66 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
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
Novel coumarins and benzocoumarins acting as isoform-selective inhibitors against the tumor-associated carbonic anhydrase IX.
S.G.S.I.T.S.
Human gene S31 encodes the pharmacologically defined serotonin 5-hydroxytryptamine1E receptor.
Synaptic Pharmaceutical
Thermodynamic and kinetic characterization of host-guest association between bolaform surfactants and alpha- and beta-cyclodextrins.
Lund University
Identification of a potent synthetic FXR agonist with an unexpected mode of binding and activation.
Merck Research Laboratories
5-(1H-Benzimidazol-1-yl)-3-alkoxy-2-thiophenecarbonitriles as potent, selective, inhibitors of IKK-epsilon kinase.
Gsk
Design, synthesis, and biological evaluation of Plasmodium falciparum lactate dehydrogenase inhibitors.
University of Mississippi
Structure-based design and synthesis of non-nucleoside, potent, and orally bioavailable adenosine deaminase inhibitors.
Fujisawa Pharmaceutical
Identification and characterization of novel benzil (diphenylethane-1,2-dione) analogues as inhibitors of mammalian carboxylesterases.
University of Mississippi
Design, synthesis and X-ray structure of protein-ligand complexes: important insight into selectivity of memapsin 2 (beta-secretase) inhibitors.
Purdue University