HOMEPRODUCTSCOMPANYCONTACTFAQResearchDictionaryPharmaSign Up FREE or Login

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

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.
AuthorsQiong Zhang, Yuan-Zhe Wu, Yan-Mei Zhang, Xiao-Hong Ji, Qun Hao
JournalCell biochemistry and function (Cell Biochem Funct) Vol. 33 Issue 3 Pg. 134-42 (Apr 2015) ISSN: 1099-0844 [Electronic] England
PMID25753185 (Publication Type: Journal Article)
CopyrightCopyright © 2015 John Wiley & Sons, Ltd.
Chemical References
  • 1-(4-(6-bromobenzo(1,3)dioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta(c)quinolin-8-yl)ethanone
  • Cyclin B
  • Cyclopentanes
  • Quinolines
  • RNA, Small Interfering
  • Receptors, G-Protein-Coupled
  • ErbB Receptors
  • Mitogen-Activated Protein Kinase 1
  • Mitogen-Activated Protein Kinase 3
Topics
  • Cell Line, Tumor
  • Cell Proliferation (drug effects)
  • Cyclin B (metabolism)
  • Cyclopentanes (pharmacology)
  • ErbB Receptors (metabolism)
  • Female
  • G2 Phase Cell Cycle Checkpoints (drug effects)
  • HeLa Cells
  • Humans
  • M Phase Cell Cycle Checkpoints (drug effects)
  • MCF-7 Cells
  • Mitogen-Activated Protein Kinase 1 (metabolism)
  • Mitogen-Activated Protein Kinase 3 (metabolism)
  • Quinolines (pharmacology)
  • RNA Interference
  • RNA, Small Interfering (metabolism)
  • Receptors, G-Protein-Coupled (agonists, genetics, metabolism)
  • Signal Transduction
  • Uterine Cervical Neoplasms (metabolism, pathology)

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.
Realize the full power of the drug-disease research graph!


Choose Username:
Email:
Password:
Verify Password:
Enter Code Shown: