6MH1

CRYSTAL STRUCTURE OF THE FIRST BROMODOMAIN OF HUMAN BRD4 IN COMPLEX WITH HU-10, A 1,4,5-Trisubstituted Imidazole Analogue

6MH1 の概要

• エントリーDOI: 10.2210/pdb6mh1/pdb
• 分子名称: Bromodomain-containing protein 4, N-(3,5-dimethylphenyl)-4-[4-(4-fluorophenyl)-1-(piperidin-4-yl)-1H-imidazol-5-yl]pyrimidin-2-amine, 1,2-ETHANEDIOL, ... (4 entities in total)
• 機能のキーワード: cap, hunk1, mcap, protein binding-inhibitor complex, inhibitor, transcription-inhibitor complex, inflammation, map-kinase inhibition, transcription-transcription inhibitor complex, transcription/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: 31270.03

構造登録者

Zhu, J.-Y.,Schonbrunn, E. (登録日: 2018-09-17, 公開日: 2019-08-07, 最終更新日: 2024-03-13)

• 主引用文献: Divakaran, A.,Talluri, S.K.,Ayoub, A.M.,Mishra, N.K.,Cui, H.,Widen, J.C.,Berndt, N.,Zhu, J.Y.,Carlson, A.S.,Topczewski, J.J.,Schonbrunn, E.K.,Harki, D.A.,Pomerantz, W.C.K.; Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.; J.Med.Chem., 61:9316-9334, 2018; PubMed: 30253095; DOI: 10.1021/acs.jmedchem.8b01248

実験手法

X-RAY DIFFRACTION (1.6 Å)