5HLS

Crystal structure of the first bromodomain of human BRD4 bound to CPI-0610

5HLS の概要

• エントリーDOI: 10.2210/pdb5hls/pdb
• 分子名称: Bromodomain-containing protein 4, CPI-0610 (3 entities in total)
• 機能のキーワード: bromodomain, 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: 15492.15

構造登録者

Jayaram, H.,Poy, F.,Setser, J.W.,Bellon, S.F. (登録日: 2016-01-15, 公開日: 2016-02-10, 最終更新日: 2023-09-27)

• 主引用文献: Albrecht, B.K.,Gehling, V.S.,Hewitt, M.C.,Vaswani, R.G.,Cote, A.,Leblanc, Y.,Nasveschuk, C.G.,Bellon, S.,Bergeron, L.,Campbell, R.,Cantone, N.,Cooper, M.R.,Cummings, R.T.,Jayaram, H.,Joshi, S.,Mertz, J.A.,Neiss, A.,Normant, E.,O'Meara, M.,Pardo, E.,Poy, F.,Sandy, P.,Supko, J.,Sims, R.J.,Harmange, J.C.,Taylor, A.M.,Audia, J.E.; Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials.; J.Med.Chem., 59:1330-1339, 2016; PubMed: 26815195; DOI: 10.1021/acs.jmedchem.5b01882

実験手法

X-RAY DIFFRACTION (2.182 Å)