7UJW

Estrogen Receptor Alpha Ligand Binding Domain Y537S Mutant in Complex with a Methylated Lasofoxifene Derivative that Possesses Selective Estrogen Receptor Degrader Activities

「6VVP」から置き換えられました

7UJW の概要

• エントリーDOI: 10.2210/pdb7ujw/pdb
• 分子名称: Estrogen receptor, (5R,6S)-5-(4-{2-[(3S)-3-methylpyrrolidin-1-yl]ethoxy}phenyl)-6-phenyl-5,6,7,8-tetrahydronaphthalen-2-ol (3 entities in total)
• 機能のキーワード: estrogen receptor alpha, y537s, activating mutation, antiestrogen, alpha helical bundle, transcription
• 由来する生物種: Homo sapiens (human)
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 122299.06

構造登録者

Hosfield, D.J.,Greene, G.L.,Fanning, S.W. (登録日: 2022-03-31, 公開日: 2022-06-15, 最終更新日: 2023-10-18)

• 主引用文献: Hosfield, D.J.,Weber, S.,Li, N.S.,Suavage, M.,Joiner, C.F.,Hancock, G.R.,Sullivan, E.A.,Ndukwe, E.,Han, R.,Cush, S.,Laine, M.,Mader, S.C.,Greene, G.L.,Fanning, S.W.; Stereospecific lasofoxifene derivatives reveal the interplay between estrogen receptor alpha stability and antagonistic activity in ESR1 mutant breast cancer cells.; Elife, 11:-, 2022; PubMed: 35575456; DOI: 10.7554/eLife.72512

実験手法

X-RAY DIFFRACTION (2.6 Å)