Histone deacetylase inhibitors down-regulate G-protein-coupled estrogen receptor and the GPER-antagonist G-15 inhibits proliferation in endometriotic cells
Histone deacetylase inhibitors reduce GPER expression, and the GPER antagonist G-15 inhibits endometriotic cell proliferation.
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This paper investigated in vitro whether histone deacetylase inhibitors reduce expression of the G-protein-coupled estrogen receptor (GPER) and whether blocking GPER with the antagonist G-15 decreases proliferation of endometriotic cells. Using immortalized epithelial endometriotic cells, the authors treated cells with the histone deacetylase inhibitors romidepsin or SAHA, and/or with G-15, and assessed GPER-related outcomes and cell proliferation. The study found that histone deacetylase inhibitors down-regulated GPER expression and that the GPER antagonist G-15 inhibited proliferation in endometriotic cells, supporting a role for GPER in endometriotic cell growth. A key limitation is that experiments were performed only in immortalized epithelial endometriotic cells in a university-hospital in vitro setting. This paper is centrally about endometriosis — it examines how histone deacetylase inhibitors regulate GPER and how GPER inhibition affects proliferation in endometriotic cells.
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