5MKZ

N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH 4-chloro-2-methyl-5-(((3-methylthiophen-2-yl)methyl)amino)pyridazin-3(2H)-one

5MKZ の概要

• エントリーDOI: 10.2210/pdb5mkz/pdb
• 分子名称: Bromodomain-containing protein 4, 4-chloranyl-2-methyl-5-[(3-methylthiophen-2-yl)methylamino]pyridazin-3-one, GLYCEROL, ... (4 entities in total)
• 機能のキーワード: inhibitor, histone, epigenetic reader, bromodomain, brd4, bromodomain containing protein 4, antagonist, transcription
• 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: 1
• 化学式量合計: 15645.41

構造登録者

Chung, C.-W. (登録日: 2016-12-05, 公開日: 2017-12-20, 最終更新日: 2024-05-08)

• 主引用文献: Humphreys, P.G.,Bamborough, P.,Chung, C.W.,Craggs, P.D.,Gordon, L.,Grandi, P.,Hayhow, T.G.,Hussain, J.,Jones, K.L.,Lindon, M.,Michon, A.M.,Renaux, J.F.,Suckling, C.J.,Tough, D.F.,Prinjha, R.K.; Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe.; J. Med. Chem., 60:695-709, 2017; PubMed: 28002667; DOI: 10.1021/acs.jmedchem.6b01566

実験手法

X-RAY DIFFRACTION (1.62 Å)