HOMEPRODUCTSCOMPANYCONTACTFAQResearchDictionaryPharmaSign Up FREE or Login

The G protein-coupled receptor GPR30 mediates the proliferative and invasive effects induced by hydroxytamoxifen in endometrial cancer cells.

Abstract
The selective ER modulator tamoxifen (TAM(1)) is the most widely used ER antagonist for treatment of women with hormone-dependent breast tumor. However, long-term treatment is associated with an increased risk of endometrial cancer. The aim of the present study was to demonstrate new insight into the role of G-protein coupled receptor 30 (GPR30) in the activity of TAM, which promoted endometrial cancer. In endometrial cancer cell lines ISHIKAWA and KLE, the potential of 4-hydroxytamoxifen (OHT), the active metabolite of TAM, 17β-estradiol (E2) and G1, a non-steroidal GPR30-specific agonist to promote cell proliferation and invasion was evaluated. All agents above induced high proliferative and invasive effects, while the down-regulation of GPR30 or the interruption of MAPK signal pathway partly or completely prevented the action of the regent. Moreover, the RNA and protein expression of GPR30 was up-regulated by G1, E2 or OHT in both cell lines. The present study provided a new insight into the mechanism involved in the agonistic activity exerted by TAM in the uterus.
AuthorsGui-Qiang Du, Long Zhou, Xiao-Yue Chen, Xiao-Ping Wan, Yin-Yan He
JournalBiochemical and biophysical research communications (Biochem Biophys Res Commun) Vol. 420 Issue 2 Pg. 343-9 (Apr 06 2012) ISSN: 1090-2104 [Electronic] United States
PMID22425989 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2012 Elsevier Inc. All rights reserved.
Chemical References
  • GPER1 protein, human
  • Receptors, Estrogen
  • Receptors, G-Protein-Coupled
  • Selective Estrogen Receptor Modulators
  • Tamoxifen
  • afimoxifene
Topics
  • Cell Line, Tumor
  • Cell Proliferation (drug effects)
  • Endometrial Neoplasms (chemically induced, metabolism, pathology)
  • Female
  • Humans
  • Neoplasm Invasiveness
  • Receptors, Estrogen (metabolism)
  • Receptors, G-Protein-Coupled (metabolism)
  • Selective Estrogen Receptor Modulators (adverse effects)
  • Tamoxifen (adverse effects, analogs & derivatives)
  • Up-Regulation

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: