Article
Giredestrant reverses progesterone hypersensitivity driven by estrogen receptor mutations in breast cancer.
Science translational medicine - 21 Sept 2022
Liang Jackson, Ingalla Ellen Rei, Yao Xiaosai, Wang Bu-Er, Tai Lisa, Giltnane Jennifer, Liang Yuxin, Daemen Anneleen, Moore Heather M, Aimi Junko, Chang Ching-Wei, Gates Mary R, Eng-Wong Jennifer, Tam Lucinda, Bacarro Natasha, Roose-Girma Merone, Bellet Meritxell, Hafner Marc, Metcalfe Ciara
Abstract excerpt
ESR1 (estrogen receptor 1) hotspot mutations are major contributors to therapeutic resistance in estrogen receptor-positive (ER+) breast cancer. Such mutations confer estrogen independence to ERα, providing a selective advantage in the presence of estrogen-depleting aromatase inhibitors. In addition, ESR1 mutations reduce the potency of tamoxifen and fulvestrant, therapies that bind ERα directly. These...
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