登録情報 | データベース: PDB / ID: 6mh7 |
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タイトル | Crystal structure of the first bromodomain of human BRD4 in complex with SKT-68, a 1,4,5-trisubstituted imidazole analogue |
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要素 | Bromodomain-containing protein 4 |
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キーワード | PROTEIN BINDING/INHIBITOR / bromodomain / CAP / HUNK1 / MCAP / PROTEIN BINDING-INHIBITOR complex / inhibitor / transcription-inhibitor complex / inflammation / 19F-NMR / MAP-kinase inhibition |
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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: 1.74 Å |
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データ登録者 | Zhu, J.-Y. / Schonbrunn, E. |
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資金援助 | 米国, 2件 組織 | 認可番号 | 国 |
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National Science Foundation (NSF, United States) | CHE-1352019 | 米国 | American Heart Association | 15SDG25710427 | 米国 |
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引用 | ジャーナル: J.Med.Chem. / 年: 2018 タイトル: Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor. 著者: Divakaran, A. / Talluri, S.K. / Ayoub, A.M. / Mishra, N.K. / Cui, H. / Widen, J.C. / Berndt, N. / Zhu, J.Y. / Carlson, A.S. / Topczewski, J.J. / Schonbrunn, E.K. / Harki, D.A. / Pomerantz, W.C.K. |
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履歴 | 登録 | 2018年9月17日 | 登録サイト: RCSB / 処理サイト: RCSB |
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改定 1.0 | 2019年8月7日 | Provider: repository / タイプ: Initial release |
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改定 1.1 | 2019年11月27日 | Group: Author supporting evidence / カテゴリ: pdbx_audit_support / Item: _pdbx_audit_support.funding_organization |
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改定 1.2 | 2023年10月11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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