6Z8P

C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH GSK973

これはPDB形式変換不可エントリーです。

6Z8P の概要

• エントリーDOI: 10.2210/pdb6z8p/pdb
• 分子名称: Bromodomain-containing protein 2, 1,2-ETHANEDIOL, 2-(2-{2-[2-(2-METHOXY-ETHOXY)-ETHOXY]-ETHOXY}-ETHOXY)-ETHANOL, ... (5 entities in total)
• 機能のキーワード: inhibitor, histone, epigenetic reader, bromodomain, brd2, bromodomain containing protein 2, antagonist, transcription
• 由来する生物種: Homo sapiens (Human)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 14281.41

構造登録者

Chung, C. (登録日: 2020-06-02, 公開日: 2020-10-21, 最終更新日: 2024-05-01)

主引用文献

Preston, A.,Atkinson, S.J.,Bamborough, P.,Chung, C.W.,Gordon, L.J.,Grandi, P.,Gray, J.R.J.,Harrison, L.A.,Lewis, A.J.,Lugo, D.,Messenger, C.,Michon, A.M.,Mitchell, D.J.,Prinjha, R.K.,Rioja, I.,Seal, J.,Taylor, S.,Thesmar, P.,Wall, I.D.,Watson, R.J.,Woolven, J.M.,Demont, E.H.
GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family.
Acs Med.Chem.Lett., 11:1581-1587, 2020

PubMed Abstract: Pan-BET inhibitors have shown profound efficacy in a number of in vivo preclinical models and have entered the clinic in oncology trials where adverse events have been reported. These inhibitors interact equipotently with the eight bromodomains of the BET family of proteins. To better understand the contribution of each domain to their efficacy and to improve from their safety profile, selective inhibitors are required. This Letter discloses the profile of GSK973, a highly selective inhibitor of the second bromodomains of the BET proteins that has undergone extensive preclinical in vitro and in vivo characterization.

PubMed: 32832027
DOI: 10.1021/acsmedchemlett.0c00247

実験手法

X-RAY DIFFRACTION (1.55 Å)