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Gene Review

GPER1  -  G protein-coupled estrogen receptor 1

Homo sapiens

Synonyms: CEPR, CMKRL2, Chemoattractant receptor-like 2, DRY12, FEG-1, ...
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Disease relevance of GPR30


High impact information on GPR30

  • We found that suppression of GPR30 but not ER-alpha prevented E2-BSA- or E2-induced PKA activation and Bcl-2 expression [6].
  • At 2 hours after trauma-hemorrhage, administration of E2-conjugated to bovine serum albumin (E2-BSA, membrane impermeable) or E2 induced the up-regulation of ER-alpha and GPR30 and attenuated hepatic injury [6].
  • Isolated hepatocytes were transfected with small interfering RNA to suppress GPR30 or ER [6].
  • GPR30 also acts independently of the ER to promote activation of the protein kinase A (PKA) pathway, which protects cells from apoptosis through Bcl-2 [6].
  • G protein-coupled receptor 30-dependent protein kinase a pathway is critical in nongenomic effects of estrogen in attenuating liver injury after trauma-hemorrhage [6].

Chemical compound and disease context of GPR30


Biological context of GPR30


Anatomical context of GPR30


Associations of GPR30 with chemical compounds

  • Thus, our data delineate a novel mechanism, requiring GPR30 and estrogen, that acts to regulate Erk-1/-2 activity via an inhibitory signal mediated by cAMP [8].
  • In addition, GPR30-dependent Erk-1/-2 activation was triggered by ER antagonists, including ICI 182,780, yet not by 17alpha-estradiol or progesterone [1].
  • These data suggest that the orphan receptor, GPR30, is important for the inhibitory effect of progestin on growth [10].
  • Progesterone-induced increases and small interfering RNA-induced decreases in GPR30 expression in SKBR3 cells were accompanied by parallel changes in specific estradiol-17beta (E2) binding [12].
  • Interestingly, the decrease of ERK activity induced by MPA was abrogated by GPR30 antisense [11].

Regulatory relationships of GPR30


Other interactions of GPR30


Analytical, diagnostic and therapeutic context of GPR30


  1. Estrogen-induced activation of Erk-1 and Erk-2 requires the G protein-coupled receptor homolog, GPR30, and occurs via trans-activation of the epidermal growth factor receptor through release of HB-EGF. Filardo, E.J., Quinn, J.A., Bland, K.I., Frackelton, A.R. Mol. Endocrinol. (2000) [Pubmed]
  2. G protein-coupled receptor 30 down-regulates cofactor expression and interferes with the transcriptional activity of glucocorticoid. Ylikomi, T., Vienonen, A., Ahola, T.M. Eur. J. Biochem. (2004) [Pubmed]
  3. Cloning of novel LERGU mRNAs in GPR30 3' untranslated region and detection of 2 bp-deletion polymorphism in gastric cancer. Kakinuma, N., Sato, M., Yamada, T., Kohu, K., Nakajima, M., Akiyama, T., Ohwada, S., Shibanaka, Y. Cancer Sci. (2005) [Pubmed]
  4. The G protein-coupled receptor GPR30 mediates the proliferative effects induced by 17beta-estradiol and hydroxytamoxifen in endometrial cancer cells. Vivacqua, A., Bonofiglio, D., Recchia, A.G., Musti, A.M., Picard, D., Andò, S., Maggiolini, M. Mol. Endocrinol. (2006) [Pubmed]
  5. Distribution of GPR30, a Seven Membrane-Spanning Estrogen Receptor, in Primary Breast Cancer and its Association with Clinicopathologic Determinants of Tumor Progression. Filardo, E.J., Graeber, C.T., Quinn, J.A., Resnick, M.B., Giri, D., Delellis, R.A., Steinhoff, M.M., Sabo, E. Clin. Cancer Res. (2006) [Pubmed]
  6. G protein-coupled receptor 30-dependent protein kinase a pathway is critical in nongenomic effects of estrogen in attenuating liver injury after trauma-hemorrhage. Hsieh, Y.C., Yu, H.P., Frink, M., Suzuki, T., Choudhry, M.A., Schwacha, M.G., Chaudry, I.H. Am. J. Pathol. (2007) [Pubmed]
  7. Progestin upregulates G-protein-coupled receptor 30 in breast cancer cells. Ahola, T.M., Purmonen, S., Pennanen, P., Zhuang, Y.H., Tuohimaa, P., Ylikomi, T. Eur. J. Biochem. (2002) [Pubmed]
  8. Estrogen action via the G protein-coupled receptor, GPR30: stimulation of adenylyl cyclase and cAMP-mediated attenuation of the epidermal growth factor receptor-to-MAPK signaling axis. Filardo, E.J., Quinn, J.A., Frackelton, A.R., Bland, K.I. Mol. Endocrinol. (2002) [Pubmed]
  9. Epidermal growth factor receptor (EGFR) transactivation by estrogen via the G-protein-coupled receptor, GPR30: a novel signaling pathway with potential significance for breast cancer. Filardo, E.J. J. Steroid Biochem. Mol. Biol. (2002) [Pubmed]
  10. G protein-coupled receptor 30 is critical for a progestin-induced growth inhibition in MCF-7 breast cancer cells. Ahola, T.M., Manninen, T., Alkio, N., Ylikomi, T. Endocrinology (2002) [Pubmed]
  11. Progestin and G protein-coupled receptor 30 inhibit mitogen-activated protein kinase activity in MCF-7 breast cancer cells. Ahola, T.M., Alkio, N., Manninen, T., Ylikomi, T. Endocrinology (2002) [Pubmed]
  12. Identity of an estrogen membrane receptor coupled to a G protein in human breast cancer cells. Thomas, P., Pang, Y., Filardo, E.J., Dong, J. Endocrinology (2005) [Pubmed]
  13. 17Beta-estradiol enhances the production of nerve growth factor in THP-1-derived macrophages or peripheral blood monocyte-derived macrophages. Kanda, N., Watanabe, S. J. Invest. Dermatol. (2003) [Pubmed]
  14. Identification of a gene (GPR30) with homology to the G-protein-coupled receptor superfamily associated with estrogen receptor expression in breast cancer. Carmeci, C., Thompson, D.A., Ring, H.Z., Francke, U., Weigel, R.J. Genomics (1997) [Pubmed]
  15. A transmembrane intracellular estrogen receptor mediates rapid cell signaling. Revankar, C.M., Cimino, D.F., Sklar, L.A., Arterburn, J.B., Prossnitz, E.R. Science (2005) [Pubmed]
  16. G protein-coupled receptor 30 is an estrogen receptor in the plasma membrane. Funakoshi, T., Yanai, A., Shinoda, K., Kawano, M.M., Mizukami, Y. Biochem. Biophys. Res. Commun. (2006) [Pubmed]
  17. Discovery of three novel G-protein-coupled receptor genes. O'Dowd, B.F., Nguyen, T., Marchese, A., Cheng, R., Lynch, K.R., Heng, H.H., Kolakowski, L.F., George, S.R. Genomics (1998) [Pubmed]
  18. The G protein-coupled receptor GPR30 inhibits human urothelial cell proliferation. Teng, J., Wang, Z.Y., Prossnitz, E.R., Bjorling, D.E. Endocrinology (2008) [Pubmed]
  19. An external audit of laparoscopic cholecystectomy performed in medical treatment facilities of the department of Defense. Wherry, D.C., Rob, C.G., Marohn, M.R., Rich, N.M. Ann. Surg. (1994) [Pubmed]
  20. Isolation rates and pathogenicity of enterococci in obstetric and gynecological operations. Kubota, T., Iwasa, T., Saito, H., Kaneko, T., Takada, M., Oguri, T. Kansenshogaku Zasshi (1992) [Pubmed]
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