GPR30

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G protein-spregnuti estrogenski receptor 1
Identifikatori
Simboli GPER; GPR30; CMKRL2; DRY12; FEG-1; GPCR-Br; LERGU; LERGU2; LyGPR; MGC99678
Vanjski ID OMIM601805 MGI1924104 HomoloGene15855 IUPHAR: GPER GeneCards: GPER Gene
Pregled RNK izražavanja
PBB GE GPR30 210640 s at tn.png
PBB GE GPR30 211829 s at tn.png
podaci
Ortolozi
Vrsta Čovek Miš
Entrez 2852 76854
Ensembl ENSG00000164850 ENSMUSG00000053647
UniProt Q99527 Q8BMP4
RefSeq (mRNA) NM_001039966 NM_029771
RefSeq (protein) NP_001035055 NP_084047
Lokacija (UCSC) Chr 7:
1.09 - 1.1 Mb
Chr 5:
139.68 - 139.68 Mb
PubMed pretraga [1] [2]

G-protein spregnuti estrogenski receptor 1 (GPER), takođe poznat kao membranski estrogenski receptor (mER) ili G-protein spregnuti receptor 30 (GPR30), je G protein-spregnuti receptor koji je kod čoveka kodiran GPER genom.[1] GPR30 je integralni membranski protein sa visokim afinitetom za estrogen.[2][3][4][5]

Funkcija[uredi - уреди | uredi izvor]

Ovaj protein je član familije rodopsinu-sličnih G protein-spregnutih receptora. GPR30 vezuje estrogen, što dovodi do mobilizacije intracelularnog kalcijuma i sinteze fosfatidilinozitol (3,4,5)-trisfosfata u nukleusu. Ovaj protein učestvuje u brzim negenomskim signalnim eventima. Alternativne transkripcione splajsne varijante koje kodiraju isti protein su bile karakterisane.[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]

Klinički značaj[uredi - уреди | uredi izvor]

GPR30 ima važnu ulogu u razvoju tamoksifen otpornosti kod ćelija raka dojke.[8]

Literatura[uredi - уреди | uredi izvor]

  1. O'Dowd BF, Nguyen T, Marchese A, Cheng R, Lynch KR, Heng HH, Kolakowski LF, George SR (January 1998). "Discovery of three novel G-protein-coupled receptor genes". Genomics 47 (2): 310–3. PMID 9479505. doi:10.1006/geno.1998.5095. 
  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. PMID 15705806. doi:10.1126/science.1106943. 
  3. Filardo EJ, Thomas P (2005). "GPR30: a seven-transmembrane-spanning estrogen receptor that triggers EGF release". Trends Endocrinol. Metab. 16 (8): 362–7. PMID 16125968. doi:10.1016/j.tem.2005.08.005. 
  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. PMID 16270355. doi:10.1002/jcp.20551. 
  5. Prossnitz ER, Arterburn JB, Sklar LA (2007). "GPR30: A G protein-coupled receptor for estrogen". Mol. Cell. Endocrinol. 265-266: 138–42. PMC 1847610. PMID 17222505. doi:10.1016/j.mce.2006.12.010. 
  6. "Entrez Gene: GPR30 G protein-coupled receptor 30". http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=2852. 
  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. 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. PMID 19911269. doi:10.1007/s10549-009-0624-6. 

Dodatna literatura[uredi - уреди | uredi izvor]

  • 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. PMID 11897506. doi:10.1016/S0960-0760(01)00190-X. 
  • Filardo EJ, Thomas P (2005). "GPR30: a seven-transmembrane-spanning estrogen receptor that triggers EGF release.". Trends Endocrinol. Metab. 16 (8): 362–7. PMID 16125968. doi:10.1016/j.tem.2005.08.005. 
  • Bonaldo MF, Lennon G, Soares MB (1997). "Normalization and subtraction: two approaches to facilitate gene discovery.". Genome Res. 6 (9): 791–806. PMID 8889548. doi:10.1101/gr.6.9.791. 
  • 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. PMID 8920907. doi:10.1006/bbrc.1996.1654. 
  • 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. PMID 9070864. doi:10.1006/bbrc.1997.6161. 
  • 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. PMID 9141481. doi:10.1016/S0014-5793(97)00278-0. 
  • 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. PMID 9367686. doi:10.1006/geno.1997.4972. 
  • 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. PMID 9398636. doi:10.1006/bbrc.1997.7734. 
  • 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. PMID 11043579. doi:10.1210/me.14.10.1649. 
  • 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. PMID 11773440. doi:10.1210/me.16.1.70. 
  • 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. PMID 12027886. doi:10.1046/j.1432-1033.2002.02912.x. 
  • 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. PMID 12193550. doi:10.1210/en.2001-211445. 
  • 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. PMID 12446589. doi:10.1210/en.2002-220492. 
  • 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. PMC 139241. PMID 12477932. doi:10.1073/pnas.242603899. 
  • Scherer SW, Cheung J, MacDonald JR et al. (2003). "Human chromosome 7: DNA sequence and biology.". Science 300 (5620): 767–72. PMC 2882961. PMID 12690205. doi:10.1126/science.1083423. 
  • 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. PMID 14632195. doi:10.1046/j.1523-1747.2003.12487.x. 
  • 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. PMID 14675202. doi:10.1111/j.1523-1747.2003.12617.x. 

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