Article
Stereospecific lasofoxifene derivatives reveal the interplay between estrogen receptor alpha stability and antagonistic activity in ESR1 mutant breast cancer cells.
eLife - 16 May 2022
Hosfield David J, Weber Sandra, Li Nan-Sheng, Sauvage Madline, Joiner Carstyn F, Hancock Govinda R, Sullivan Emily A, Ndukwe Estelle, Han Ross, Cush Sydney, Lainé Muriel, Mader Sylvie C, Greene Geoffrey L, Fanning Sean W
Abstract excerpt
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 antagonists in the breast but agonists in the uterine epithelium and/or in bone. Selective estrogen receptor...
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