Estrogen Receptor Alpha Ligand Binding Domain in Complex with a Methylated Lasofoxifene Derivative with Selective Estrogen Receptor Degrader Properties

Estrogen Receptor Alpha Ligand Binding Domain in Complex with a Methylated Lasofoxifene Derivative with Selective Estrogen Receptor Degrader Properties Descriptor: (5R,6S)-5-(4-{2-[(3S)-3-methylpyrrolidin-1-yl]ethoxy}phenyl)-6-phenyl-5,6,7,8-tetrahydronaphthalen-2-ol, Estrogen receptor Authors: Hosfield, D.J, Greene, G.L, Fanning, S.W. Deposit date: 2022-03-30 Release date: 2022-06-15 Last modified: 2023-10-18 Method: X-RAY DIFFRACTION (1.7 Å) Cite: Stereospecific lasofoxifene derivatives reveal the interplay between estrogen receptor alpha stability and antagonistic activity in ESR1 mutant breast cancer cells. Elife, 11, 2022

与具有选择性雌激素受体降解剂（Selective Estrogen Receptor Degrader, SERD）特性的甲基化拉索昔芬衍生物结合的雌激素受体α（Estrogen Receptor Alpha, ERα）配体结合域，描述物：(5R,6S)-5-(4-{2-[(3S)-3-甲基吡咯烷-1-基]乙氧基}苯基)-6-苯基-5,6,7,8-四氢萘-2-醇、雌激素受体，作者：Hosfield, D.J.、Greene, G.L.、Fanning, S.W.，沉积日期：2022-03-30，发布日期：2022-06-15，最后修改日期：2023-10-18，实验方法：X射线衍射（分辨率1.7埃），引用文献：立体特异性拉索昔芬衍生物揭示ESR1突变乳腺癌细胞中雌激素受体α稳定性与拮抗活性的相互作用，《Elife》，第11卷，2022年