Methylation

Discovery of potent DNMT1 inhibitors against sickle cell disease using structural-based virtual screening, MM-GBSA and molecular dynamics simulation-based approaches

181 | Jan 25 2024

The study's rigorous virtual screening and molecular dynamics simulations identified promising compounds with potential to inhibit DNMT1, offering a hopeful avenue for improving sickle cell disease treatment pending further in vitro and in vivo validation. [Read the Full Post]

MRTX1719 Is an MTA-Cooperative PRMT5 Inhibitor That Exhibits Synthetic Lethality in Preclinical Models and Patients with MTAP-Deleted Cancer

199 | Jan 24 2024

MRTX1719, a selective PRMT5 inhibitor, displays remarkable efficacy against MTAP-deleted cancers while sparing MTAP wild-type cells, showcasing promising therapeutic potential and early clinical success across a spectrum of malignancies. [Read the Full Post]

Evaluation of Histone Demethylase Inhibitor ML324 and Acyclovir against Cyprinid herpesvirus 3 Infection

0 | Jan 03 2024

ML324 demonstrates significant potential as an effective treatment against Cyprinid herpesvirus 3 (CyHV-3) infection in koi fish, outperforming traditional antiviral drugs like acyclovir in inhibiting virus replication both in vitro and in vivo. [Read the Full Post]

Conformational-Design-Driven Discovery of EZM0414: A Selective, Potent SETD2 Inhibitor for Clinical Studies

243 | Dec 25 2023

The evolution from a novel SETD2 inhibitor tool compound to the potent and orally bioavailable EZM0414 marks a significant achievement in drug development, promising potential clinical implications for conditions like multiple myeloma featuring a t(4,14) translocation. [Read the Full Post]

Medicare's Hospital Readmission Reduction Program reduced fall-related health care use: An unexpected benefit?

129 | Dec 21 2023

The study found that Medicare's Hospital Readmissions Reduction Program (HRRP) was associated with significant reductions in severe fall-related injuries, particularly for congestive heart failure and pneumonia patients, indicating potential improvements in transitional care and post-acute referral patterns. [Read the Full Post]

Effect of feed enriched by products formulated from coconut water, palm sap sugar, and mushroom on the chemical composition of feed and carcass, growth performance, body indices, and gut micromorphology of giant gourami, Osphronemus goramy (Lacepède, 1801), juveniles

70 | Dec 05 2023

The study found that the formulation KP3, incorporating palm sap sugar, coconut water, and specific microorganisms, significantly improved the nutrition, growth, and body composition of giant gourami juveniles, making it a promising option for aquaculture in Indonesia. [Read the Full Post]

ALKBH5 causes retinal pigment epithelium anomalies and choroidal neovascularization in age-related macular degeneration via the AKT/mTOR pathway

185 | Dec 02 2023

ALKBH5 upregulation in age-related macular degeneration leads to retinal pigment epithelium dysfunction and choroidal neovascularization through its demethylation activity, activating the PIK3C2B-mediated AKT/mTOR pathway, and pharmacological inhibitors like IOX1 offer potential therapeutic interventions. [Read the Full Post]

Lysin (K)-specific demethylase 1 inhibition enhances proteasome inhibitor response and overcomes drug resistance in multiple myeloma

203 | Nov 20 2023

The study demonstrates that inhibiting lysine-specific demethylase 1 (LSD1) synergizes with proteasome inhibitors, such as carfilzomib, overcoming drug resistance in multiple myeloma and other B-cell malignancies, offering a promising therapeutic strategy. [Read the Full Post]

Inhibiting SETD7 methyl-transferase activity impairs differentiation, lipid metabolism and lactogenesis in mammary epithelial cells

198 | Nov 19 2023

Inhibiting SETD7 catalytic activity using (R)-PFI-2 disrupts mammary epithelial cell differentiation by increasing proliferation, downregulating differentiation markers, and altering lipid metabolism. [Read the Full Post]

Evaluation of Histone Demethylase Inhibitor ML324 and Acyclovir against Cyprinid herpesvirus 3 Infection

363 | Nov 16 2023

ML324, a specific inhibitor of JMJD2 histone demethylase, has demonstrated promising potential as a treatment against CyHV-3 infection in koi fish, effectively inhibiting viral replication both in vitro and in vivo. [Read the Full Post]

Novel small molecule inhibitors of the transcription factor ETS-1 and their antitumor activity against hepatocellular carcinoma

182 | Nov 08 2023

This study identified four novel small molecule inhibitors of the transcription factor ETS-1, demonstrating their potential to suppress HCC cell proliferation and invasion, offering safer and more effective therapeutic strategies for hepatocellular carcinoma. [Read the Full Post]

Relationship among cattle breed and anabolic implant protocol relative to feedlot performance: Growth, temperament, feeding behavior, carcass traits, and economic return

170 | Oct 24 2023

The study found that a moderate intensity anabolic implant protocol was optimal for feedlot steers of different breed types, resulting in increased average daily gain and higher net return per head compared to non-implanted and high intensity implant groups in a temperate climate. [Read the Full Post]

PRMT3 drives glioblastoma progression by enhancing HIF1A and glycolytic metabolism

193 | Oct 11 2023

PRMT3 promotes the progression of glioblastoma by enhancing HIF1α-mediated glycolysis and metabolic rewiring, presenting a potential therapeutic target for treating malignant gliomas. [Read the Full Post]

The Functional Role and Regulatory Mechanism of FTO m6A RNA Demethylase in Human Uterine Leiomyosarcoma

344 | Oct 08 2023

In summary, the study highlights the aberrant upregulation of FTO m6A RNA demethylase in uterine leiomyosarcoma tissues and demonstrates that inhibiting FTO with Dac51 can significantly decrease uLMS cell proliferation, modulate key pathways, and potentially offer a novel therapeutic strategy for this aggressive uterine cancer. [Read the Full Post]

Targeting of epigenetic co-dependencies enhances anti-AML efficacy of Menin inhibitor in AML with MLL1-r or mutant NPM1

158 | Sep 15 2023

Pre-clinical studies demonstrate that monotherapy with a Menin inhibitor (MI) induces clinical remissions in some relapsed/refractory AML patients, but the combination of MI with inhibitors targeting BRD4, MOZ, LSD1, or CBP/p300 shows synergistic effects and superior efficacy, suggesting potential strategies to overcome therapy resistance and prevent relapse. [Read the Full Post]

Automated CUT&Tag profiling of chromatin heterogeneity in mixed-lineage leukemia

216 | Sep 10 2023

This study utilizes automated chromatin profiling techniques to map fusion-specific targets of KMT2A oncofusion proteins, revealing aberrant chromatin regulation and potential therapeutic vulnerabilities in acute myeloid and lymphoid leukemias. [Read the Full Post]

Dual inhibition of EZH1/2 induces cell cycle arrest of B cell acute lymphoblastic leukemia cells through upregulation of CDKN1C and TP53INP1

311 | Sep 09 2023

The study demonstrates that the EZH1/2 dual inhibitor DS-3201 (valemetostat) shows significant antitumor effects against B cell acute lymphoblastic leukemia (B-ALL) by inhibiting cell growth, inducing cell cycle arrest and apoptosis, and upregulating CDKN1C and TP53INP1 expression, offering a potential treatment option for B-ALL. [Read the Full Post]

[LLY-283 inhibits proliferation and metastasis of head and neck squamous cell carcinoma by targeting PRMT5]

169 | Sep 05 2023

LLY-283, by inhibiting PRMT5 expression, effectively suppresses the proliferation and metastasis of Head and Neck Squamous Cell Carcinoma (HNSCC) and reduces tumor growth in vivo. [Read the Full Post]

Phase 1 study of GSK3368715, a type I PRMT inhibitor, in patients with advanced solid tumors

143 | Sep 03 2023

The Phase 1 study of GSK3368715, a reversible inhibitor of type I protein methyltransferases, was terminated early due to a higher-than-expected incidence of thromboembolic events, limited target engagement at lower doses, and lack of observed clinical efficacy. [Read the Full Post]

Anti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715, Synergizes with PRMT5 Inhibition through MTAP Loss

155 | Sep 03 2023

GSK3368715, a potent type I PRMT inhibitor, demonstrates anti-tumor effects and its combination with PRMT5 inhibition and consideration of MTAP status as a biomarker strategy show promise for effective oncology treatment. [Read the Full Post]

m6A demethylase FTO renders radioresistance of nasopharyngeal carcinoma via promoting OTUB1-mediated anti-ferroptosis

215 | Aug 31 2023

The upregulation of the m6A mRNA demethylase FTO in radioresistant nasopharyngeal carcinoma (NPC) promotes radiotherapy resistance by inhibiting radiation-induced ferroptosis, suggesting FTO as a potential therapeutic target and prognostic biomarker for NPC. [Read the Full Post]

Inhibiting Histone and DNA Methylation Improves Cancer Vaccination in an Experimental Model of Melanoma

188 | Aug 28 2023

The study demonstrated that a dual inhibitor targeting histone methyltransferase G9a and DNA methyltransferases (DNMTs) induced tumor cell cycle arrest, apoptosis, and an IFN-I response, while promoting dendritic cell and T-cell infiltration, ultimately increasing the overall survival of mice with melanoma in combination with TCR-redirected T-cell therapy and dendritic cell vaccination. [Read the Full Post]

JNJ-64619178 radiosensitizes and suppresses fractionated ionizing radiation-induced neuroendocrine differentiation (NED) in prostate cancer

257 | Aug 15 2023

The study demonstrates that JNJ-64619178 inhibits DNA damage repair, radiosensitizes prostate cancer cells, and suppresses FIR-induced neuroendocrine differentiation, suggesting its potential as a therapeutic agent for enhancing the effectiveness of radiation therapy in prostate cancer treatment. [Read the Full Post]

EZH2 presents a therapeutic target for neuroendocrine tumors of the small intestine

181 | Jul 30 2023

The study suggests that targeting the EZH2 histone methyltransferase with inhibitors like CPI-1205 and utilizing metformin may hold promise as potential therapeutic options for patients with small intestinal neuroendocrine tumors (SI-NETs). [Read the Full Post]

Prototropic forms of hydroxy derivatives of naphthoic acid within deep eutectic solvents

169 | Jul 29 2023

The prototropic behavior of probes in deep eutectic solvents (DESs) is strongly influenced by the varying hydrogen-bonding capabilities of the DES constituents, as observed through the presence or absence of specific prototropic forms of the probes in different DES compositions. [Read the Full Post]

TP53 mutations and RNA-binding protein MUSASHI-2 drive resistance to PRMT5-targeted therapy in B-cell lymphoma

262 | Jul 18 2023

The proposed therapeutic strategy in lymphoma combines PRMT5 inhibition with either MSI2 or BCL-2 inhibition, leveraging the synergistic effects observed to potentially enhance therapeutic efficacy. [Read the Full Post]

Prmt1 upregulated by Hdc deficiency aggravates acute myocardial infarction via NETosis

151 | Jul 18 2023

The study reveals that histidine decarboxylase deficiency in mice leads to disorderly recruitment of neutrophils, enhanced migration and ROS/NETs production, promoting cardiac damage, but treatment with histamine or PRMT1 inhibitors attenuates these effects, suggesting potential therapeutic strategies for cardiovascular disease. [Read the Full Post]

The pattern of histone H3 epigenetic posttranslational modifications is regulated by the VRK1 chromatin kinase

0 | Jul 16 2023

The chromatin kinase VRK1 plays a crucial role in regulating the epigenetic patterns of histone H3 acetylation and methylation, thereby influencing chromatin organization and associated nuclear functions. [Read the Full Post]

Regulation, genomics, and clinical characteristics of cuproptosis regulators in pan-cancer

294 | Jul 16 2023

This study comprehensively elucidated the expression, prognostic significance, biological functions, genomic characteristics, immune microenvironment interactions, and drug sensitivity of cuproptosis regulators in pan-cancer, providing valuable insights into their potential role in cancer biology. [Read the Full Post]

In silico enhancer mining reveals SNS-032 and EHMT2 inhibitors as therapeutic candidates in high-grade serous ovarian cancer

391 | Jul 11 2023

This study utilized epigenomic profiling and a computational pipeline to identify potential therapeutic candidates and enhance stratification for ovarian cancer, with a focus on high-grade serous carcinoma. [Read the Full Post]

Pelabresib (CPI-0610): An Exciting Novel Drug for the Treatment of Myelofibrosis

203 | Jul 02 2023

Pelabresib (CPI-0610), an investigational BET inhibitor, shows promising potential as a novel treatment approach for myelofibrosis, based on preclinical and clinical data demonstrating its ability to target key oncogenic signaling pathways and provide favorable responses in symptom control and disease-related parameters. [Read the Full Post]

A Phase I Study of Pelabresib (CPI-0610), a Small-Molecule Inhibitor of BET Proteins, in Patients with Relapsed or Refractory Lymphoma

155 | Jul 02 2023

The first-in-human phase I study of pelabresib demonstrated its safety, pharmacokinetics, pharmacodynamics, and preliminary clinical activity, establishing a maximum tolerated dose of 225 mg once daily and supporting its potential as a therapeutic agent for relapsed/refractory lymphomas. [Read the Full Post]

PRMT6-CDC20 facilitates glioblastoma progression via the degradation of CDKN1B

179 | Jul 01 2023

PRMT6, an overexpressed arginine methyltransferase in glioma/GBM, promotes cell proliferation and progression by destabilizing CDKN1B through CDC20-mediated degradation, suggesting potential therapeutic targeting of the PRMT6-CDC20-CDKN1B axis in GBM. [Read the Full Post]

Downregulation of BASP1 promotes temozolomide resistance in gliomas via epigenetic activation of the FBXO32/NF-κB/MGMT axis

74 | Jul 01 2023

Downregulation of BASP1 in gliomas leads to enhanced resistance to TMZ therapy through activation of the FBXO32/NF-κB/MGMT axis via epigenetic modifications mediated by the WDR5/MLL complex, suggesting a potential therapeutic target for combating TMZ-resistant gliomas. [Read the Full Post]

The role of EZH2 as a potential therapeutic target in retinoblastoma

225 | Jun 30 2023

The study reveals that the high expression of EZH2 in retinoblastoma tissues is associated with poor overall survival, and inhibiting EZH2 with UNC1999 shows promising results in suppressing RB cell proliferation, metastasis, and tumor glycolysis, making it a potential target for anti-RB treatment. [Read the Full Post]

Resistance to Pyrrolobenzodiazepine Dimers Is Associated with SLFN11 Downregulation and Can Be Reversed through Inhibition of ATR

312 | Jun 30 2023

This study identified downregulation of Schlafen family member 11 (SLFN11) and its association with PBD resistance in cancer cells, highlighting the potential of targeting SLFN11 and combining ATR inhibitors to overcome resistance to PBD-conjugated ADCs. [Read the Full Post]

The pattern of histone H3 epigenetic posttranslational modifications is regulated by the VRK1 chromatin kinase

525 | Jun 29 2023

The chromatin kinase VRK1 regulates the epigenetic patterns of histone H3 acetylation and methylation, particularly at lysines 4, 9, and 27, and is essential for coordinating chromatin organization and nuclear functions. [Read the Full Post]

LSD1 inhibitors for cancer treatment: Focus on multi-target agents and compounds in clinical trials

0 | Jun 29 2023

This review summarizes the structure and functions of LSD1, its role in cancer and non-cancer diseases, and the potential of covalent and non-covalent LSD1 inhibitors, including those in clinical trials, as potent and selective anticancer agents. [Read the Full Post]

New therapy for pancreatic cancer based on extracellular vesicles

288 | Jun 25 2023

The study demonstrates that loading chemotherapeutic drugs into small extracellular vesicles derived from the RWP-1 cell line using the direct incubation method holds promise as an efficient drug delivery system for pancreatic ductal adenocarcinoma, with potential for further preclinical investigation and combination with a PRMT5 inhibitor in clinical trials. [Read the Full Post]

PRMT5-mediated RNF4 methylation promotes therapeutic resistance of APL cells to As2O3 by stabilizing oncoprotein PML-RARα

162 | Jun 25 2023

The study demonstrates that PRMT5 is highly expressed in APL patients and its inhibition, either alone or in combination with As2O3, shows promising therapeutic potential by promoting the degradation of the oncogenic PML-RARα protein and inhibiting APL cell growth, differentiation, and survival. [Read the Full Post]

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

0 | Jun 22 2023

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

Targeting the undruggable: menin inhibitors ante portas

176 | Jun 18 2023

The menin-MLL axis inhibitors show promise as targeted therapies for acute myeloid leukemias with MLL rearrangements and NPM1 mutations, with early clinical data demonstrating favorable response rates and potential for improved outcomes. [Read the Full Post]

GSK-J1-loaded, hyaluronic acid-decorated metal-organic frameworks for the treatment of ovarian cancer

301 | Jun 17 2023

The study demonstrates the potential of hyaluronic acid-decorated metal-organic frameworks delivering the JMJD3 demethylase inhibitor GSK-J1 (HA@MOF@GSK-J1) as an effective and targeted strategy for treating carboplatin-resistant ovarian cancer. [Read the Full Post]

Inhibition of histone methyltransferase SETD8 represses DNA virus replication

197 | Jun 16 2023

UNC0379, an inhibitor of histone H4K20 methyltransferase SETD8, shows promise as an effective inhibitor of multiple DNA viruses by enhancing the expression of anti-viral genes and repressing viral replication, potentially offering a new strategy for the treatment of DNA virus-related diseases. [Read the Full Post]

Episodes of Early Pleistocene West Antarctic Ice Sheet Retreat Recorded by Iceberg Alley Sediments

199 | Jun 16 2023

This study in the Scotia Sea provides evidence of past episodes of West Antarctic Ice Sheet instability and suggests that intense IBRD deposition, likely sourced from the Weddell Sea and/or Amundsen Sea embayment(s), occurred during a warm climate phase approximately 1.2 million years ago. [Read the Full Post]

Comparison of pharmacological inhibitors of lysine-specific demethylase 1 in glioblastoma stem cells reveals inhibitor-specific efficacy profiles

232 | Jun 16 2023

This study demonstrates the cytotoxic effects of LSD1 inhibitors in patient-derived glioblastoma models and identifies potential resistance-associated genes, providing valuable insights for the development of future combination therapies. [Read the Full Post]

From PROTAC to inhibitor: Structure-guided discovery of potent and orally bioavailable BET inhibitors

304 | Jun 04 2023

The passage describes the discovery of a potent BET inhibitor called 1q (SJ1461) through a CLICK chemistry-based approach, which shows improved profiles compared to existing BET inhibitors and has promising potential for further development as a cancer therapy. [Read the Full Post]

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

188 | Jun 01 2023

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

Dieting reverses histone methylation and hypothalamic AgRP regulation in obese rats

216 | Jun 01 2023

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

Right Ventricular Dysfunction and Exercise Impairment in Patients with Heart Failure, Insulin Resistance, and Diabetes Mellitus: Insights from the T.O.S.CA. Registry (Cardiovascular Diabetology 2022)

158 | May 31 2023

The study findings suggest that insulin resistance and type 2 diabetes mellitus have a negative impact on right ventricular function, exercise tolerance, and cardiovascular outcomes, highlighting the need for early detection and management of these conditions. [Read the Full Post]

G9a/GLP Targeting Ameliorates Pulmonary Vascular Remodeling in Pulmonary Arterial Hypertension

128 | May 30 2023

This study suggests that inhibiting the histone methyltransferase G9a and its partner protein GLP may be a new therapeutic approach in pulmonary arterial hypertension. [Read the Full Post]

Dual inhibition of EZH2 and G9A/GLP histone methyltransferases by HKMTI-1-005 promotes differentiation of acute myeloid leukemia cells

303 | May 26 2023

The study investigates the potential of using an EZH2 inhibitor, HKMTI-1-005, to improve the response of non-APL AML cells to ATRA-based therapy by inducing differentiation and upregulating the expression of differentiation pathway genes. [Read the Full Post]

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

203 | May 26 2023

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

A patent review of EZH2 inhibitors from 2017 and beyond

285 | May 23 2023

EZH2 inhibitors are a promising class of drugs for the treatment of various diseases, particularly cancers, but further research is needed to optimize their efficacy and safety. [Read the Full Post]

FZD7, Regulated by Non-CpG Methylation, Plays an Important Role in Immature Porcine Sertoli Cell Proliferation

143 | May 22 2023

This study explores the regulatory roles of non-CpG methylation in testicular development, identifying several hub genes such as FZD7, which is found to be important in linking the proliferation and apoptosis of Sertoli cells. [Read the Full Post]

The Protective Effect of Zebularine, an Inhibitor of DNA Methyltransferase, on Renal Tubulointerstitial Inflammation and Fibrosis

183 | May 22 2023

Inhibiting DNA methylation can restore the balance between pro-inflammatory and anti-inflammatory pathways, alleviate renal inflammation and fibrosis, and highlight DNA methyltransferases as potential therapeutic targets for treating chronic kidney disease. [Read the Full Post]

JMJD3 Promotes Myeloid Fibroblast Activation and Macrophage Polarization in Kidney Fibrosis

277 | May 20 2023

This study demonstrates that JMJD3 plays a crucial role in myeloid fibroblast activation, macrophage polarization, and renal fibrosis development, making it a potential therapeutic target for chronic kidney disease. [Read the Full Post]

DOT1L promotes cell proliferation and invasion by epigenetically regulating STAT5B in renal cell carcinoma

173 | May 20 2023

Targeting DOT1L may be a potential therapeutic intervention for renal cell carcinoma as it promotes RCC progression by epigenetically promoting STAT5B transcription in a histone methyltransferase-dependent manner. [Read the Full Post]

The Effect of Direct and Indirect EZH2 Inhibition in Rhabdomyosarcoma Cell Lines

192 | May 17 2023

The study found that direct and indirect inhibition of EZH2 affect cellular functions differently, and the alveolar cell line RH30 is more sensitive to epigenetic intervention than the embryonal cell line RD, suggesting EZH2 as a potential therapeutic target in RMS. [Read the Full Post]

LSD1 inhibitors for cancer treatment: Focus on multi-target agents and compounds in clinical trials

209 | May 13 2023

LSD1 is an epigenetic enzyme overexpressed in many types of cancers, and its inhibitors have emerged as a promising therapeutic strategy for selectively targeting cancer cells while sparing normal cells. [Read the Full Post]

Recent advances of LSD1/KDM1A inhibitors for disease therapy

174 | May 13 2023

The review highlights recent advances and challenges in LSD1-targeted drug discovery for the treatment of various diseases, including hematologic malignancies. [Read the Full Post]

A small-molecule degrader of TET3 as treatment for anorexia nervosa in an animal model

122 | May 11 2023

Bobcat339, a synthetic small molecule that binds to the catalytic pockets of TET proteins, shows potential as a therapeutic for anorexia nervosa and stress-related disorders by inducing TET3 protein degradation and stimulating the expression of AGRP, NPY, and VGAT in a TET3-dependent manner. [Read the Full Post]

Clinical benefit of MAO-B and COMT inhibition in Parkinson's disease: practical considerations

274 | Apr 16 2023

MAO-B and COMT inhibitors are important strategies for managing motor fluctuations in Parkinson's disease patients, with several drugs available on the market targeting these enzymes, and ongoing studies exploring new formulations and combinations of these inhibitors. [Read the Full Post]

Prelimbic Cortical Stimulation with L-methionine Enhances Cognition through Hippocampal DNA Methylation and Neuroplasticity Mechanisms

146 | Apr 07 2023

The study suggests that targeting hippocampal DNA methyltransferase (DNMT) through prelimbic cortical deep brain stimulation (PrL DBS) and L-methionine (MET) co-administration may enhance memory and serve as a potential therapeutic approach for treating dementia. [Read the Full Post]

Development and Optimisation of Inhalable EGCG Nano-Liposomes as a Potential Treatment for Pulmonary Arterial Hypertension by Implementation of the Design of Experiments Approach

454 | Mar 21 2023

The research developed an inhalable EGCG nano-liposome formulation with desirable properties and demonstrated its potential effectiveness in treating PAH by inhibiting the TGFβ pathway. [Read the Full Post]

Clinical Characteristics and Treatment of Blastic Plasmacytoid Dendritic Cell Neoplasm

397 | Mar 08 2023

Blastic plasmacytoid dendritic cell neoplasm is a rare and aggressive hematological malignancy with diverse clinical manifestations and poor prognosis that requires a combination of clinical, morphological and immunophenotypic features for diagnosis and individualized treatment. [Read the Full Post]

Results from a phase I/II trial of cusatuzumab combined with azacitidine in patients with newly diagnosed acute myeloid leukemia who are ineligible for intensive chemotherapy

308 | Mar 07 2023

The phase I/II trial showed that cusatuzumab plus azacitidine was generally well-tolerated and showed preliminary efficacy in newly diagnosed AML patients ineligible for intensive chemotherapy, with ongoing investigation into the combination with venetoclax and azacitidine. [Read the Full Post]

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

272 | Feb 05 2023

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

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

306 | Feb 05 2023

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

MAT2A as Key Regulator and Therapeutic Target in MLL r Leukemogenesis

97 | Dec 11 2022

Kathy-Ann Secker et al. uncovered MAT2A as a key regulator in MLL leukemogenesis and its inhibition led to significant anti-leukemic effects. [Read the Full Post]

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

179 | Dec 01 2022

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

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

414 | Nov 28 2022

Aissa Benyoucef et al. revealed the novel involvement of ZEB2/LSD1 complexes in repressing the intrinsic apoptosis pathway by inhibiting the expression of several pro-apoptotic proteins such as BIM (BCL2L11) as a major driver for ETP-ALL survival. [Read the Full Post]

HO-1 promotes resistance to an EZH2 inhibitor through the pRB-E2F pathway: correlation with the progression of myelodysplastic syndrome into acute myeloid leukemia

0 | Nov 17 2022

Zhengchang He et al. thought that HO-1 could influence MDS resistance and progression to AML. [Read the Full Post]

Binding of the SARS-CoV-2 envelope E protein to human BRD4 is essential for infection

187 | Nov 06 2022

Kendra R Vann et al. provided insight into molecular mechanisms that contributed to SARS-CoV-2 pathogenesis and shed light on a new strategy to block SARS-CoV-2 infection. [Read the Full Post]

Non-canonical H3K79me2-dependent pathways promote the survival of MLL-rearranged leukemia

0 | Oct 21 2022

William F Richter et al. defined alternative proliferation pathways that more directly derived from H3K79me2 loss. [Read the Full Post]

Menin‑MLL inhibitors induce ferroptosis and enhance the anti‑proliferative activity of auranofin in several types of cancer cells

0 | Sep 27 2022

Ichiroh Kato et al. thought that the MI‑463‑induced decreased in cell viability might be at least partly associated with the inhibition of SCD1 activity. [Read the Full Post]

Design, Synthesis, and Biological Evaluations of DOT1L Peptide Mimetics Targeting the Protein-Protein Interactions between DOT1L and MLL-AF9/MLL-ENL

163 | Aug 22 2022

Yinan Yuan et al. found that inhibiting the protein-protein interactions between DOT1L and MLL fusion proteins was a potentially effective strategy for the treatment of MLL rearranged leukemias. [Read the Full Post]

Therapeutic potential of inhibiting histone 3 lysine 27 demethylases: a review of the literature

200 | Aug 08 2022

Jeries Abu-Hanna et al. suggested that inhibiting H3K27 demethylases held immense therapeutic potential in many diseases. [Read the Full Post]

Loss of METTL3 Attenuates Blastic Plasmacytoid Dendritic Cell Neoplasm Response to PRMT5 Inhibition via IFN Signalling

212 | Jul 17 2022

Malini Rethnam et al. implicated PRMT5 as a therapeutic target in BPDCN and provided insight into the involvement of METTL3 and interferon pathway in regulating response to PRMT5 inhibition. [Read the Full Post]

Combined inhibition of EZH2 and ATM is synthetic lethal in BRCA1-deficient breast cancer

306 | Jun 19 2022

Leonie Ratz et al. identified a synthetic lethal interaction between EZH2 and ATM and proposed this synergistic interaction as a novel molecular combination for the treatment of BRCA1-mutant breast cancer. [Read the Full Post]

Discovery of precision targeting EZH2 degraders for triple-negative breast cancer

375 | Jun 13 2022

Cheng Wang et al. found that U3i could degrade PRC2 complex in TNBC cells, induce apoptosis, and cause little damage to normal cells. [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

535 | 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]

Sotorasib Tackles KRASG12C-Mutated Pancreatic Cancer

387 | Apr 19 2022

Xinting Zheng et al. found that the mechanisms of resistance to sotorasib and determine the efficacy and safety of combination therapy for the treatment of NSCLC containing the KRAS G12C mutation. [Read the Full Post]

[Magnetic resonance imaging analysis on the effect of marathon on the dynamic changes of morphological characteristics of patellar tendon in amateur marathon runners after half marathon]

288 | Apr 06 2022

Y Zhang et al. thought that marathon had effect on the normal PT morphology in male amateur marathon runners, showing an increase in proximal CSA. [Read the Full Post]

JIB-04 Has Broad-Spectrum Antiviral Activity and Inhibits SARS-CoV-2 Replication and Coronavirus Pathogenesis

466 | Apr 03 2022

Juhee Son et al. found that a limited but still promising utility of JIB-04 as an antiviral agent in the combat against COVID-19 and potentially other viral diseases. [Read the Full Post]

A comprehensive study of epigenetic alterations in hepatocellular carcinoma identifies potential therapeutic targets

0 | Mar 23 2022

Juan Bayo et al. thought that the epigenetic alterations identified in HCC could be used to predict prognosis and to define a subgroup of high-risk patients that would potentially benefit from JmjC inhibitor therapy. [Read the Full Post]

AZD5153 reverses palbociclib resistance in ovarian cancer by inhibiting cell cycle-related proteins and the MAPK/PI3K-AKT pathway

499 | Mar 22 2022

Chen Liu et al. revealed that it was anticipated that this class of drugs, including AZD5153, which inhibited the cell cycle-related protein and MAPK/PI3K-AKT pathway, would exhibit synergistic effects with palbociclib in OC. [Read the Full Post]

Recruitment of MLL1 complex is essential for SETBP1 to induce myeloid transformation

513 | Mar 11 2022

Nhu Nguyen et al. thought that the MLL1 complex played a critical role in Setbp1-induced transcriptional activation and transformation. [Read the Full Post]

Discovery and Pharmacological Characterization of JNJ-64619178, a Novel Small-Molecule Inhibitor of PRMT5 with Potent Antitumor Activity

294 | Mar 08 2022

Dirk Brehmer et al. supported the continued clinical evaluation of JNJ-64619178 in patients with aberrant PRMT5 activity-driven tumors. [Read the Full Post]

EPZ015666, a selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an antitumour effect in retinoblastoma

0 | Jan 23 2022

Xing Liu et al. found that PRMT5 promoted retinoblastoma growth, the PRMT5 inhibitor EPZ015666 inhibited retinoblastoma in vitro by regulating P53-P21/P27-CDK2 signaling pathways and slowed retinoblastoma growth in a xenograft model. [Read the Full Post]

Protein Arginine Methyltransferase 5 Promotes the Migration of AML Cells by Regulating the Expression of Leukocyte Immunoglobulin-Like Receptor B4

269 | Jan 22 2022

Lu Zhao found that PRMT5 plays an important role in the invasion of AML, which acts via regulating the expression of LILRB4. PRMT5 could act as a potential therapeutic candidate for AML. Copyright © 2021 Lu Zhao et al. [Read the Full Post]

Disruptor of telomeric silencing 1-like promotes ovarian cancer tumor growth by stimulating pro-tumorigenic metabolic pathways and blocking apoptosis

0 | Jan 07 2022

Suresh Chava et al. found that DOT1L promoted ovarian cancer tumor growth by regulating apoptotic and metabolic pathways as well as NK cell-mediated eradication of ovarian cancer. [Read the Full Post]

Comprehensive in Vitro Characterization of the LSD1 Small Molecule Inhibitor Class in Oncology

405 | Jan 05 2022

Natalia Sacilotto et al. highlighted significant differences in potency and selectivity among the clinical compounds with iadademstat being the most potent and revealed that most of the tool compounds had very low activity and selectivity. [Read the Full Post]

HO-1 promotes resistance to an EZH2 inhibitor through the pRB-E2F pathway: correlation with the progression of myelodysplastic syndrome into acute myeloid leukemia

404 | Dec 26 2021

Zhengchang He et al. found that HO-1 could influence MDS resistance and progression to AML. [Read the Full Post]

Biological Effects of BET Inhibition by OTX015 (MK-8628) and JQ1 in NPM1-Mutated (NPM1c) Acute Myeloid Leukemia (AML)

534 | Dec 13 2021

Hanane Djamai et al. found that BETi, similar to ATO + ATRA, induced differentiation and apoptosis which was TP53 independent in the NPM1c cell line OCI-AML3 and primary cells. [Read the Full Post]

Non-canonical H3K79me2-dependent pathways promote the survival of MLL-rearranged leukemia

566 | Nov 27 2021

William F Richter et al. found that this pathway also depends on MLL1, indicating combinations of DOT1L, MLL1 and FLT3 inhibitors should be explored for treating FLT3-mutant leukemia. [Read the Full Post]

Menin‑MLL inhibitors induce ferroptosis and enhance the anti‑proliferative activity of auranofin in several types of cancer cells

903 | Nov 05 2021

Ichiroh Kato et al. thought that menin‑MLL inhibitors, such as MI‑463, in combination with auranofin represented an effective therapeutic approach for several types of cancer via the induction of ferroptosis. [Read the Full Post]

Disruptor of telomeric silencing 1-like promotes ovarian cancer tumor growth by stimulating pro-tumorigenic metabolic pathways and blocking apoptosis

702 | Sep 28 2021

Suresh Chava et al. demonstrated that DOT1L promoted ovarian cancer tumor growth by regulating apoptotic and metabolic pathways as well as NK cell-mediated eradication of ovarian cancer and identified DOT1L as a new pharmacological target for ovarian cancer therapy. [Read the Full Post]

Overexpression of UTX promotes tumor progression in Oral tongue squamous cell carcinoma patients receiving surgical resection: a case control study

546 | Sep 14 2021

Yen-Hao Chen et al. found that UTX played an important role in the process of OTSCC and overexpression of UTX might predict poor prognosis in OTSCC patients who received surgical resection. [Read the Full Post]

Myelocytomatosis-Protein Arginine N-Methyltransferase 5 Axis Defines the Tumorigenesis and Immune Response in Hepatocellular Carcinoma

577 | Aug 24 2021

Yuhong Luo et al. revealed that PRMT5 was an epigenetic executer of MYC, leading to repression of the transcriptional regulation of downstream genes that promoted hepatocellular carcinogenesis. [Read the Full Post]

TCF3 is epigenetically silenced by EZH2 and DNMT3B and functions as a tumor suppressor in endometrial cancer

621 | Jul 28 2021

Tao Gui et al. found that TCF3 functions as a tumor suppressor epigenetically silenced by EZH2 and DNMT3B in EC. [Read the Full Post]

CDKN2A Determines Mesothelioma Cell Fate to EZH2 Inhibition

647 | Jul 22 2021

Giulia Pinton et al. found that the expression of CDKN2A predicted cell fate in response to EZH2 inhibition and could potentially stratify tumors likely to undergo apoptosis. [Read the Full Post]

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

814 | 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]

SMALL MOLECULE IMAGING AGENT FOR MUTANT KRAS G12C

593 | May 19 2021

Peter D Koch et al. found that two fluorescent derivatives (BODIPY FL and BODIPY TMR) of ARS-1323 bind mutant KRAS and could be used for biochemical binding screens. [Read the Full Post]

MLL1 combined with GSK3 and MAP2K inhibition improves the development of in vitro-fertilized embryos

712 | Apr 27 2021

Xuejie Han et al. found that the application of 3i provided a new method for improving IVF embryo production in domestic animals. [Read the Full Post]

H3K36 methylation reprograms gene expression to drive early gametocyte development in Plasmodium falciparum

776 | Apr 25 2021

Jessica Connacher et al. found that H3K36me2&3-associated repression of genes was therefore involved in key transcriptional shifts that accompanied the transition from early gametocyte differentiation to intermediate development. [Read the Full Post]

A comprehensive study of epigenetic alterations in hepatocellular carcinoma identifies potential therapeutic targets

1087 | Apr 11 2021

Juan Bayo et al. found that mutations and changes in expression of epigenetic modifiers were common events in human hepatocellular carcinoma, leading to an aggressive gene expression program and poor clinical prognosis. [Read the Full Post]

Dissecting the Role of BET Bromodomain Proteins BRD2 and BRD4 in Human NK Cell Function

620 | Apr 10 2021

Adam P Cribbs et al. found that compelling argument for further clinical investigation. [Read the Full Post]

Oxidative stress abrogates the degradation of KMT2D to promote degeneration in nucleus pulposus

605 | Mar 23 2021

Wenbin Xu et al. approved that oxidative stress induced ROS production promote the process of NP degeneration by enhancing KMT2D mediated transcriptional regulation of matrix degeneration related genes during NP degeneration. [Read the Full Post]

Rational Design, synthesis and biological evaluation of novel triazole derivatives as potent and selective PRMT5 inhibitors with antitumor activity

475 | Mar 21 2021

Kongkai Zhu et al. described the design, synthesis and biological evaluation of a series of novel, potent and selective PRMT5 inhibitors with antiproliferative activity against Z-138 mantle cell lymphoma cell line. [Read the Full Post]

EPZ015666, a selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an antitumour effect in retinoblastoma

645 | Jan 29 2021

Xing Liu et al. found that EPZ015666 inhibited retinoblastoma cell proliferation and led to cell cycle arrest at the G1 phase. [Read the Full Post]

Inhibition of PRMT5 Attenuates Oxidative Stress-Induced Pyroptosis via Activation of the Nrf2/HO-1 Signal Pathway in a Mouse Model of Renal Ischemia-Reperfusion Injury

558 | Jan 29 2021

Changhui Diao et al. thought that PRMT5 might be a promising therapeutic target. [Read the Full Post]

Histone methyltransferase DOT1L coordinates AR and MYC stability in prostate cancer

709 | Jan 17 2021

R Vatapalli et al. thought that DOT1L selectively regulated the tumorigenicity of AR-positive prostate cancer cells and was a promising therapeutic target for PCa. [Read the Full Post]

Targeting LSD1 for acute myeloid leukemia (AML) treatment

617 | Jan 14 2021

Shujing Zhang et al. discussed the main epigenetic drugs targeting LSD1 for AML therapy. [Read the Full Post]

Inhibition of Methyltransferase DOT1L Sensitizes to Sorafenib Treatment AML Cells Irrespective of MLL-Rearrangements: A Novel Therapeutic Strategy for Pediatric AML

527 | Dec 09 2020

Annalisa Lonetti et al. highlighted a novel therapeutic strategy for pediatric AML patients. [Read the Full Post]

Menin regulates the serine biosynthetic pathway in Ewing sarcoma

0 | Nov 14 2020

Laurie K Svoboda et al. demonstrated that the SSP was highly active in Ewing sarcoma and that its oncogenic activation was maintained, at least in part, by menin-dependent epigenetic mechanisms involving trithorax complexes. [Read the Full Post]

Nullifying epigenetic writer DOT1L attenuates neointimal hyperplasia

678 | Sep 22 2020

Yitao Huang et al. presented a strong rationale for continued mechanistic and translational investigation into DOT1L targeting for treatment of (re)stenotic vascular conditions. [Read the Full Post]

Palmitate-TLR4 signaling regulates the histone demethylase, JMJD3, in macrophages and impairs diabetic wound healing

591 | Aug 31 2020

Frank M Davis et al. concluded that palmitate contributed to the chronic Jmjd3-mediated activation of macrophages in diabetic peripheral tissue and a histone demethylase inhibitor-based therapy might represent a novel treatment for nonhealing diabetic wounds. [Read the Full Post]

EZH2 Supports Osteoclast Differentiation and Bone Resorption Via Epigenetic and Cytoplasmic Targets

591 | Aug 08 2020

Juraj Adamik et al. found that EZH2 exhibits complex roles in supporting osteoclast differentiation and function. [Read the Full Post]

PRMT5 control of cGAS/STING and NLRC5 pathways defines melanoma response to antitumor immunity

670 | Aug 03 2020

Hyungsoo Kim et al. provided a rationale to test PRMT5 inhibitors in immunotherapy-based clinical trials as a means to enhance an antitumor immune response. [Read the Full Post]

HMTase Inhibitors as a Potential Epigenetic-Based Therapeutic Approach for Friedreich's Ataxia

718 | Jun 28 2020

Mursal Sherzai et al. showed that a combination treatment of BIX0194 and GSK126, significantly increased FXN gene expression levels and reduced the repressive histone marks. However, no increase in frataxin protein levels was observed. [Read the Full Post]

EZH2 Is Involved in Vulnerability to Neuroinflammation and Depression-Like Behaviors Induced by Chronic Stress in Different Aged Mice

596 | Jun 23 2020

Wei Wang et al. found that EZH2 might be involved in susceptibility to neuroinflammation and depression-like behaviors in different aged mice. [Read the Full Post]

The DOT1L inhibitor Pinometostat decreases the host-response against infections: Considerations about its use in human therapy

729 | Mar 03 2020

Marcos-Villar Let al. supported a possible increased vulnerability to infection in MLL-r leukemia patients undergoing pinometostat treatment. Close follow up of infection should be considered in pinometostat therapy to reduce some severe side effects during the treatment. [Read the Full Post]

Menin regulates the serine biosynthetic pathway in Ewing sarcoma

0 | Feb 04 2020

Svoboda LK et al. demonstrated that the SSP is highly active in Ewing sarcoma and that its oncogenic activation is maintained, at least in part, by menin-dependent epigenetic mechanisms involving trithorax complexes. [Read the Full Post]

EZH2 targeting reduces medulloblastoma growth through epigenetic reactivation of the BAI1/p53 tumor suppressor pathway

677 | Jan 31 2020

Zhang H et al. demonstrated that reactivation of BAI1 expression underlies EPZ-6438 antitumorigenic action, and provided preclinical proof-of-principle evidence for targeting EZH2 in patients with MB. [Read the Full Post]

Tri-methylation of H3K79 is decreased in TGF-β1-induced epithelial-to-mesenchymal transition in lung cancer

1425 | Nov 29 2019

Evanno E et al. showed that histone methylation was modified during EMT, and combination of epigenetic compounds with conventional or targeted chemotherapy might contribute to reduce metastasis and to enhance clinical responses. [Read the Full Post]

Epigenetic Profiling Identifies LIF as a Super-enhancer-Controlled Regulator of Stem Cell-like Properties in Osteosarcoma

794 | Nov 12 2019

Lu B et al. revealed osteosarcoma SE profiles and uncovers a distinct tumor-stemness epigenetic regulatory mechanism in which an osteosarcoma-specific SE-mediated factor, LIF, promotes osteosarcoma stemness gene activation via NOTCH1 signaling pathway. [Read the Full Post]

Regulation of PRMT5-MDM4 axis is critical in the response to CDK4/6 inhibitors in melanoma

708 | Oct 16 2019

AbuHammad S et al. provided a strong rationale for further investigation of novel combinations of CDK4/6 and PRMT5 inhibitors, not only in melanoma but other tumor types, including breast, pancreatic, and esophageal carcinoma. [Read the Full Post]

Blocking EZH2 methylation transferase activity by GSK126 decreases stem cell-like myeloma cells

0 | Aug 27 2019

Zeng D et al. suggested that EZH2 inactivation by GSK126 is effective in killing MM cells and CSCs as a single agent or in combination with bortezomib. Clinical trial of GSK126in patients with MM may be warranted. [Read the Full Post]

Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma

780 | Aug 19 2019

Knutson SK et al. indicated these data confirm the dependency of EZH2-mutant NHL on EZH2 activity and portend the utility of EPZ-6438 as a potential treatment for these genetically defined cancers. [Read the Full Post]

A patent review of arginine methyltransferase inhibitors (2010-2018)

845 | Jul 10 2019

Li X et al. summarized the updated patented inhibitors targeting PRMTs from 2010 to 2018. The authors illustrate the chemical structures, molecular mechanism of action, pharmacological activities as well as the potential clinical application including combination therapy and biomarker-guided therapy. PRMT inhibitors in clinical trials are also highlighted. The authors provide a future perspective for further development of potent and selective PRMT inhibitors. [Read the Full Post]

Inhibition of G9a by a small molecule inhibitor, UNC0642, induces apoptosis of human bladder cancer cells

799 | Jun 26 2019

Cao YP et al. demonstrated that G9a may be a promising therapeutic target for UBC, and an epigenetics-based therapy by UNC0642 is suggested. [Read the Full Post]

Elevating H3K27me3 level sensitizes colorectal cancer to oxaliplatin

829 | Jun 06 2019

Wang Q et al. suggested that elevating H3K27me3 level can improve drug sensitivity in CRC patients. [Read the Full Post]

Menin regulates the serine biosynthetic pathway in Ewing sarcoma

1088 | May 09 2019

Svoboda LK et al. demonstrated that the SSP is highly active in Ewing sarcoma and that its oncogenic activation is maintained, at least in part, by menin-dependent epigenetic mechanisms involving trithorax complexes. [Read the Full Post]

Randomized phase 2 study of low-dose decitabine vs low-dose azacitidine in lower-risk MDS and MDS/MPN

1089 | Mar 10 2019

Jabbour E et al. indicated that treatment was well tolerated, with a 6-week mortality rate of 0%. The use of low-dose HMAs is safe and effective in patients with lower-risk MDS and MDS/MPN. Their effect on the natural history of lower-risk disease needs to be further studied. [Read the Full Post]

Inhibition of H3K27me3 Histone Demethylase Activity Prevents the Proliferative Regeneration of Zebrafish Lateral Line Neuromasts

1052 | Mar 06 2019

Bao B et al. indicated that H3K27me3 demethylation is a key epigenetic regulator in the process of hair cell regeneration in zebrafish and suggest that H3K27me3 histone demethylase activity might be a novel therapeutic target for the treatment of hearing loss. [Read the Full Post]

Inactivation of PBX3 and HOXA9 by down-regulating H3K79 methylation represses NPM1-mutated leukemic cell survival

1065 | Feb 27 2019

Zhang W et al. indicated that NPMc+ leukemic cell survival requires upregulation of PBX3 and HOXA9, and this action can be largely attenuated by a DOT1L inhibitor. [Read the Full Post]

Preclinical evaluation of the BET bromodomain inhibitor BAY 1238097 for the treatment of lymphoma

829 | Jan 02 2019

Bernasconi E et al. indicated the use of combination schemes targeting EZH2, mTOR and BTK alongside BET bromodomains. [Read the Full Post]

BAP1 dependent expression of long non-coding RNA NEAT-1 contributes to sensitivity to gemcitabine in cholangiocarcinoma

866 | Jan 02 2019

Parasramka M et al. showed that NEAT-1 is a downstream effector of gemcitabine sensitivity in CCA. The expression of BAP1 is a determinant of sensitivity to therapeutic drugs that can be exploited to enhance responses through combination strategies. [Read the Full Post]

Menin regulates Inhbb expression through an Akt/Ezh2-mediated H3K27 histone modification

820 | Dec 31 2018

Gherardi S et al. suggested therefore that Menin could take an important part to the Ezh2-epigenetic repressive landscape in many cells and tissues through its capacity to modulate Akt phosphorylation. [Read the Full Post]

Epigenetic drug combination induces remission in mouse xenograft models of pediatric acute myeloid leukemia

1148 | Nov 18 2018

Gopalakrishnapillai A et al. indicated the expression of mutant p53 in MV4;11 cells reduced sensitivity to azacitidine-panobinostat combination, suggesting that p53 may be a predictor of response to epigenetic therapy in pediatric AML. [Read the Full Post]

Epigenetic repression of miR-375 is the dominant mechanism for constitutive activation of the PDPK1/RPS6KA3 signalling axis in multiple myeloma.

1056 | Oct 12 2018

Tatekawa S et al. showed the universal involvement of overlapping epigenetic dysregulation for abnormal miR-375 repression in MM, which is likely to contribute to myelomagenesis and to subsequent myeloma progression by activating oncogenic signalling pathways. [Read the Full Post]

Multi-omics maps of cotton fibre reveal epigenetic basis for staged single-cell differentiation

1410 | May 06 2018

Wang M et al. illustrated two divergent pathways mediating a continuous increase of DNA methylation and also sheds further light on the epigenetic basis for single-cell differentiation in plants. [Read the Full Post]