Histone deacetylase inhibitors down-regulate G-protein-coupled estrogen receptor and the GPER-antagonist G-15 inhibits proliferation in endometriotic cells

组蛋白去乙酰化酶抑制剂下调 G 蛋白偶联雌激素受体,而 GPER 拮抗剂 G-15 抑制子宫内膜异位细胞增殖

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作者:Patrick Imesch, Eleftherios P Samartzis, Konstantin J Dedes, Daniel Fink, André Fedier

Objective

To investigate whether histone deacetylase inhibitors reduce the expression of the G-protein-coupled estrogen receptor (GPER) and whether the functional inhibition of GPER by the antagonist G-15 decreases the proliferation of endometriotic cells. Design: In vitro study. Setting: University hospital. Patient(s): Immortalized epithelial endometriotic cells. Intervention(s): Treatment with the histone deacetylase inhibitor romidepsin or suberoylanilide hydroxamic acid (SAHA), or with the GPER antagonist G-15. Main outcome measure(s): Western blot analysis and quantitative real-time polymerase chain reaction (PCR) were used to monitor the expression of GPER in response to drug treatment. Effects of GPER stimulation and inhibition on cell proliferation were investigated by the 93-(4,5-dimethylthiazol-2-yl)2,5-diphenyl tetrazolium bromide (Sigma) (MTT) assay. Result(s): Our

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