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 IDsOMIM: 601805 MGI: 1924104 HomoloGene: 15855 IUPHAR: GPER GeneCards: GPER Gene
RNA expression pattern
250px
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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 139241 Freely 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 2882961 Freely 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


40x30px This transmembrane receptor-related article is a stub. You can help ssf by expanding it.

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

Class A: Rhodopsin like
α1 (A, B, D) · α2 (A, B, C) · β1 · β2 · β3
Adenosine (A1, A2A, A2B, A3) · P2Y (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)
(all but 5-HT3) 5-HT1 (A, B, D, E, F) · 5-HT2 (A, B, C) · 5-HT (4, 5A, 6, 7)
Other
Acetylcholine (M1, M2, M3, M4, M5) · Dopamine (D1, D2, D3, D4, D5) · Histamine (H1, H2, H3, H4) · Melatonin (1A, 1B, 1C) · TAAR (1, 2, 3, 5, 6, 8, 9)
Metabolites and
signaling molecules
CysLT (1, 2) · LTB4 (1, 2) · FPRL1 · OXE · Prostaglandin (DP (1, 2), EP (1, 2, 3, 4), FP) · Prostacyclin · Thromboxane
Other
Bile acid · Cannabinoid (CB1, CB2, GPR (18, 55, 119)) · EBI2 · Estrogen · Free fatty acid (1, 2, 3, 4) · Lactate  · Lysophosphatidic acid (1, 2, 3, 4, 5, 6)  · Lysophospholipid (1, 2, 3, 4, 5, 6, 7, 8) · Niacin (1, 2) · Oxoglutarate · PAF · Sphingosine-1-phosphate (1, 2, 3, 4, 5) · Succinate
Peptide
B/W (1, 2) · FF (1, 2) · S · Y (1, 2, 4, 5) · Neuromedin (B, U (1, 2)) · Neurotensin (1, 2)
Other
Miscellaneous
GPR (1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 81, 82, 83, 84, 85, 87, 88, 92, 101, 103, 109A, 109B, 119, 120, 132, 135, 137B, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 173, 174, 176, 177, 182, 183)
Other
Class B: Secretin like
GPR (56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 155, 157)
Other
Class C: Metabotropic
glutamate / pheromone
TAS1R (1, 2, 3) · TAS2R (1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 19, 20, 30, 31, 38, 39, 40, 41, 42, 43, 45, 46, 50)
Other
Class F:
Frizzled / Smoothened
Frizzled
Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10)
Smoothened
  1. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  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 1847610 Freely 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. 
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