6SBO

Estrogen receptor mutant L536S

6SBO の概要

• エントリーDOI: 10.2210/pdb6sbo/pdb
• 分子名称: Estrogen receptor, 6-(2,4-dichlorophenyl)-5-[4-[(3~{S})-1-(3-fluoranylpropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7~{H}-benzo[7]annulene-2-carboxylic acid (3 entities in total)
• 機能のキーワード: receptor, transcription
• 由来する生物種: Homo sapiens (Human)
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 60326.70

構造登録者

Vallee, F.,Steier, V.,Rak, A. (登録日: 2019-07-22, 公開日: 2019-11-27, 最終更新日: 2024-05-15)

• 主引用文献: El-Ahmad, Y.,Tabart, M.,Halley, F.,Certal, V.,Thompson, F.,Filoche-Romme, B.,Gruss-Leleu, F.,Muller, C.,Brollo, M.,Fabien, L.,Loyau, V.,Bertin, L.,Richepin, P.,Pilorge, F.,Desmazeau, P.,Girardet, C.,Beccari, S.,Louboutin, A.,Lebourg, G.,Le-Roux, J.,Terrier, C.,Vallee, F.,Steier, V.,Mathieu, M.,Rak, A.,Abecassis, P.Y.,Vicat, P.,Benard, T.,Bouaboula, M.,Sun, F.,Shomali, M.,Hebert, A.,Levit, M.,Cheng, H.,Courjaud, A.,Ginesty, C.,Perrault, C.,Garcia-Echeverria, C.,McCort, G.,Schio, L.; Discovery of 6-(2,4-Dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylic acid (SAR439859), a Potent and Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen-Receptor-Positive Breast Cancer.; J.Med.Chem., 63:512-528, 2020; PubMed: 31721572; DOI: 10.1021/acs.jmedchem.9b01293

実験手法

X-RAY DIFFRACTION (1.48 Å)