登録情報 | データベース: PDB / ID: 5dt2 |
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タイトル | Crystal structure of Dot1L in complex with inhibitor CPD11 [N4-methyl-N2-(2-methyl-1-(2-phenoxyphenyl)-1H-indol-6-yl)pyrimidine-2,4-diamine] |
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要素 | Histone-lysine N-methyltransferase, H3 lysine-79 specific |
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キーワード | TRANSFERASE / Inhibitor / Complex / Methyltransferase |
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機能・相同性 | 機能・相同性情報
histone H3K79 trimethyltransferase activity / [histone H3]-lysine79 N-trimethyltransferase / histone H3K79 methyltransferase activity / regulation of transcription regulatory region DNA binding / histone H3 methyltransferase activity / regulation of receptor signaling pathway via JAK-STAT / histone methyltransferase activity / heterochromatin formation / telomere organization / DNA damage checkpoint signaling ...histone H3K79 trimethyltransferase activity / [histone H3]-lysine79 N-trimethyltransferase / histone H3K79 methyltransferase activity / regulation of transcription regulatory region DNA binding / histone H3 methyltransferase activity / regulation of receptor signaling pathway via JAK-STAT / histone methyltransferase activity / heterochromatin formation / telomere organization / DNA damage checkpoint signaling / PKMTs methylate histone lysines / gene expression / methylation / RNA polymerase II-specific DNA-binding transcription factor binding / nucleic acid binding / transcription coactivator activity / intracellular membrane-bounded organelle / DNA repair / positive regulation of cell population proliferation / positive regulation of transcription by RNA polymerase II / protein-containing complex / DNA binding / nucleoplasm / nucleus / cytoplasm類似検索 - 分子機能 434 Repressor (Amino-terminal Domain) - #60 / Histone H3-K79 methyltransferase, metazoa / Histone-lysine N-methyltransferase DOT1 domain / Histone H3-K79 methyltransferase / Histone methylation protein DOT1 / Histone-lysine N-methyltransferase DOT1 (EC 2.1.1.43) domain profile. / 434 Repressor (Amino-terminal Domain) / Vaccinia Virus protein VP39 / S-adenosyl-L-methionine-dependent methyltransferase superfamily / Rossmann fold ...434 Repressor (Amino-terminal Domain) - #60 / Histone H3-K79 methyltransferase, metazoa / Histone-lysine N-methyltransferase DOT1 domain / Histone H3-K79 methyltransferase / Histone methylation protein DOT1 / Histone-lysine N-methyltransferase DOT1 (EC 2.1.1.43) domain profile. / 434 Repressor (Amino-terminal Domain) / Vaccinia Virus protein VP39 / S-adenosyl-L-methionine-dependent methyltransferase superfamily / Rossmann fold / Orthogonal Bundle / 3-Layer(aba) Sandwich / Mainly Alpha / Alpha Beta類似検索 - ドメイン・相同性 Chem-5EV / Histone-lysine N-methyltransferase, H3 lysine-79 specific類似検索 - 構成要素 |
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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: 2.3 Å |
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データ登録者 | Scheufler, C. / Gaul, C. / Be, C. / Moebitz, H. |
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引用 | ジャーナル: Acs Med.Chem.Lett. / 年: 2016 タイトル: Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach. 著者: Chen, C. / Zhu, H. / Stauffer, F. / Caravatti, G. / Vollmer, S. / Machauer, R. / Holzer, P. / Mobitz, H. / Scheufler, C. / Klumpp, M. / Tiedt, R. / Beyer, K.S. / Calkins, K. / Guthy, D. / ...著者: Chen, C. / Zhu, H. / Stauffer, F. / Caravatti, G. / Vollmer, S. / Machauer, R. / Holzer, P. / Mobitz, H. / Scheufler, C. / Klumpp, M. / Tiedt, R. / Beyer, K.S. / Calkins, K. / Guthy, D. / Kiffe, M. / Zhang, J. / Gaul, C. |
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履歴 | 登録 | 2015年9月17日 | 登録サイト: RCSB / 処理サイト: PDBE |
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改定 1.0 | 2016年6月15日 | Provider: repository / タイプ: Initial release |
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改定 1.1 | 2016年9月7日 | Group: Database references |
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改定 1.2 | 2024年1月10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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