Activation of G-protein coupled estrogen receptor inhibits the proliferation of cervical cancer cells via sustained activation of ERK1/2

Cell Biochemistry and Function
Qiong ZhangQun Hao

Abstract

Cervical cancer is one of the most common gynaecological women cancer and suggested to be modulated by estrogenic signals. G protein-coupled receptor (GPER), a seven-transmembrane G protein-coupled receptor, has been reported to regulate the cell proliferation of various cancers. But there is no study investigating the effects of GPER on the progression of cervical cancer. In the present study, we revealed for the first time that GPER was also highly expressed in various human cervical cancer cells. Activation of GPER via its specific agonist G-1 induced G2/M cell cycle arrest and down regulation of cyclin B via a time dependent manner. Furthermore, G-1 treatment induced sustained activation of extracellular-signal-regulated kinases (ERK)1/2 via epidermal growth factor receptor (EGFR) signals. Both inhibitors of ERK1/2 and EGFR significantly abolished G-1-induced suppression of cell proliferation and down regulation of cyclin B. Generally, our study revealed that GPER is highly expressed in human cervical cancer cells and its activation inhibits cell proliferation via EGFR/ERK1/2 signals. It suggested that G-1 can be considered as a potential new pharmacological tool to reduce the growth of cervical cancer.

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Citations

Jan 14, 2016·Human Reproduction Update·Ignacio ZapardielJuan A Garcia-Velasco
Apr 14, 2016·Toxicological Sciences : an Official Journal of the Society of Toxicology·Mary O HuffCarolyn M Klinge
Oct 25, 2016·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·M WesołowskaP P Jagodziński
Sep 20, 2017·Journal of Cancer Research and Clinical Oncology·Klaus FrieseSabine Heublein
Jan 16, 2019·International Journal of Molecular Sciences·Sabine HeubleinAurelia Vattai
Feb 8, 2019·Anti-cancer Agents in Medicinal Chemistry·Christian D. Hernandez-SilvaAna L Pereira-Suárez
Nov 12, 2019·Frontiers in Endocrinology·Shen XuLeo Tsz On Lee
Jul 30, 2020·Journal of Cancer Research and Clinical Oncology·Daniel BeilnerHelene Hildegard Heidegger
Sep 26, 2020·Frontiers in Endocrinology·Christian David Hernández-SilvaAna Laura Pereira-Suárez
Mar 13, 2017·The Journal of Steroid Biochemistry and Molecular Biology·Eric R Prossnitz
Mar 27, 2021·Frontiers in Oncology·Yu-An QiuTenghua Yu

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