登録情報 データベース : PDB / ID : 5ls6 構造の表示 ダウンロードとリンクタイトル Structure of Human Polycomb Repressive Complex 2 (PRC2) with inhibitor 要素(Polycomb protein ...) x 2 Histone-lysine N-methyltransferase EZH2,Histone-lysine N-methyltransferase EZH2,Histone-lysine N-methyltransferase EZH2 Jarid2 K116me3 詳細キーワード Transferase/Inhibitor / Human PRC2 / Inhibitor / H3K27 / Transferase-Inhibitor complex機能・相同性 機能・相同性情報分子機能 ドメイン・相同性 構成要素
protein localization to pericentric heterochromatin / hepatocyte homeostasis / cellular response to trichostatin A / regulation of gliogenesis / negative regulation of striated muscle cell differentiation / regulation of kidney development / [histone H3]-lysine27 N-trimethyltransferase / response to tetrachloromethane / negative regulation of keratinocyte differentiation / histone H3K27 trimethyltransferase activity ... protein localization to pericentric heterochromatin / hepatocyte homeostasis / cellular response to trichostatin A / regulation of gliogenesis / negative regulation of striated muscle cell differentiation / regulation of kidney development / [histone H3]-lysine27 N-trimethyltransferase / response to tetrachloromethane / negative regulation of keratinocyte differentiation / histone H3K27 trimethyltransferase activity / negative regulation of retinoic acid receptor signaling pathway / cerebellar cortex development / primary miRNA binding / random inactivation of X chromosome / regulatory ncRNA-mediated heterochromatin formation / regulation of adaxial/abaxial pattern formation / skeletal muscle satellite cell maintenance involved in skeletal muscle regeneration / negative regulation of cardiac muscle cell proliferation / histone H3K27 methyltransferase activity / sex chromatin / ubiquitin-modified histone reader activity / positive regulation of cell cycle G1/S phase transition / facultative heterochromatin formation / genomic imprinting / ESC/E(Z) complex / RSC-type complex / negative regulation of stem cell differentiation / protein-lysine N-methyltransferase activity / cardiac muscle hypertrophy in response to stress / chromatin silencing complex / histone H3K9me2/3 reader activity / pronucleus / G1 to G0 transition / positive regulation of dendrite development / histone H3 methyltransferase activity / histone methyltransferase activity / DNA methylation-dependent constitutive heterochromatin formation / negative regulation of G1/S transition of mitotic cell cycle / spinal cord development / lncRNA binding / negative regulation of gene expression, epigenetic / synaptic transmission, GABAergic / Transcriptional Regulation by E2F6 / : / positive regulation of MAP kinase activity / histone methyltransferase complex / pericentric heterochromatin / oligodendrocyte differentiation / negative regulation of transcription elongation by RNA polymerase II / negative regulation of cell differentiation / positive regulation of GTPase activity / positive regulation of protein serine/threonine kinase activity / cardiac muscle cell proliferation / positive regulation of epithelial to mesenchymal transition / subtelomeric heterochromatin formation / ribonucleoprotein complex binding / RNA polymerase II core promoter sequence-specific DNA binding / nucleosome binding / keratinocyte differentiation / spleen development / protein localization to chromatin / negative regulation of cytokine production involved in inflammatory response / liver regeneration / SUMOylation of chromatin organization proteins / thymus development / cellular response to leukemia inhibitory factor / B cell differentiation / Regulation of PTEN gene transcription / ubiquitin binding / central nervous system development / transcription corepressor binding / PRC2 methylates histones and DNA / Defective pyroptosis / stem cell differentiation / hippocampus development / enzyme activator activity / promoter-specific chromatin binding / chromatin DNA binding / liver development / G1/S transition of mitotic cell cycle / regulation of circadian rhythm / protein-DNA complex / PKMTs methylate histone lysines / protein modification process / Activation of anterior HOX genes in hindbrain development during early embryogenesis / cellular response to hydrogen peroxide / HCMV Early Events / rhythmic process / transcription corepressor activity / heterochromatin formation / response to estradiol / regulation of gene expression / chromosome / chromatin organization / Oxidative Stress Induced Senescence / histone binding / methylation / chromosome, telomeric region / cell population proliferation / nuclear body 類似検索 - 分子機能 Polycomb protein SUZ12-like, Zn domain / EZH2, SET domain / Polycomb protein, VEFS-Box / VEFS-Box of polycomb protein / 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 ... Polycomb protein SUZ12-like, Zn domain / EZH2, SET domain / Polycomb protein, VEFS-Box / VEFS-Box of polycomb protein / 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 / Ezh2, MCSS domain / Tesmin/TSO1-like CXC domain / Tesmin/TSO1-like CXC domain / CXC domain / Histone-lysine N-methyltransferase EZH1/2-like / CXC domain profile. / : / Zinc finger, C5HC2-type / C5HC2 zinc finger / ARID DNA-binding domain / ARID DNA-binding domain superfamily / ARID/BRIGHT DNA binding domain / ARID domain profile. / BRIGHT, ARID (A/T-rich interaction domain) domain / ARID/BRIGHT DNA binding domain / JmjN domain / JmjN domain profile. / Small domain found in the jumonji family of transcription factors / A domain family that is part of the cupin metalloenzyme superfamily. / JmjC domain / JmjC domain profile. / jmjN domain / SET (Su(var)3-9, Enhancer-of-zeste, Trithorax) domain / SET domain / JmjC domain, hydroxylase / SET domain superfamily / SET domain profile. / SET domain / SANT SWI3, ADA2, N-CoR and TFIIIB'' DNA-binding domains / SANT/Myb domain / Zinc finger C2H2 type domain signature. / YVTN repeat-like/Quinoprotein amine dehydrogenase / 7 Propeller / Methylamine Dehydrogenase; Chain H / WD domain, G-beta repeat / WD40 repeat, conserved site / Trp-Asp (WD) repeats signature. / Trp-Asp (WD) repeats profile. / Trp-Asp (WD) repeats circular profile. / 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-74D / Polycomb protein EED / Polycomb protein SUZ12 / Histone-lysine N-methyltransferase EZH2 / Protein Jumonji 類似検索 - 構成要素生物種 Homo sapiens (ヒト)手法 X線回折 / シンクロトロン / 分子置換 / 解像度 : 3.47 Å 詳細データ登録者 Zhang, Y. / Justin, N. / Chen, S. / Wilson, J. / Gamblin, S. 引用ジャーナル : J. Med. Chem. / 年 : 2016タイトル: 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 ... タイトル : 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 Lymphomas.著者: Vaswani, R.G. / Gehling, V.S. / Dakin, L.A. / Cook, A.S. / Nasveschuk, C.G. / Duplessis, M. / Iyer, P. / Balasubramanian, S. / Zhao, F. / Good, A.C. / Campbell, R. / Lee, C. / Cantone, N. / ... 著者 : Vaswani, R.G. / Gehling, V.S. / Dakin, L.A. / Cook, A.S. / Nasveschuk, C.G. / Duplessis, M. / Iyer, P. / Balasubramanian, S. / Zhao, F. / Good, A.C. / Campbell, R. / Lee, C. / Cantone, N. / Cummings, R.T. / Normant, E. / Bellon, S.F. / Albrecht, B.K. / Harmange, J.C. / Trojer, P. / Audia, J.E. / Zhang, Y. / Justin, N. / Chen, S. / Wilson, J.R. / Gamblin, S.J. 履歴 登録 2016年8月22日 登録サイト : PDBE / 処理サイト : PDBE改定 1.0 2017年2月22日 Provider : repository / タイプ : Initial release改定 1.1 2019年2月20日 Group : Advisory / Data collection / Derived calculationsカテゴリ : diffrn_source / pdbx_data_processing_status ... diffrn_source / pdbx_data_processing_status / pdbx_validate_close_contact / struct_conn Item : _diffrn_source.pdbx_synchrotron_site改定 1.2 2019年7月10日 Group : Data collection / カテゴリ : diffrn_source / Item : _diffrn_source.pdbx_synchrotron_site改定 1.3 2024年1月17日 Group : Data collection / Database references ... Data collection / Database references / Derived calculations / Refinement description カテゴリ : chem_comp_atom / chem_comp_bond ... chem_comp_atom / chem_comp_bond / database_2 / pdbx_initial_refinement_model / pdbx_struct_conn_angle / struct_conn / struct_conn_type Item : _database_2.pdbx_DOI / _database_2.pdbx_database_accession ... _database_2.pdbx_DOI / _database_2.pdbx_database_accession / _pdbx_struct_conn_angle.ptnr1_auth_comp_id / _pdbx_struct_conn_angle.ptnr1_auth_seq_id / _pdbx_struct_conn_angle.ptnr1_label_atom_id / _pdbx_struct_conn_angle.ptnr1_label_comp_id / _pdbx_struct_conn_angle.ptnr1_label_seq_id / _pdbx_struct_conn_angle.ptnr2_auth_seq_id / _pdbx_struct_conn_angle.ptnr2_label_asym_id / _pdbx_struct_conn_angle.ptnr3_auth_comp_id / _pdbx_struct_conn_angle.ptnr3_auth_seq_id / _pdbx_struct_conn_angle.ptnr3_label_atom_id / _pdbx_struct_conn_angle.ptnr3_label_comp_id / _pdbx_struct_conn_angle.ptnr3_label_seq_id / _pdbx_struct_conn_angle.value / _struct_conn.conn_type_id / _struct_conn.id / _struct_conn.pdbx_dist_value / _struct_conn.pdbx_leaving_atom_flag / _struct_conn.ptnr1_auth_asym_id / _struct_conn.ptnr1_auth_comp_id / _struct_conn.ptnr1_auth_seq_id / _struct_conn.ptnr1_label_asym_id / _struct_conn.ptnr1_label_atom_id / _struct_conn.ptnr1_label_comp_id / _struct_conn.ptnr1_label_seq_id / _struct_conn.ptnr2_auth_asym_id / _struct_conn.ptnr2_auth_comp_id / _struct_conn.ptnr2_auth_seq_id / _struct_conn.ptnr2_label_asym_id / _struct_conn.ptnr2_label_atom_id / _struct_conn.ptnr2_label_comp_id / _struct_conn.ptnr2_label_seq_id / _struct_conn_type.id
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