85 articles for thisTarget
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Article Title
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Novel 3-methylindoline inhibitors of EZH2: Design, synthesis and SAR.
Integral Biosciences
Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors.
Pfizer
Identification of novel EZH2 inhibitors through pharmacophore-based virtual screening and biological assays.
College of Chemical and Environmental Engineering
The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat.
Epizyme
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
Constellation Pharmaceuticals
Selective inhibitors of protein methyltransferases.
Icahn School of Medicine At Mount Sinai
The role of enhancer of zeste homologue 2 inhibitors in controlling epigenetics and their potential for cancer treatment.
Therachem Research Medilab (India)
Discovery and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2.
Constellation Pharmaceuticals
Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2.
TBA
Fused Tetrahydroquinolines Are Interfering with Your Assay.
University of North Carolina At Chapel Hill
First-in-Class Dual EZH2-HSP90 Inhibitor Eliciting Striking Antiglioblastoma Activity
Taipei Medical University
Recent advances in EZH2-based dual inhibitors in the treatment of cancers.
Xinxiang University
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
Discovery of cysteine-targeting covalent histone methyltransferase inhibitors.
Nanjing Medical University
A decade of approved first-in-class small molecule orphan drugs: Achievements, challenges and perspectives.
China Pharmaceutical University
Small-Molecule Hydrophobic Tagging: A Promising Strategy of Druglike Technology for Targeted Protein Degradation.
China Pharmaceutical University
Design, synthesis and mechanism studies of dual EZH2/BRD4 inhibitors for cancer therapy.
China Pharmaceutical University
Design, Synthesis, and Biological Evaluation of a Potent Dual EZH2-BRD4 Inhibitor for the Treatment of Some Solid Tumors.
Sichuan University
Discovery of a Novel Covalent EZH2 Inhibitor Based on Tazemetostat Scaffold for the Treatment of Ovarian Cancer.
Sichuan University
Structural Modification and Pharmacological Evaluation of Substituted Quinoline-5,8-diones as Potent NSD2 Inhibitors.
Shanghai Jiao Tong University
Quinoline anticancer agents active on DNA and DNA-interacting proteins: From classical to emerging therapeutic targets.
University of Palermo
Blocking Non-enzymatic Functions by PROTAC-Mediated Targeted Protein Degradation.
Second Military Medical University (Naval Medical University)
Focused Libraries for Epigenetic Drug Discovery: The Importance of Isosteres.
University of Pennsylvania
Recent advances in epigenetic proteolysis targeting chimeras (Epi-PROTACs).
"Sapienza" University of Rome
Targeting Autophagy-Related Epigenetic Regulators for Cancer Drug Discovery.
West China Hospital of Sichuan University
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
Menoufia University
Structure-Aided Design, Synthesis, and Biological Evaluation of Potent and Selective Non-Nucleoside Inhibitors Targeting Protein Arginine Methyltransferase 5.
Sun Yat-Sen University
Design and Synthesis of Dual EZH2/BRD4 Inhibitors to Target Solid Tumors.
Sun Yat-Sen University Cancer Center
Fascinating Transformation of SAM-Competitive Protein Methyltransferase Inhibitors from Nucleoside Analogues to Non-Nucleoside Analogues.
Csir-Indian Institute of Chemical Biology
Novel Quinoline Compounds as EZH2 Inhibitors for Treating Cancer.
Smith, Gambrell & Russell
Recent strategies targeting Embryonic Ectoderm Development (EED) for cancer therapy: Allosteric inhibitors, PPI inhibitors, and PROTACs.
Sanquan College of Xinxiang Medical University
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
Structural modification aimed for improving solubility of lead compounds in early phase drug discovery.
Indian Institute of Technology (B.H.U.)
Histone Deacetylase and Enhancer of Zeste Homologue 2 Dual Inhibitors Presenting a Synergistic Effect for the Treatment of Hematological Malignancies.
China Pharmaceutical University
Targeting EZH2 for cancer therapy: From current progress to novel strategies.
West China Hospital
A Chemical Strategy toward Novel Brain-Penetrant EZH2 Inhibitors.
Tri-Institutional Therapeutics Discovery Institute
Design and Synthesis of EZH2-Based PROTACs to Degrade the PRC2 Complex for Targeting the Noncatalytic Activity of EZH2.
Sichuan University
Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
Chinese Academy of Sciences
Discovery of First-in-Class Dual PARP and EZH2 Inhibitors for Triple-Negative Breast Cancer with Wild-Type BRCA.
China Pharmaceutical University
Discovery of a potent MLL1 and WDR5 protein-protein interaction inhibitor with in vivo antitumor activity.
China Pharmaceutical University
5-Aminonaphthalene derivatives as selective nonnucleoside nuclear receptor binding SET domain-protein 2 (NSD2) inhibitors for the treatment of multiple myeloma.
Chinese Academy of Sciences
Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymp
Constellation Pharmaceuticals
Design and Characterization of a Pyridone-Containing EZH2 Inhibitor Phosphate Prodrug.
TBA
Small Molecule Approaches for Targeting the Polycomb Repressive Complex 2 (PRC2) in Cancer.
Northwestern University
Identification of DOT1L inhibitors by structure-based virtual screening adapted from a nucleoside-focused library.
University of Michigan Medical School
Design and synthesis of (E)-1,2-diphenylethene-based EZH2 inhibitors.
Sichuan University and Collaborative Innovation Center
Design, Synthesis, and Pharmacological Evaluation of Second Generation EZH2 Inhibitors with Long Residence Time.
Constellation Pharmaceuticals
Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells.
Sapienza University of Rome
New small molecule inhibitors of histone methyl transferase DOT1L with a nitrile as a non-traditional replacement for heavy halogen atoms.
University College London
Structure-Activity Relationship Studies for Enhancer of Zeste Homologue 2 (EZH2) and Enhancer of Zeste Homologue 1 (EZH1) Inhibitors.
Icahn School of Medicine At Mount Sinai
Histone methyl transferases: A class of epigenetic opportunities to counter uncontrolled cell proliferation.
Punjabi University
Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin's Lymphoma.
Shanghai Hengrui Pharmaceutical
Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquin
Wuxi Apptec
Fused tetracyclic quinazoline derivatives as inhibitors of ErbB2
Enliven Therapeutics
Compounds as neuronal histamine receptor-3 antagonists and uses thereof
Xw Laboratories
Carbonic anhydrases inhibitory effects of new benzenesulfonamides synthesized by using superacid chemistry.
Laboratoire Synthese Et Reactivite Des Substances Naturelles
Oxysterol-binding protein (OSBP)-related protein 4 (ORP4) is essential for cell proliferation and survival.
Dalhousie University
Discovery of novel irreversible inhibitors of interleukin (IL)-2-inducible tyrosine kinase (Itk) by targeting cysteine 442 in the ATP pocket.
Glaxosmithkline
Discovery of Allosteric and Selective Inhibitors of Inorganic Pyrophosphatase from Mycobacterium tuberculosis.
University of Kentucky
Substituted pyrrolo[2,3-h][1,6]naphthyridines and compositions thereof as JAK inhibitors
Nissan Chemical Industries
Design, synthesis, biological screening, and molecular docking studies of piperazine-derived constrained inhibitors of DPP-IV for the treatment of type 2 diabetes.
Csir-Central Drug Research Institute
Arylazopyrazole AAP1742 inhibits CDKs and induces apoptosis in multiple myeloma cells via Mcl-1 downregulation.
Institute of Experimental Botany Ascr and Palacky University
Comparison of pharmacological activities of three distinct kappa ligands (Salvinorin A, TRK-820 and 3FLB) on kappa opioid receptors in vitro and their antipruritic and antinociceptive activities in vivo.
Temple University
Pharmacological properties of J-104132 (L-753,037), a potent, orally active, mixed ETA/ETB endothelin receptor antagonist.
Banyu Pharmaceutical