登録情報 | データベース: PDB / ID: 5khm |
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タイトル | The first BET bromodomain of BRD4 bound to compound 13 in a bivalent manner |
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要素 | Bromodomain-containing protein 4 |
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キーワード | Transcription Factor / bromodomain |
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機能・相同性 | 機能・相同性情報
RNA polymerase II C-terminal domain binding / negative regulation of DNA damage checkpoint / P-TEFb complex binding / negative regulation by host of viral transcription / positive regulation of T-helper 17 cell lineage commitment / positive regulation of G2/M transition of mitotic cell cycle / histone reader activity / RNA polymerase II CTD heptapeptide repeat kinase activity / condensed nuclear chromosome / positive regulation of transcription elongation by RNA polymerase II ...RNA polymerase II C-terminal domain binding / negative regulation of DNA damage checkpoint / P-TEFb complex binding / negative regulation by host of viral transcription / positive regulation of T-helper 17 cell lineage commitment / positive regulation of G2/M transition of mitotic cell cycle / histone reader activity / RNA polymerase II CTD heptapeptide repeat kinase activity / condensed nuclear chromosome / positive regulation of transcription elongation by RNA polymerase II / transcription coregulator activity / lysine-acetylated histone binding / p53 binding / chromosome / regulation of inflammatory response / positive regulation of canonical NF-kappaB signal transduction / Potential therapeutics for SARS / transcription coactivator activity / transcription cis-regulatory region binding / chromatin remodeling / DNA damage response / chromatin binding / regulation of transcription by RNA polymerase II / positive regulation of DNA-templated transcription / enzyme binding / positive regulation of transcription by RNA polymerase II / nucleoplasm / nucleus類似検索 - 分子機能 Bromodomain protein 4, C-terminal / C-terminal domain of bromodomain protein 4 / : / NET domain superfamily / NET domain profile. / Brdt, bromodomain, repeat II / Brdt, bromodomain, repeat I / NET domain / Bromodomain extra-terminal - transcription regulation / Bromodomain-like ...Bromodomain protein 4, C-terminal / C-terminal domain of bromodomain protein 4 / : / NET domain superfamily / NET domain profile. / Brdt, bromodomain, repeat II / Brdt, bromodomain, repeat I / NET domain / Bromodomain extra-terminal - transcription regulation / Bromodomain-like / Histone Acetyltransferase; Chain A / Bromodomain, conserved site / Bromodomain signature. / Bromodomain / Bromodomain profile. / bromo domain / Bromodomain / Bromodomain-like superfamily / Up-down Bundle / Mainly Alpha類似検索 - ドメイン・相同性 |
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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: 1.48 Å |
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データ登録者 | Patel, J. |
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引用 | ジャーナル: J.Med.Chem. / 年: 2016 タイトル: Optimization of a Series of Bivalent Triazolopyridazine Based Bromodomain and Extraterminal Inhibitors: The Discovery of (3R)-4-[2-[4-[1-(3-Methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)- ...タイトル: Optimization of a Series of Bivalent Triazolopyridazine Based Bromodomain and Extraterminal Inhibitors: The Discovery of (3R)-4-[2-[4-[1-(3-Methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-piperidyl]phenoxy]ethyl]-1,3-dimethyl-piperazin-2-one (AZD5153). 著者: Bradbury, R.H. / Callis, R. / Carr, G.R. / Chen, H. / Clark, E. / Feron, L. / Glossop, S. / Graham, M.A. / Hattersley, M. / Jones, C. / Lamont, S.G. / Ouvry, G. / Patel, A. / Patel, J. / ...著者: Bradbury, R.H. / Callis, R. / Carr, G.R. / Chen, H. / Clark, E. / Feron, L. / Glossop, S. / Graham, M.A. / Hattersley, M. / Jones, C. / Lamont, S.G. / Ouvry, G. / Patel, A. / Patel, J. / Rabow, A.A. / Roberts, C.A. / Stokes, S. / Stratton, N. / Walker, G.E. / Ward, L. / Whalley, D. / Whittaker, D. / Wrigley, G. / Waring, M.J. |
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履歴 | 登録 | 2016年6月15日 | 登録サイト: RCSB / 処理サイト: RCSB |
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改定 1.0 | 2016年9月21日 | Provider: repository / タイプ: Initial release |
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改定 1.1 | 2017年8月9日 | Group: Database references / Derived calculations / カテゴリ: citation / pdbx_struct_oper_list Item: _citation.journal_id_CSD / _pdbx_struct_oper_list.symmetry_operation |
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改定 1.2 | 2023年9月27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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