The putative G-protein coupled estrogen receptor agonist G-1 suppresses proliferation of ovarian and breast cancer cells in a GPER-independent manner

Cheng Wang, Xiangmin Lv, Chao Jiang, John S Davis

Research output: Chapter in Book/Report/Conference proceedingChapter

39 Citations (Scopus)

Abstract

G-protein coupled estrogen receptor 1 (GPER) plays an important role in mediating estrogen action in many different tissues under both physiological and pathological conditions. G-1 (1-[4-(6-bromobenzo[1,3]dioxol-5yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta [c]quinolin-8-yl]-ethanone) has been developed as a selective GPER agonist to distinguish estrogen actions mediated by GPER from those mediated by classic estrogen receptors. In the present study, we surprisingly found that G-1 suppressed proliferation and induced apoptosis of KGN cells (a human ovarian granulosa cell tumor cell line), actions that were not blocked by a selective GPER antagonist G15 or siRNA knock-down of GPER. G-1 also suppressed proliferation and induced cell apoptosis in GPER-negative HEK-293 cells and MDA-MB 231 breast cancer cells. Our results demonstrate that G-1 suppresses proliferation of ovarian and breast cancer cells in a GPER-independent manner. G-1 may be a candidate for the development of drugs against ovarian and breast cancer.

Original languageEnglish (US)
Title of host publicationAmerican Journal of Translational Research
Pages390-402
Number of pages13
Volume4
Edition4
StatePublished - 2012

Fingerprint

Estrogen Receptor alpha
G-Protein-Coupled Receptors
GTP-Binding Proteins
Ovarian Neoplasms
Estrogens
Cells
Breast Neoplasms
Apoptosis
Granulosa Cell Tumor
HEK293 Cells
Tumor Cell Line
Estrogen Receptors
Small Interfering RNA
Tumors
Cell Proliferation
Tissue
Pharmaceutical Preparations

Keywords

  • Breast cancer
  • Estrogen receptors
  • G-1
  • G15
  • GPR30/GPER
  • Ovarian cancer

ASJC Scopus subject areas

  • Medicine(all)
  • Cancer Research
  • Clinical Biochemistry
  • Molecular Medicine

Cite this

Wang, C., Lv, X., Jiang, C., & Davis, J. S. (2012). The putative G-protein coupled estrogen receptor agonist G-1 suppresses proliferation of ovarian and breast cancer cells in a GPER-independent manner. In American Journal of Translational Research (4 ed., Vol. 4, pp. 390-402)

The putative G-protein coupled estrogen receptor agonist G-1 suppresses proliferation of ovarian and breast cancer cells in a GPER-independent manner. / Wang, Cheng; Lv, Xiangmin; Jiang, Chao; Davis, John S.

American Journal of Translational Research. Vol. 4 4. ed. 2012. p. 390-402.

Research output: Chapter in Book/Report/Conference proceedingChapter

Wang, Cheng ; Lv, Xiangmin ; Jiang, Chao ; Davis, John S. / The putative G-protein coupled estrogen receptor agonist G-1 suppresses proliferation of ovarian and breast cancer cells in a GPER-independent manner. American Journal of Translational Research. Vol. 4 4. ed. 2012. pp. 390-402
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