G protein–coupled estrogen receptor 1 agonist G-1 induces cell cycle arrest in the mitotic phase, leading to apoptosis in endometriosis

Taisuke Mori, Mori T, Fumitake Ito, Ito F, Matsushima H, Hiroshi Matsushima, Takaoka O, Osamu Takaoka, Tanaka Y, Yukiko Tanaka, Akemi Koshiba, Koshiba A, Kusuki I, Izumi Kusuki, Kitawaki J, Jo Kitawaki
Fertility and sterility · 2015 · vol. 103(5) , pp. 1228–1235.e1 · doi:10.1016/j.fertnstert.2015.01.026 · PMID:25724739 · W2059770258
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The G protein-coupled estrogen receptor 1 agonist G-1 was found to induce cell cycle arrest in the mitotic phase, ultimately leading to apoptosis in endometriosis.

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Abstract

ObjectiveTo demonstrate the effects of the selective G protein-coupled estrogen receptor 1 (GPER) agonist G-1 in human ovarian endometriotic stromal cells (ESCs).DesignExperimental in vitro study.SettingUniversity hospital.Patient(s)A total of 33 patients with ovarian endometrioma.Intervention(s)Endometriotic stromal cells from ovarian chocolate cysts were treated with the GPER agonist G-1.Main outcome measure(s)The primary outcomes were cell proliferation, measured using the WST-8 assay; cell cycle, as analyzed using flow cytometry, fluorescent immunocytochemistry, and cytotoxicity; caspase activity, as measured by fluorescent and luminescent enzyme assays; and protein expression levels, as determined by Western blot analysis.Result(s)G-1 suppressed ESC proliferation in a concentration-dependent manner. The inhibitory effect was not blocked when GPER signaling pathways, including the GPER itself, were inhibited. G-1 induced cell cycle arrest and accumulation in the sub-G1 phase in ESCs. Immunofluorescence analysis demonstrated that G-1 interrupted microtubule assembly at the mitotic phase. G-1 also induced caspase-3-dependent apoptosis without significant cytotoxicity.Conclusion(s)G-1 suppressed proliferation and induced apoptosis in ESCs, suggesting the potential use of this compound as a therapeutic drug for the treatment of endometriosis.

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Condition tags

endometriosis

MeSH descriptors

Apoptosis Cell Proliferation Cyclopentanes Endometriosis M Phase Cell Cycle Checkpoints Ovarian Cysts Ovary Quinolines Receptors, G-Protein-Coupled Stromal Cells Adult Apoptosis Caspase 3 Caspase 3 Cell Proliferation Cells, Cultured Cyclopentanes Dose-Response Relationship, Drug Endometriosis Endometriosis

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