GPR30

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G protein-spregnuti estrogenski receptor 1
Identifikatori
SimboliGPER; GPR30; CMKRL2; DRY12; FEG-1; GPCR-Br; LERGU; LERGU2; LyGPR; MGC99678
Vanjski IDOMIM601805 MGI1924104 HomoloGene15855 IUPHAR: GPER GeneCards: GPER Gene
Pregled RNK izražavanja
podaci
Ortolozi
VrstaČovekMiš
Entrez285276854
EnsemblENSG00000164850ENSMUSG00000053647
UniProtQ99527Q8BMP4
RefSeq (mRNA)NM_001039966NM_029771
RefSeq (protein)NP_001035055NP_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

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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

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

Literatura

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  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. DOI:10.1006/geno.1998.5095. PMID 9479505. 
  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. 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. 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. 

Dodatna literatura

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Spoljašnje veze

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