5MLJ

Bromodomain of Human GCN5 with 4-bromo-2-methyl-5-(((3R,5R)-1-methyl-5-phenylpiperidin-3-yl)amino)pyridazin-3(2H)-one

5MLJ の概要

• エントリーDOI: 10.2210/pdb5mlj/pdb
• 分子名称: Histone acetyltransferase KAT2A, 1,2-ETHANEDIOL, 4-bromo-2-methyl-5-[[(3~{R},5~{R})-1-methyl-5-phenyl-piperidin-3-yl]amino]pyridazin-3-one, ... (4 entities in total)
• 機能のキーワード: inhibitor, histone, epigenetic reader, bromodomain, gcn5, kat2a, antagonist, transcription
• 由来する生物種: Homo sapiens (Human)
• 細胞内の位置: Nucleus : Q92830
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 27453.32

構造登録者

Chung, C.-W. (登録日: 2016-12-06, 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 (1.8 Å)