Article
Targeted degradation of activating estrogen receptor α ligand-binding domain mutations in human breast cancer.
Breast cancer research and treatment - 1 Apr 2020
Gonzalez Thomas L, Hancock Molly, Sun Siqi, Gersch Christina L, Larios Jose M, David Wadie, Hu Jiantao, Hayes Daniel F, Wang Shaomeng, Rae James M
Abstract excerpt
PURPOSE: Studies have identified several estrogen receptor α (ERα) ligand-binding domain (LBD) somatic mutations in endocrine therapy resistant, metastatic ER-positive breast cancers. The most common mutations, Tyr537Ser (Y537S) and Asp538Gly (D538G), are detected in ~ 30% of endocrine resistant metastatic breast cancer patients. These ESR1 mutations induce the agonist conformation of ERα, confer an...
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