登録情報 | データベース: PDB / ID: 4lrg |
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タイトル | Structure of BRD4 bromodomain 1 with a dimethyl thiophene isoxazole azepine carboxamide |
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要素 | Bromodomain-containing protein 4 |
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キーワード | TRANSCRIPTION REGULATOR/INHIBITOR / BET inhibitor / Brd4 first bromodomain / TRANSCRIPTION REGULATOR-INHIBITOR complex |
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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 / 分子置換 / 解像度: 2.21 Å |
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データ登録者 | Ravichandran, S. / Jayaram, H. / Poy, F. / Gehling, V. / Hewitt, M. / Vaswani, R. / Leblanc, Y. / Cote, A. / Nasveschuk, C. / Taylor, A. ...Ravichandran, S. / Jayaram, H. / Poy, F. / Gehling, V. / Hewitt, M. / Vaswani, R. / Leblanc, Y. / Cote, A. / Nasveschuk, C. / Taylor, A. / Harmange, J.-C. / Audia, J. / Pardo, E. / Joshi, S. / Sandy, P. / Mertz, J. / Sims, R. / Bergeron, L. / Bryant, B. / Yellapuntala, S. / Nandana, B.S. / Birudukota, S. / Albrecht, B. / Bellon, S. |
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引用 | ジャーナル: ACS Med Chem Lett / 年: 2013 タイトル: Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors. 著者: Gehling, V.S. / Hewitt, M.C. / Vaswani, R.G. / Leblanc, Y. / Cote, A. / Nasveschuk, C.G. / Taylor, A.M. / Harmange, J.C. / Audia, J.E. / Pardo, E. / Joshi, S. / Sandy, P. / Mertz, J.A. / ...著者: Gehling, V.S. / Hewitt, M.C. / Vaswani, R.G. / Leblanc, Y. / Cote, A. / Nasveschuk, C.G. / Taylor, A.M. / Harmange, J.C. / Audia, J.E. / Pardo, E. / Joshi, S. / Sandy, P. / Mertz, J.A. / Sims, R.J. / Bergeron, L. / Bryant, B.M. / Bellon, S. / Poy, F. / Jayaram, H. / Sankaranarayanan, R. / Yellapantula, S. / Bangalore Srinivasamurthy, N. / Birudukota, S. / Albrecht, B.K. |
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履歴 | 登録 | 2013年7月19日 | 登録サイト: RCSB / 処理サイト: RCSB |
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改定 1.0 | 2013年8月7日 | Provider: repository / タイプ: Initial release |
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改定 1.1 | 2013年8月14日 | Group: Other / Structure summary |
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改定 1.2 | 2014年10月8日 | Group: Database references |
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改定 1.3 | 2017年11月15日 | Group: Refinement description / カテゴリ: software / Item: _software.name |
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改定 1.4 | 2024年2月28日 | Group: Data collection / Database references / Derived calculations カテゴリ: chem_comp_atom / chem_comp_bond ...chem_comp_atom / chem_comp_bond / database_2 / struct_ref_seq_dif / struct_site Item: _database_2.pdbx_DOI / _database_2.pdbx_database_accession ..._database_2.pdbx_DOI / _database_2.pdbx_database_accession / _struct_ref_seq_dif.details / _struct_site.pdbx_auth_asym_id / _struct_site.pdbx_auth_comp_id / _struct_site.pdbx_auth_seq_id |
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