GPR30

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G protein-coupled estrogen receptor 1
Identifiers
SymbolsGPER; GPR30; CMKRL2; DRY12; FEG-1; GPCR-Br; LERGU; LERGU2; LyGPR; MGC99678
External IDsOMIM601805 MGI1924104 HomoloGene15855 IUPHAR: GPER GeneCards: GPER Gene
RNA expression pattern
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250px
More reference expression data
Orthologs
SpeciesHumanMouse
Entrez285276854
EnsemblENSG00000164850ENSMUSG00000053647
UniProtQ99527Q8BMP4
RefSeq (mRNA)NM_001039966NM_029771
RefSeq (protein)NP_001035055NP_084047
Location (UCSC)Chr 7:
1.09 - 1.1 Mb
Chr 5:
139.68 - 139.68 Mb
PubMed search[1][2]

G-protein coupled estrogen receptor 1 (GPER) also known as the membrane estrogen receptor (mER) or G-protein coupled receptor 30 (GPR30) is a G protein-coupled receptor that in humans is encoded by the GPER gene.[1] GPR30 is an integral membrane protein with high affinity for estrogen.[2][3][4][5]

Function

This protein is a member of the rhodopsin-like family of G protein-coupled receptors and is a multi-pass membrane protein that localizes to the endoplasmic reticulum. The protein binds estrogen, resulting in intracellular calcium mobilization and synthesis of phosphatidylinositol (3,4,5)-trisphosphate in the nucleus. This protein therefore plays a role in the rapid nongenomic signaling events widely observed following stimulation of cells and tissues with estrogen. Alternate transcriptional splice variants which encode the same protein have been characterized.[6] The distribution of GPR30 is well established in the rodent, with high expression observed in the hypothalamus, pituitary gland, adrenal medulla, kidney medulla and developing follicles of the ovary.[7]

Clinical significance

Female GPR30 knockout mice display hyperglycemia and impaired glucose tolerance, reduced body growth, and increased blood pressure.[8]

GPR30 plays an improtant role in development of tamoxifen resistance in breast cancer cells.[9]

References

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Further reading

  • Filardo EJ (2002). "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". J. Steroid Biochem. Mol. Biol. 80 (2): 231–8. doi:10.1016/S0960-0760(01)00190-X. PMID 11897506. 
  • Filardo EJ, Thomas P (2005). "GPR30: a seven-transmembrane-spanning estrogen receptor that triggers EGF release". Trends Endocrinol. Metab. 16 (8): 362–7. doi:10.1016/j.tem.2005.08.005. PMID 16125968. 
  • Bonaldo MF, Lennon G, Soares MB (1997). "Normalization and subtraction: two approaches to facilitate gene discovery". Genome Res. 6 (9): 791–806. doi:10.1101/gr.6.9.791. PMID 8889548. 
  • Owman C, Blay P, Nilsson C, Lolait SJ (1996). "Cloning of human cDNA encoding a novel heptahelix receptor expressed in Burkitt's lymphoma and widely distributed in brain and peripheral tissues". Biochem. Biophys. Res. Commun. 228 (2): 285–92. doi:10.1006/bbrc.1996.1654. PMID 8920907. 
  • Feng Y, Gregor P (1997). "Cloning of a novel member of the G protein-coupled receptor family related to peptide receptors". Biochem. Biophys. Res. Commun. 231 (3): 651–4. doi:10.1006/bbrc.1997.6161. PMID 9070864. 
  • Kvingedal AM, Smeland EB (1997). "A novel putative G-protein-coupled receptor expressed in lung, heart and lymphoid tissue". FEBS Lett. 407 (1): 59–62. doi:10.1016/S0014-5793(97)00278-0. PMID 9141481. 
  • Carmeci C, Thompson DA, Ring HZ; et al. (1998). "Identification of a gene (GPR30) with homology to the G-protein-coupled receptor superfamily associated with estrogen receptor expression in breast cancer". Genomics. 45 (3): 607–17. doi:10.1006/geno.1997.4972. PMID 9367686. 
  • Takada Y, Kato C, Kondo S; et al. (1998). "Cloning of cDNAs encoding G protein-coupled receptor expressed in human endothelial cells exposed to fluid shear stress". Biochem. Biophys. Res. Commun. 240 (3): 737–41. doi:10.1006/bbrc.1997.7734. PMID 9398636. 
  • Filardo EJ, Quinn JA, Bland KI, Frackelton AR (2001). "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". Mol. Endocrinol. 14 (10): 1649–60. doi:10.1210/me.14.10.1649. PMID 11043579. 
  • Filardo EJ, Quinn JA, Frackelton AR, Bland KI (2002). "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". Mol. Endocrinol. 16 (1): 70–84. doi:10.1210/me.16.1.70. PMID 11773440. 
  • Ahola TM, Purmonen S, Pennanen P; et al. (2002). "Progestin upregulates G-protein-coupled receptor 30 in breast cancer cells". Eur. J. Biochem. 269 (10): 2485–90. doi:10.1046/j.1432-1033.2002.02912.x. PMID 12027886. 
  • Ahola TM, Manninen T, Alkio N, Ylikomi T (2002). "G protein-coupled receptor 30 is critical for a progestin-induced growth inhibition in MCF-7 breast cancer cells". Endocrinology. 143 (9): 3376–84. doi:10.1210/en.2001-211445. PMID 12193550. 
  • Ahola TM, Alkio N, Manninen T, Ylikomi T (2002). "Progestin and G protein-coupled receptor 30 inhibit mitogen-activated protein kinase activity in MCF-7 breast cancer cells". Endocrinology. 143 (12): 4620–6. doi:10.1210/en.2002-220492. PMID 12446589. 
  • Strausberg RL, Feingold EA, Grouse LH; et al. (2003). "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences". Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–903. doi:10.1073/pnas.242603899. PMC 139241Freely accessible. PMID 12477932. 
  • Scherer SW, Cheung J, MacDonald JR; et al. (2003). "Human chromosome 7: DNA sequence and biology". Science. 300 (5620): 767–72. doi:10.1126/science.1083423. PMC 2882961Freely accessible. PMID 12690205. 
  • Hamza A, Sarma MH, Sarma RH (2004). "Plausible interaction of an alpha-fetoprotein cyclopeptide with the G-protein-coupled receptor model GPR30: docking study by molecular dynamics simulated annealing". J. Biomol. Struct. Dyn. 20 (6): 751–8. PMID 12744705. 
  • Kanda N, Watanabe S (2003). "17Beta-estradiol enhances the production of nerve growth factor in THP-1-derived macrophages or peripheral blood monocyte-derived macrophages". J. Invest. Dermatol. 121 (4): 771–80. doi:10.1046/j.1523-1747.2003.12487.x. PMID 14632195. 
  • Kanda N, Watanabe S (2004). "17beta-estradiol inhibits oxidative stress-induced apoptosis in keratinocytes by promoting Bcl-2 expression". J. Invest. Dermatol. 121 (6): 1500–9. doi:10.1111/j.1523-1747.2003.12617.x. PMID 14675202. 

External links


This article incorporates text from the United States National Library of Medicine, which is in the public domain.

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  2. Revankar CM, Cimino DF, Sklar LA, Arterburn JB, Prossnitz ER (2005). "A transmembrane intracellular estrogen receptor mediates rapid cell signaling". Science. 307 (5715): 1625–30. doi:10.1126/science.1106943. PMID 15705806. 
  3. Filardo EJ, Thomas P (2005). "GPR30: a seven-transmembrane-spanning estrogen receptor that triggers EGF release". Trends Endocrinol. Metab. 16 (8): 362–7. doi:10.1016/j.tem.2005.08.005. PMID 16125968. 
  4. Manavathi B, Kumar R (2006). "Steering estrogen signals from the plasma membrane to the nucleus: two sides of the coin". J. Cell. Physiol. 207 (3): 594–604. doi:10.1002/jcp.20551. PMID 16270355. 
  5. Prossnitz ER, Arterburn JB, Sklar LA (2007). "GPR30: A G protein-coupled receptor for estrogen". Mol. Cell. Endocrinol. 265-266: 138–42. doi:10.1016/j.mce.2006.12.010. PMC 1847610Freely accessible. PMID 17222505. 
  6. "Entrez Gene: GPR30 G protein-coupled receptor 30". 
  7. GGJ Hazell, ST Yao, JA Roper, ER Prossnitz, AM O'Carroll, and SJ Lolait "Localisation of GPR30, a novel G protein-coupled oestrogen receptor, suggests multiple functions in rodent brain and peripheral tissues" J Endocrinol. 2009 August; 202(2): 223–236.
  8. Mårtensson UE, Salehi SA, Windahl S, Gomez MF, Swärd K, Daszkiewicz-Nilsson J, Wendt A, Andersson N, Hellstrand P, Grände PO, Owman C, Rosen CJ, Adamo ML, Lundquist I, Rorsman P, Nilsson BO, Ohlsson C, Olde B, Leeb-Lundberg LM (2008). "Deletion of the G protein-coupled Receptor GPR30 Impairs Glucose Tolerance, Reduces Bone Growth, Increases Blood Pressure, and Eliminates Estradiol-stimulated Insulin Release in Female Mice". Endocrinology. 150 (2): 687. doi:10.1210/en.2008-0623. PMID 18845638. 
  9. Ignatov A, Ignatov T, Roessner A, Costa SD, Kalinski T (2010). "Role of GPR30 in the mechanisms of tamoxifen resistance in breast cancer MCF-7 cells". Breast Cancer Research and Treatment. 123 (1): 87–96. doi:10.1007/s10549-009-0624-6. PMID 19911269.