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G-protein-coupled estrogen receptor agonist G-1 inhibits the proliferation of breast cancer cells through induction of apoptosis and cycle arrest
Abstract
Purpose: To determine the effect of G-1, a G-protein-linked estrogen receptor (GPER) agonist on apoptosis, cell cycle, and proliferative potential of mammary tumor cells, and the associated mechanisms of action.
Methods: Three groups of human breast cancer cell line MDA-MB-231 were used: control group, estradiol (E2) group and G-1 group. Control group was not treated. The effects of treatment (10 M G1) on cell proliferation were determined and compared amongst the groups. Cell cycle distribution and apoptosis were determined while expression levels of proteins related to pi3k/AKT/MAPK were assessed by western blotting.
Results: Apoptosis was significantly reduced in E2 group relative to control, but was enhanced in G-1 group, when compared to the other 2 groups (p < 0.05). There were marked down-regulations in protein levels of cylinb1, p21, caspase 6, p53, p-ERK in E2 group, relative to the corresponding expression levels in the control group.
Conclusion: GPER agonist G-1 suppresses the proliferation of mammary tumor cells and induces apoptotic changes and cycle blockage in the cells via inhibition of pi3k/AKT pathway and activation of MAPKs pathway. Thus, GPER is a potential target in breast tumor treatment, and G-1 is a potential new anti-tumor drug.
