Modulation of Estrogen Receptor Alpha (ERα) and Tumor Suppressor Gene BRCA1 in Breast Cancer Cells by Bazedoxifene Acetate (BZA).
Document Type
Article
Publication Date
2-7-2024
Publication Title
Cancers
Abstract
Selective estrogen receptor modulators (SERMs) are steroid analogs with dual functionality, acting as partial estrogen receptor agonists to preserve postmenopausal bone density and as estrogen receptor antagonists in breast tissue. Bazedoxifene acetate (BZA) is an FDA-approved, third-generation SERM used in the treatment of osteoporosis in women. It demonstrates potential as a therapeutic option for breast cancer patients undergoing endocrine therapy. Our study aimed to assess BZA's effects on Estrogen Receptor Alpha (ERα) and tumor suppressor gene BRCA1 in T-47D and MCF-7 breast cancer cells, using Western blots, cellular viability, apoptosis assays, and RT-qPCR. Cells were cultured in 5% charcoal-stripped fetal bovine serum for six days to deplete endogenous steroids. Following a 24 h exposure to 2 µM BZA (optimal concentration determined from 1 nM-2 µM studies), Western blot analyses revealed reduced ERα and BRCA1 protein levels in both cell lines. ERα decreased by 48-63% and BRCA1 by 61-64%, indicating sensitivity to antiestrogens. Cytolocalization of ERα and BRCA1 remained unchanged after BZA and 17-β-estradiol (E
Volume
16
Issue
4
First Page
699
Recommended Citation
Szmyd M, Zanib A, Behlow V, Hallman E, Pfiffner S, Yaldo R, et al. [Farrar K]. Modulation of estrogen receptor alpha (ERα) and tumor suppressor gene BRCA1 in breast cancer cells by bazedoxifene acetate (BZA). Cancers. 2024 Feb 7;16(4):699. doi: 10.3390/cancers16040699. PMID: 38398090.
DOI
10.3390/cancers16040699
ISSN
2072-6694
PubMed ID
38398090
