登録情報 | データベース: PDB / ID: 7axr |
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タイトル | Crystal structure of BRD4(1) bound to the dual BET-HDAC inhibitor LSH24 |
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要素 | Bromodomain-containing protein 4 |
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キーワード | PROTEIN BINDING / BRD4(1) / BRD4 / BD1 / first Bromodomain / Bromodomain / BET / HDAC / BETi / HDACi / dual Inhibitor / LSH24 |
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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 / chromatin / 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, conserved site / Bromodomain signature. ...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, conserved site / Bromodomain signature. / Bromodomain / Bromodomain profile. / bromo domain / Bromodomain / Bromodomain-like superfamily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: 1.5 Å |
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データ登録者 | Huegle, M. |
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資金援助 | ドイツ, 1件 組織 | 認可番号 | 国 |
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German Research Foundation (DFG) | GU1225 3 1 | ドイツ |
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引用 | ジャーナル: J.Med.Chem. / 年: 2021 タイトル: 4-Acyl Pyrrole Capped HDAC Inhibitors: A New Scaffold for Hybrid Inhibitors of BET Proteins and Histone Deacetylases as Antileukemia Drug Leads. 著者: Schaker-Hubner, L. / Warstat, R. / Ahlert, H. / Mishra, P. / Kraft, F.B. / Schliehe-Diecks, J. / Scholer, A. / Borkhardt, A. / Breit, B. / Bhatia, S. / Hugle, M. / Gunther, S. / Hansen, F.K. |
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履歴 | 登録 | 2020年11月10日 | 登録サイト: PDBE / 処理サイト: PDBE |
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改定 1.0 | 2021年10月6日 | Provider: repository / タイプ: Initial release |
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改定 1.1 | 2021年10月13日 | Group: Data collection / Database references カテゴリ: citation / citation_author ...citation / citation_author / database_PDB_rev / database_PDB_rev_record / pdbx_database_proc Item: _citation.pdbx_database_id_PubMed / _citation.title / _citation_author.name |
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改定 1.2 | 2021年10月27日 | Group: Data collection / Database references / カテゴリ: citation / pdbx_database_proc Item: _citation.journal_volume / _citation.page_first / _citation.page_last |
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改定 1.3 | 2024年1月31日 | Group: Data collection / Refinement description カテゴリ: chem_comp_atom / chem_comp_bond / pdbx_initial_refinement_model |
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