5ULA

Crystal Structure of the First Bromodomain of Human BRD4 in Complex With Cyclic Vinylogous Amide Inhibitor MS402

5ULA の概要

• エントリーDOI: 10.2210/pdb5ula/pdb
• 分子名称: Bromodomain-containing protein 4, 3-chloranyl-~{N}-(4-methoxyphenyl)-4-[(2-methyl-3-oxidanylidene-cyclopenten-1-yl)amino]benzamide (3 entities in total)
• 機能のキーワード: bromodomain, inhibitor, transcription, transcription-inhibitor complex, transcription/inhibitor
• 由来する生物種: Homo sapiens (Human)
• 細胞内の位置: Nucleus: O60885
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 30940.42

構造登録者

Plotnikov, A.N.,Joshua, j.,Zhou, M.-M. (登録日: 2017-01-24, 公開日: 2017-03-22, 最終更新日: 2024-03-06)

• 主引用文献: Cheung, K.,Lu, G.,Sharma, R.,Vincek, A.,Zhang, R.,Plotnikov, A.N.,Zhang, F.,Zhang, Q.,Ju, Y.,Hu, Y.,Zhao, L.,Han, X.,Meslamani, J.,Xu, F.,Jaganathan, A.,Shen, T.,Zhu, H.,Rusinova, E.,Zeng, L.,Zhou, J.,Yang, J.,Peng, L.,Ohlmeyer, M.,Walsh, M.J.,Zhang, D.Y.,Xiong, H.,Zhou, M.M.; BET N-terminal bromodomain inhibition selectively blocks Th17 cell differentiation and ameliorates colitis in mice.; Proc. Natl. Acad. Sci. U.S.A., 114:2952-2957, 2017; PubMed: 28265070; DOI: 10.1073/pnas.1615601114

実験手法

X-RAY DIFFRACTION (1.5 Å)