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The SERM/SERD Bazedoxifene Disrupts ESR1 Helix 12 to Overcome Acquired Hormone Resistance in Breast Cancer Cells
Sean W. Fanning,
Christopher G. Mayne,
Colin E Fowler,
Kathryn E Carlson,
Teresa A Martin,
David J Hosfield,
Kendall W Nettles,
Patrick R. Griffin,
John A Katzenellenbogen,
Geoffrey L. Greene
Posted 23 Apr 2018
bioRxiv DOI: 10.1101/306472 (published DOI: 10.7554/elife.37161)
Posted 23 Apr 2018
Acquired resistance to endocrine therapy remains a significant clinical burden for breast cancer patients. Somatic mutations in the ESR1 (estrogen receptor alpha (ERα) gene ligand-binding domain (LBD) represent a recognized mechanism of acquired resistance. Antiestrogens with improved efficacy versus tamoxifen might overcome the resistant phenotype in ER+ breast cancers. Bazedoxifene (BZA) is a potent antiestrogen that is clinically approved for use in hormone replacement therapies. We find BZA possesses improved inhibitory potency against the Y537S and D538G ERα mutants compared to tamoxifen and has additional inhibitory activity in combination with the CDK4/6 inhibitor palbociclib. In addition, comprehensive biophysical and structural biology studies show that BZA’s selective estrogen receptor degrading (SERD) properties that override the stabilizing effects of the Y537S and D538G ERα mutations.
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