5VBQ

CRYSTAL STRUCTURE OF THE FIRST BROMODOMAIN OF HUMAN BRDT IN COMPLEX WITH BI2536

5VBQ の概要

• エントリーDOI: 10.2210/pdb5vbq/pdb
• 関連するPDBエントリー: 5VBO 5VBP 5VBR
• 分子名称: Bromodomain testis-specific protein, 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, CHLORIDE ION, ... (5 entities in total)
• 機能のキーワード: bromodomain, cap, hunk1, mcap, protein binding-inhibitor complex, mitotic chromosome associated protein, inhibitor, transcription-inhibitor complex, transcription/inhibitor
• 由来する生物種: Homo sapiens (Human)
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 28710.58

構造登録者

EMBER, S.W.,ZHU, J.-Y.,SCHONBRUNN, E. (登録日: 2017-03-30, 公開日: 2018-04-04, 最終更新日: 2023-10-04)

• 主引用文献: Karim, R.M.,Bikowitz, M.J.,Chan, A.,Zhu, J.Y.,Grassie, D.,Becker, A.,Berndt, N.,Gunawan, S.,Lawrence, N.J.,Schonbrunn, E.; Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.; J.Med.Chem., 2021; PubMed: 34710325; DOI: 10.1021/acs.jmedchem.1c01096

実験手法

X-RAY DIFFRACTION (1.65 Å)