Entry Database : PDB / ID : 5h24 Structure visualization Downloads & linksTitle EED in complex with PRC2 allosteric inhibitor compound 8 ComponentsHistone-lysine N-methyltransferase EZH2 Polycomb protein EED DetailsKeywords Transferase/Transferase Inhibitor / EED / PRC2 / inhibitor / Transferase-Transferase Inhibitor complexFunction / homology Function and homology informationFunction Domain/homology Component
regulation of kidney development / hepatocyte homeostasis / cellular response to trichostatin A / regulation of gliogenesis / [histone H3]-lysine27 N-trimethyltransferase / negative regulation of striated muscle cell differentiation / negative regulation of keratinocyte differentiation / histone H3K27 trimethyltransferase activity / negative regulation of retinoic acid receptor signaling pathway / primary miRNA binding ... regulation of kidney development / hepatocyte homeostasis / cellular response to trichostatin A / regulation of gliogenesis / [histone H3]-lysine27 N-trimethyltransferase / negative regulation of striated muscle cell differentiation / negative regulation of keratinocyte differentiation / histone H3K27 trimethyltransferase activity / negative regulation of retinoic acid receptor signaling pathway / primary miRNA binding / regulatory ncRNA-mediated heterochromatin formation / skeletal muscle satellite cell maintenance involved in skeletal muscle regeneration / response to tetrachloromethane / cerebellar cortex development / facultative heterochromatin formation / histone H3K27 methyltransferase activity / positive regulation of cell cycle G1/S phase transition / ESC/E(Z) complex / chromatin silencing complex / protein-lysine N-methyltransferase activity / negative regulation of stem cell differentiation / pronucleus / cardiac muscle hypertrophy in response to stress / synaptic transmission, GABAergic / positive regulation of dendrite development / histone H3 methyltransferase activity / lncRNA binding / negative regulation of G1/S transition of mitotic cell cycle / G1 to G0 transition / negative regulation of gene expression, epigenetic / spinal cord development / histone methyltransferase activity / negative regulation of transcription elongation by RNA polymerase II / Transcriptional Regulation by E2F6 / subtelomeric heterochromatin formation / negative regulation of cytokine production involved in inflammatory response / RNA polymerase II core promoter sequence-specific DNA binding / pericentric heterochromatin / ribonucleoprotein complex binding / positive regulation of epithelial to mesenchymal transition / keratinocyte differentiation / protein localization to chromatin / enzyme activator activity / Regulation of PTEN gene transcription / liver regeneration / B cell differentiation / transcription corepressor binding / PRC2 methylates histones and DNA / positive regulation of MAP kinase activity / positive regulation of GTPase activity / Defective pyroptosis / stem cell differentiation / regulation of circadian rhythm / promoter-specific chromatin binding / hippocampus development / HCMV Early Events / PKMTs methylate histone lysines / protein modification process / positive regulation of protein serine/threonine kinase activity / G1/S transition of mitotic cell cycle / heterochromatin formation / chromatin DNA binding / Activation of anterior HOX genes in hindbrain development during early embryogenesis / cellular response to hydrogen peroxide / rhythmic process / chromosome / transcription corepressor activity / chromatin organization / response to estradiol / chromosome, telomeric region / Oxidative Stress Induced Senescence / methylation / positive regulation of cell migration / RNA polymerase II cis-regulatory region sequence-specific DNA binding / negative regulation of DNA-templated transcription / chromatin binding / positive regulation of cell population proliferation / synapse / chromatin / regulation of DNA-templated transcription / negative regulation of transcription by RNA polymerase II / nucleoplasm / identical protein binding / nucleus / cytosol Similarity search - Function EZH2, SET domain / : / Ezh2, MCSS domain / Histone-lysine N-methyltransferase EZH1/EZH2 / Polycomb repressive complex 2 subunit EZH1/EZH2, tri-helical domain / Pre-SET CXC domain / WD repeat binding protein EZH2 / Polycomb repressive complex 2 tri-helical domain / CXC domain / Tesmin/TSO1-like CXC domain ... EZH2, SET domain / : / Ezh2, MCSS domain / Histone-lysine N-methyltransferase EZH1/EZH2 / Polycomb repressive complex 2 subunit EZH1/EZH2, tri-helical domain / Pre-SET CXC domain / WD repeat binding protein EZH2 / Polycomb repressive complex 2 tri-helical domain / CXC domain / Tesmin/TSO1-like CXC domain / Tesmin/TSO1-like CXC domain / Histone-lysine N-methyltransferase EZH1/2-like / CXC domain / CXC domain profile. / : / SET (Su(var)3-9, Enhancer-of-zeste, Trithorax) domain / SET domain superfamily / SET domain / SET domain profile. / SET domain / SANT SWI3, ADA2, N-CoR and TFIIIB'' DNA-binding domains / SANT/Myb domain / YVTN repeat-like/Quinoprotein amine dehydrogenase / 7 Propeller / Methylamine Dehydrogenase; Chain H / WD40 repeat, conserved site / Trp-Asp (WD) repeats signature. / Trp-Asp (WD) repeats profile. / Trp-Asp (WD) repeats circular profile. / WD domain, G-beta repeat / WD40 repeats / WD40 repeat / WD40-repeat-containing domain superfamily / WD40/YVTN repeat-like-containing domain superfamily / Mainly Beta Similarity search - Domain/homologyBiological species Homo sapiens (human)Method X-RAY DIFFRACTION / SYNCHROTRON / MOLECULAR REPLACEMENT / Resolution : 2.5 Å DetailsAuthors Zhao, K. / Zhao, M. / Luo, X. / Zhang, H. CitationJournal : J. Med. Chem. / Year : 2017Title : Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer EfficacyAuthors: Huang, Y. / Zhang, J. / Yu, Z. / Zhang, H. / Wang, Y. / Lingel, A. / Qi, W. / Gu, J. / Zhao, K. / Shultz, M.D. / Wang, L. / Fu, X. / Sun, Y. / Zhang, Q. / Jiang, X. / Zhang, J. / Zhang, C. / ... Authors : Huang, Y. / Zhang, J. / Yu, Z. / Zhang, H. / Wang, Y. / Lingel, A. / Qi, W. / Gu, J. / Zhao, K. / Shultz, M.D. / Wang, L. / Fu, X. / Sun, Y. / Zhang, Q. / Jiang, X. / Zhang, J. / Zhang, C. / Li, L. / Zeng, J. / Feng, L. / Zhang, C. / Liu, Y. / Zhang, M. / Zhang, L. / Zhao, M. / Gao, Z. / Liu, X. / Fang, D. / Guo, H. / Mi, Y. / Gabriel, T. / Dillon, M.P. / Atadja, P. / Oyang, C. History Deposition Oct 14, 2016 Deposition site : PDBJ / Processing site : PDBJRevision 1.0 Jan 25, 2017 Provider : repository / Type : Initial releaseRevision 1.1 Apr 5, 2017 Group : Database referencesRevision 1.2 Nov 8, 2023 Group : Data collection / Database references / Refinement descriptionCategory : chem_comp_atom / chem_comp_bond ... chem_comp_atom / chem_comp_bond / database_2 / pdbx_initial_refinement_model Item : _database_2.pdbx_DOI / _database_2.pdbx_database_accession
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