Stereospecific lasofoxifene derivatives reveal the interplay between estrogen receptor alpha stability and antagonistic activity in ESR1 mutant breast cancer cells

Stereospecific lasofoxifene derivatives reveal the interplay between estrogen receptor alpha stability and antagonistic activity in ESR1 mutant breast cancer cells

Chemical manipulation of estrogen receptor alpha ligand binding domain structural mobility tunes receptor lifetime and influences breast cancer therapeutic activities. Selective estrogen receptor modulators (SERMs) extend estrogen receptor alpha (ERα) cellular lifetime/accumulation. They are antagon...

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Bibliographic Details
Main Authors: David J Hosfield, Sandra Weber, Nan-Sheng Li, Madline Sauvage, Carstyn F Joiner, Govinda R Hancock, Emily A Sullivan, Estelle Ndukwe, Ross Han, Sydney Cush, Muriel Lainé, Sylvie C Mader, Geoffrey L Greene, Sean W Fanning
Format: Article
Language:English
Published: eLife Sciences Publications Ltd 2022-05-01
Series:eLife
Subjects:
breast cancer
Y537S ESR1 Mutation
antiestrogen
hormone resistance
drug resistance
estrogen receptor degradation
Online Access:https://elifesciences.org/articles/72512

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