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Crystal structure of the second bromodomain (BD2) of human TAF1 bound to PLK1 kinase inhibitor BI2536

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Protein Data Bank Japan2023-10-18 更新2026-03-21 收录
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Crystal structure of the second bromodomain (BD2) of human TAF1 bound to PLK1 kinase inhibitor BI2536 Descriptor: 4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl]amino}-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide, Transcription initiation factor TFIID subunit 1 Authors: Karim, M.R, Schonbrunn, E. Deposit date: 2020-09-06 Release date: 2021-09-22 Last modified: 2023-10-18 Method: X-RAY DIFFRACTION (2.52 Å) Cite: Discovery of Dual TAF1-ATR Inhibitors and Ligand-Induced Structural Changes of the TAF1 Tandem Bromodomain. J.Med.Chem., 65, 2022

人源TAF1(全称为转录起始因子TFIID亚基1)的第二个溴结构域(bromodomain,BD2)与PLK1激酶抑制剂BI2536结合的晶体结构 配体标识符:4-{[(7R)-8-环戊基-7-乙基-5-甲基-6-氧代-5,6,7,8-四氢蝶啶-2-基]氨基}-3-甲氧基-N-(1-甲基哌啶-4-基)苯甲酰胺 作者:Karim, M.R.、Schonbrunn, E. 提交日期:2020-09-06 发布日期:2021-09-22 最后修改日期:2023-10-18 实验方法:X射线衍射(分辨率2.52埃) 引用文献:《双靶点TAF1-ATR抑制剂的发现及TAF1串联溴结构域的配体诱导构象变化》,J.Med.Chem., 65, 2022
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2020-09-06
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