95 articles for thisTarget
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Discovery of novel small molecule inhibitors of lysine methyltransferase G9a and their mechanism in leukemia cell lines.
Georgia State University
Discovery, design and synthesis of 6H-anthra[1,9-cd]isoxazol-6-one scaffold as G9a inhibitor through a combination of shape-based virtual screening and structure-based molecular modification.
China Pharmaceutical University
Selective inhibitors of protein methyltransferases.
Icahn School of Medicine At Mount Sinai
Discovery of a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8.
University of North Carolina at Chapel Hill
Identifying novel selective non-nucleoside DNA methyltransferase 1 inhibitors through docking-based virtual screening.
Chinese Academy of Sciences
Analogues of the Natural Product Sinefungin as Inhibitors of EHMT1 and EHMT2.
University of Copenhagen
Using 'biased-privileged' scaffolds to identify lysine methyltransferase inhibitors.
Rockefeller University
On the histone lysine methyltransferase activity of fungal metabolite chaetocin.
Imperial College
Discovery and development of potent and selective inhibitors of histone methyltransferase g9a.
Abbvie
A medicinal chemistry perspective for targeting histone H3 lysine-79 methyltransferase DOT1L.
Baylor College of Medicine
Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP.
University of North Carolina at Chapel Hill
Exploiting an allosteric binding site of PRMT3 yields potent and selective inhibitors.
University of North Carolina at Chapel Hill
Epidithiodiketopiperazine as a pharmacophore for protein lysine methyltransferase G9a inhibitors: reducing cytotoxicity by structural simplification.
Riken Advanced Science Institute
Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2.
TBA
Gliotoxin analogues from a marine-derived fungus, Penicillium sp., and their cytotoxic and histone methyltransferase inhibitory activities.
The University of Tokyo
Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines.
University of North Carolina at Chapel Hill
Computer- and structure-based lead design for epigenetic targets.
Martin-Luther University of Halle-Wittenberg
Chemical probes for histone-modifying enzymes.
Johns Hopkins University School of Medicine
Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines.
University of North Carolina at Chapel Hill
Discovery of a 2,4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a.
University of North Carolina
An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1.
UNC Eshelman School of Pharmacy
Small molecule inhibitors and CRISPR/Cas9 mutagenesis demonstrate that SMYD2 and SMYD3 activity are dispensable for autonomous cancer cell proliferation.
Epizyme, Inc.
The Histone Methyltransferase Inhibitor A-366 Uncovers a Role for G9a/GLP in the Epigenetics of Leukemia.
Abbvie
Novel orally bioavailable EZH1/2 dual inhibitors with greater antitumor efficacy than an EZH2 selective inhibitor.
Daiichi Sankyo Co., Ltd
Discovery of novel G9a/GLP covalent inhibitors for the treatment of triple-negative breast cancer.
Sichuan University
Discovery of a Highly Potent and Selective Inhibitor Targeting Protein Lysine Methyltransferase NSD2.
Sun Yat-Sen University
Discovery of a Highly Potent Lysine Methyltransferases G9a/NSD2 Dual Inhibitor to Treat Solid Tumors.
Sun Yat-Sen University
Structure-based development of novel substrate-type G9a inhibitors as epigenetic modulators for sickle cell disease treatment.
Kyorin Pharmaceutical Co. Ltd.
Discovery of a Potent, Selective, and Cell-Active SPIN1 Inhibitor.
Icahn School of Medicine At Mount Sinai
SETDB1 as a cancer target: challenges and perspectives in drug design.
University of Sao Paulo
Dual inhibitors of HDAC and other epigenetic regulators: A novel strategy for cancer treatment.
Guru Ghasidas University
Discovery of Potent and Selective G9a Degraders for the Treatment of Pancreatic Cancer.
Shanghai Institute of Materia Medica
Discovery of potent small molecule inhibitors of histone lysine methyltransferase NSDs.
Jiangsu University of Technology
Small molecules targeting selected histone methyltransferases (HMTs) for cancer treatment: Current progress and novel strategies.
First Affiliated Hospital of Gannan Medical University
Repurposing of Raltitrexed as an Effective G9a/EHMT2 Inhibitor and Promising Anti-Alzheimer's Agent.
National Institute of Technology Durgapur
NSD3: Advances in cancer therapeutic potential and inhibitors research.
Peking University
Recent advances in EZH2-based dual inhibitors in the treatment of cancers.
Xinxiang University
Drug Discovery Targeting Nuclear Receptor Binding SET Domain Protein 2 (NSD2).
University of Texas Medical Branch (UTMB)
Discovery of novel non-nucleoside inhibitors with high potency and selectivity for DNA methyltransferase 3A.
Zhejiang University
Structure-Based Discovery of Inhibitors of the SARS-CoV-2 Nsp14 N7-Methyltransferase.
University of California San Francisco
Structure-Based Design and Characterization of the Highly Potent and Selective Covalent Inhibitors Targeting the Lysine Methyltransferases G9a/GLP.
Sun Yat-Sen University
Discovery of a New-Generation S-Adenosylmethionine-Noncompetitive Covalent Inhibitor Targeting the Lysine Methyltransferase Enhancer of Zeste Homologue 2.
Sun Yat-Sen University
Discovery of Dual Lysine Methyltransferase G9a and EZH2 Inhibitors with In Vivo Efficacy against Malignant Rhabdoid Tumor.
Shenyang Pharmaceutical University
Research progress of LSD1-based dual-target agents for cancer therapy.
Xinxiang University
Discovery of cysteine-targeting covalent histone methyltransferase inhibitors.
Nanjing Medical University
Discovery of Novel Substrate-Competitive Lysine Methyltransferase G9a Inhibitors as Anticancer Agents.
Kyorin Pharmaceutical
Research progress of dual inhibitors targeting crosstalk between histone epigenetic modulators for cancer therapy.
Xinxiang Medical University
Quinoline anticancer agents active on DNA and DNA-interacting proteins: From classical to emerging therapeutic targets.
University of Palermo
Recent contributions of quinolines to antimalarial and anticancer drug discovery research.
Ghent University
Targeting Autophagy-Related Epigenetic Regulators for Cancer Drug Discovery.
West China Hospital of Sichuan University
Fascinating Transformation of SAM-Competitive Protein Methyltransferase Inhibitors from Nucleoside Analogues to Non-Nucleoside Analogues.
Csir-Indian Institute of Chemical Biology
Discovery of the First-in-Class G9a/GLP Covalent Inhibitors.
Icahn School of Medicine At Mount Sinai
Targeting Enhancer of Zeste Homolog 2 for the Treatment of Hematological Malignancies and Solid Tumors: Candidate Structure-Activity Relationships Insights and Evolution Prospects.
Affiliated Hospital of Guangdong Medical University
Novel non-covalent LSD1 inhibitors endowed with anticancer effects in leukemia and solid tumor cellular models.
Sapienza University of Rome
Identification and in vitro characterization of a new series of potent and highly selective G9a inhibitors as novel anti-fibroadipogenic agents.
Promidis
Discovery of AL-GDa62 as a Potential Synthetic Lethal Lead for the Treatment of Gastric Cancer.
Victoria University of Wellington
Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with
University of Navarra
Discovery of a potent MLL1 and WDR5 protein-protein interaction inhibitor with in vivo antitumor activity.
China Pharmaceutical University
Recent progress on HDAC inhibitors with dual targeting capabilities for cancer treatment.
Southern Medical University
Discovery of novel histone lysine methyltransferase G9a/GLP (EHMT2/1) inhibitors: Design, synthesis, and structure-activity relationships of 2,4-diamino-6-methylpyrimidines.
Daiichi Sankyo
Selective Peptidomimetic Inhibitors of NTMT1/2: Rational Design, Synthesis, Characterization, and Crystallographic Studies.
Virginia Commonwealth University
Identification of DOT1L inhibitors by structure-based virtual screening adapted from a nucleoside-focused library.
University of Michigan Medical School
Pharmacophore-based screening of diamidine small molecule inhibitors for protein arginine methyltransferases.
University of Georgia
New small molecule inhibitors of histone methyl transferase DOT1L with a nitrile as a non-traditional replacement for heavy halogen atoms.
University College London
Discovery of a Novel Chemotype of Histone Lysine Methyltransferase EHMT1/2 (GLP/G9a) Inhibitors: Rational Design, Synthesis, Biological Evaluation, and Co-crystal Structure.
The University of Texas M.D. Anderson Cancer Center
Histone methyl transferases: A class of epigenetic opportunities to counter uncontrolled cell proliferation.
Punjabi University
Recent progress in histone methyltransferase (G9a) inhibitors as anticancer agents.
Southern Medical University
Discovery of Bisubstrate Inhibitors for Protein N-Terminal Methyltransferase 1.
Purdue University
Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1).
Icahn School of Medicine At Mount Sinai
The identification of novel small-molecule inhibitors targeting WDR5-MLL1 interaction through fluorescence polarization based high-throughput screening.
Zhejiang Sci-Tech University
Identification of novel quinazoline derivatives as potent antiplasmodial agents.
University of Lille
Novel Propargyl-Linked Bisubstrate Analogues as Tight-Binding Inhibitors for Nicotinamide
TBA
A Chemical Probe for Tudor Domain Protein Spindlin1 to Investigate Chromatin Function.
University of Oxford
Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor.
National University of Singapore
Discovery of Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase.
Icahn School of Medicine At Mount Sinai
Identification of 2,4-diamino-6,7-dimethoxyquinoline derivatives as G9a inhibitors†Electronic supplementary information (ESI) available. See DOI: 10.1039/c4md00274a.
Imperial College London
Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9.
Ludwig-Maximillians University of Munich
Histone Deacetylase Inhibitors as Treatment for Targeting Multiple Components in Cancer Therapy.
Usona Institute
Detailed Exploration around 4-Aminoquinolines Chemical Space to Navigate the Lysine Methyltransferase G9a and DNA Methyltransferase Biological Spaces.
Wuxi Apptec (Tianjin) Co.
Inhibition of histone lysine methyltransferases G9a and GLP by ejection of structural Zn(II).
Radboud University
Methyllysine binding domains: Structural insight and small molecule probe development.
University of Connecticut
Discovery of Reversible DNA Methyltransferase and Lysine Methyltransferase G9a Inhibitors with Antitumoral in Vivo Efficacy.
Universidad De Oviedo-Principado De Asturias
Structure-activity relationship studies of G9a-like protein (GLP) inhibitors.
Icahn School of Medicine At Mount Sinai
Nitrile derivative that acts as inhibitor of dipeptidyl peptidase 1 and use thereof
Haisco Pharmaceuticals
Discovery and Structure Optimization of a Series of Isatin Derivatives as Mycobacterium tuberculosis Chorismate Mutase Inhibitors.
Birla Institute of Technology