G protein-coupled estrogen receptor 1 agonist G-1 induces cell cycle arrest in the mitotic phase, leading to apoptosis in endometriosis
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⤵ 16 in-corpus citations
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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
OBJECTIVE: To demonstrate the effects of the selective G protein-coupled estrogen receptor 1 (GPER) agonist G-1 in human ovarian endometriotic stromal cells (ESCs).
DESIGN: Experimental in vitro study.
SETTING: University 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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Cited by (17)
- A multicenter randomized placebo-controlled trial evaluating daidzein-rich isoflavone aglycones in endometriosis-associated dysmenorrhea 2026
- Regulated cell death in endometrial diseases: from molecular mechanisms to targeted therapies 2025
- The "Road" to Malignant Transformation from Endometriosis to Endometriosis-Associated Ovarian Cancers (EAOCs): An mTOR-Centred Review 2024
- Luoshi Neiyi Prescription inhibits estradiol synthesis and inflammation in endometriosis through the HIF1A/EZH2/SF-1 pathway 2024
- Evaluation of survivin expression in the endometrium and endometriotic lesions in patients with genital endometriosis, type 1 diabetes mellitus and their comorbidity 2023
- Machine learning-based integrated identification of predictive combined diagnostic biomarkers for endometriosis 2023
- Extracellular vesicle-derived long non-coding RNA as circulating biomarkers for endometriosis 2021
- Role of estrogen and estrogen-related factors in endometriosis 2021
- Androgens, oestrogens and endometrium: a fine balance between perfection and pathology 2020
- Spatial and temporal changes in the expression of steroid hormone receptors in mouse model of endometriosis 2020
- AC002454.1 and CDK6 synergistically promote endometrial cell migration and invasion in endometriosis 2019
- Local estrogen formation and its regulation in endometriosis 2019
- Daidzein-rich isoflavone aglycones inhibit cell growth and inflammation in endometriosis 2018
- Expression Pattern of G-Protein-Coupled Estrogen Receptor in Myometrium of Uteri with and without Adenomyosis 2017
- Are we facing a potential effective treatment for endometriosis? 2015
- Genome-Wide Microarray Analysis of Long Non-Coding RNAs in Eutopic Secretory Endometrium with Endometriosis 2015
- MAP kinases and the inflammatory signaling cascade as targets for the treatment of endometriosis? 2015
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