登録情報 | データベース: PDB / ID: 5h24 |
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タイトル | EED in complex with PRC2 allosteric inhibitor compound 8 |
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要素 | - Histone-lysine N-methyltransferase EZH2
- Polycomb protein EED
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キーワード | Transferase/Transferase Inhibitor / EED / PRC2 / inhibitor / Transferase-Transferase Inhibitor complex |
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機能・相同性 | 機能・相同性情報
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類似検索 - 分子機能 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類似検索 - ドメイン・相同性 Chem-LQG / Polycomb protein EED / Histone-lysine N-methyltransferase EZH2類似検索 - 構成要素 |
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生物種 | Homo sapiens (ヒト) |
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手法 | X線回折 / シンクロトロン / 分子置換 / 解像度: 2.5 Å |
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データ登録者 | Zhao, K. / Zhao, M. / Luo, X. / Zhang, H. |
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引用 | ジャーナル: J. Med. Chem. / 年: 2017 タイトル: Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy 著者: 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. / ...著者: 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. |
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履歴 | 登録 | 2016年10月14日 | 登録サイト: PDBJ / 処理サイト: PDBJ |
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改定 1.0 | 2017年1月25日 | Provider: repository / タイプ: Initial release |
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改定 1.1 | 2017年4月5日 | Group: Database references |
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改定 1.2 | 2023年11月8日 | Group: Data collection / Database references / Refinement description カテゴリ: 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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