5DFD

Crystal structure of BRD2(BD2) W370F mutant with ligand 28 bound

5DFD の概要

• エントリーDOI: 10.2210/pdb5dfd/pdb
• 分子名称: Bromodomain-containing protein 2, methyl [(4S)-6-(1H-indol-4-yl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]acetate, GLYCEROL, ... (4 entities in total)
• 機能のキーワード: transcription factors, bet bromodomains, protein mutation engineering, molecular probes, transcription
• 由来する生物種: Homo sapiens (Human)
• 細胞内の位置: Nucleus : P25440
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 13843.91

構造登録者

Tallant, C.,Baud, M.,Lin-Shiao, E.,Chirgadze, D.Y.,Ciulli, A. (登録日: 2015-08-26, 公開日: 2015-11-11, 最終更新日: 2024-01-10)

• 主引用文献: Baud, M.G.,Lin-Shiao, E.,Zengerle, M.,Tallant, C.,Ciulli, A.; New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition.; J.Med.Chem., 59:1492-1500, 2016; PubMed: 26367539; DOI: 10.1021/acs.jmedchem.5b01135

実験手法

X-RAY DIFFRACTION (1.5 Å)