the examples of such kinases. Different agonists and antagonists are there that can be used for studying the role of kinases in cell signaling. Development and production tyrosine kinase inhibitor is one of the advantages of such small compounds. Kinase assays are also there that can be used for the analysis of activity of a particular kinase in specific state. [Read the Full Post]

HIGH THROUGHPUT SCREENING IN DRUG DISCOVERIES

3694 | Jul 18 2012

HIgh throughput screening: For the treatment of life taking diseases such as cancers are always in a need to be treated with novel therapeutics, in order to full fill this task many techniques are accepted. High throughput screening is found as the most remarkable strategy in order to discover new potent drugs. Another name of this technique is High throughput screening assay and this technique is being developed more and more due to latest automatic machines which also ensures its accuracy and speed. For a drug discovery High throughput screening works under pharmaceutical, biological or biochemical environment to find out the ability of drug against specific disease. Mostly the novel drug is based on the properties of any ligand, specific receptor, peptides enzymes or ion channels involved in a specific disease condition. This is a technique with dual benefits as there is another use of high throughput screening is the detection of various pathways which are potential for specific diseases. Screening libraries of kinases is one of the most important examples of high throughput screening as compared to old techniques. [Read the Full Post]

ROLE OF HIGH THROUGHPUT SCREENING IN DRUG DISCOVERIES

3561 | Jun 07 2012

INTRODUCTION: High throughput screening is one of the novel and leading technique for the discoveries of new pharmaceutical agents for the treatment of various lethal diseases. This famous technique is also called as the High throughput screening assay, this technique has been so impressive and fast due to the advancements in automatic machines. This technique is based on the properties of different chemical agents for their ability under pharmaceuticals, biochemical and biological actions against any disorder. In the era of drug discovery this technique has been proved as the most effective for the treatment of specific diseases and these treatments are based on the drugs discovered as ligands for receptors, enzymes, proteins and ion channels. High throughput screening is also used for the detection and study of cellular or biochemical pathways for the assessment of the certain therapeutics for respective cellular mechanisms. The major example includes screening library of kinases and this is leading applied example in this regard in comparison to old methods. The importance of High throughput screening can be analyzed by studying reviews of this novel method for discovering new drugs. Business of pharmaceuticals and science and research has been greatly benefited by this method. [Read the Full Post]

HIGH THROUGHPUT SCREENING AND DRUG DISCOVERIES

3695 | May 08 2012

INTRODUCTION: In pharmaceutical industries a famous technique for discovering novel therapeutics is called as High throughput screening. This is also known as High throughput screening assay, various drugs or chemical compounds are analyzed for their potency with respect to their biological, biochemical or pharmaceutical actions by the help of unique and advanced techniques based on automatic machines. This assay has been proven as one of the most effective way of discovering new drugs against specific diseases; examples are enzyme proteins, ligands for various receptors as well as ion channels and a huge number of other pharmaceutical targets. In addition to this application High throughput screening is also being applied for the verification or detection of different biochemical or cellular mechanisms which are under investigations for therapeutic purposes such as inhibitors for different cellular pathways. [Read the Full Post]

NOVEL DRUGS AND HIGH THROUGHPUT SCREENING

2097 | Apr 09 2012

INTRODUCTION: High throughput screening assay is well known technique in pharmaceutical industries and having fame due to its role in novel drug discoveries. This is also abbreviated as high throughput screening assay, by the help of this technique or assay a good number of compounds like drugs are assessed with reference to their biochemical, biological or pharmacological activities by the aid of new automatic technologies. High throughput screening has not only proven to be effective in the field of new therapeutic agents like ligands for different receptors, enzyme proteins, ion channels and many other pharmaceutical targets, But this screening technique is also being used for profiling a cellular or biochemical pathway of interest for therapeutic targeting of this pathway by unknown compounds. The one of best example is screening libraries of kinases which are now much easier way as compared to old methods. In order to understand the value of high throughput screening one should look at reviews of this technique where accuracy and speed are the main tools which have brought the improvement in scientific research and also in the business of pharmaceutical world. [Read the Full Post]

COMPOUND LIBRARY

2537 | Apr 08 2012

INTRODUCTION OF COMPOUND LIBRARY: A pool of various compounds in a position where all these compounds can be evaluated because of the high merit of their scientific storeroom is known as a compound library. Hence compound libraries are collections of various compounds. In these libraries storage, maintenance and placing is done in a scientific way. The evolution of different new technologies in managing and designing a chemical library led to some of remarkable drug discoveries, as these libraries provide a positive procedure for research. The selection criteria for biologically active and relevant compounds and chemicals includes a huge set of synthesizable chemicals, it is an important and crucial part of research and usually needs the guidance of experts in the relevant field. These experts formulate schemes and protocols which make the selection faster and efficient than a practical chemical library. [Read the Full Post]

COMPOUND LIBRARY AND ITS UTILITY

2649 | Mar 19 2012

Introduction: The concept With the advent of the computer age a different style of thinking came into play. Technology changed the way in which scientists approached things but did not alter the rationale behind the objective. In the medical field the pressure to discover new medical treatments became a financial one rather than a humanitarian one. Pharmaceutical companies made and lost huge sums of money speculating on the potential use of a molecule for clinical purposes. To regulate all of this the USA formed the “federal drug administration” or FDA, while Europe developed the EMA. Strict rules and codes of conducted made the release of new pharmaceuticals more difficult but gave the public a greater sense of security. Pharmaceutical companies found that discovering new molecules under these rules to be an expensive proposition compared to the profits they received from the marketing the drug. Hence the competition to get a drug to the market first and claim a “lions share” of the potential profits has become the guiding rule behind drug development. Every aspect of the discovery process has been streamline to the minimize costs and every labor saving device employed to decrease expenses and increase profits. The initial stage of drug developed is the selection of a molecule or a series of molecules with biological activity. [Read the Full Post]

HIGH THROUGHPUT SCREENING FOR NEW DRUGS

4653 | Mar 18 2012

In terms of medical discovery the cost represented to a drug developing pharmaceutical company is immense; hundreds of millions of dollars can be spent in developing a new medical treatment for molecular identification to final registration after clinical trials. The “magic number” introduced in 2003 by a group of economists was $802 000 000 per new drug reaching final approval. This number has been challenged [3] but still it represents the huge financial commitment pharmaceutical companies have to make. If the drug makes it through to phase III clinical trials or even registration it can still fail due to a variety of reasons (mostly safety) and have to be withdrawn, the biggest examples of this are Vioxx (2007, Merck&co) and Thalidamide (1957, Chemie Grunenthal). The total costs to these two companies for these drugs have never been documented but it has been estimated as to be in billions. [Read the Full Post]

COMPOUND LIBRARIES AND THEIR USES

2657 | Mar 18 2012

Introduction: Concept Drug design and discovery does not happen by chance but is a process of active searching by individual scientists. Often a template molecule (of proven biological activity) will be taken and systematically altered in small ways to generate whole series of structurally related compounds. These compounds can then be either tested against the original target disease or screened against a panel of diseases to find those molecules which processes biological activity. This process is extremely labor intensive and any means by which the cost of the search or the testing for activity can reduced is actively sort. A compound library is such a labor reducing facility. A simple library will consist of information regarding properties of a number of compounds; this could include such things as structure, physical properties, chemical properties, purities or even synthesis patterns. A more complex library could be would consists if small amounts of actual compounds in known concentrations accompanied by all the known physical and chemical properties. This type library can be for the high through put screening for compounds of interest, whether they be of biological importance or synthetic chemical importance. [Read the Full Post]