6CHZ

Estrogen Receptor Alpha Y537S bound to antagonist H3B-9224.

6CHZ の概要

• エントリーDOI: 10.2210/pdb6chz/pdb
• 関連するPDBエントリー: 6CHW
• 分子名称: Estrogen receptor, 4-[(2-{4-[(1E)-1-(1H-indazol-5-yl)-2-phenylbut-1-en-1-yl]phenoxy}ethyl)amino]-N,N-dimethylbutanamide, 1,2-ETHANEDIOL, ... (4 entities in total)
• 機能のキーワード: nuclear hormone receptor, antagonist, activating mutation, breast cancer, nuclear protein, nuclear protein-antagonist complex, nuclear protein/antagonist
• 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: 30691.94

構造登録者

Larsen, N.A. (登録日: 2018-02-23, 公開日: 2018-03-21, 最終更新日: 2024-03-13)

• 主引用文献: Puyang, X.,Furman, C.,Zheng, G.Z.,Wu, Z.J.,Banka, D.,Aithal, K.,Agoulnik, S.,Bolduc, D.M.,Buonamici, S.,Caleb, B.,Das, S.,Eckley, S.,Fekkes, P.,Hao, M.H.,Hart, A.,Houtman, R.,Irwin, S.,Joshi, J.J.,Karr, C.,Kim, A.,Kumar, N.,Kumar, P.,Kuznetsov, G.,Lai, W.G.,Larsen, N.,Mackenzie, C.,Martin, L.A.,Melchers, D.,Moriarty, A.,Nguyen, T.V.,Norris, J.,O'Shea, M.,Pancholi, S.,Prajapati, S.,Rajagopalan, S.,Reynolds, D.J.,Rimkunas, V.,Rioux, N.,Ribas, R.,Siu, A.,Sivakumar, S.,Subramanian, V.,Thomas, M.,Vaillancourt, F.H.,Wang, J.,Wardell, S.,Wick, M.J.,Yao, S.,Yu, L.,Warmuth, M.,Smith, P.G.,Zhu, P.,Korpal, M.; Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ER alphaWTand ER alphaMUTBreast Cancer.; Cancer Discov, 8:1176-1193, 2018; PubMed: 29991605; DOI: 10.1158/2159-8290.CD-17-1229

実験手法

X-RAY DIFFRACTION (1.68 Å)