GPR30

G protein-spregnuti estrogenski receptor 1
Identifikatori
Simboli	GPER; GPR30; CMKRL2; DRY12; FEG-1; GPCR-Br; LERGU; LERGU2; LyGPR; MGC99678
Vanjski ID	OMIM: 601805 MGI: 1924104 HomoloGene: 15855 IUPHAR: GPER GeneCards: GPER Gene
Ontologija gena
Molekularna funkcija	• rodopsinu-slična receptorska aktivnost; • receptorska aktivnost; • aktivnost purinskog nukleotidnog receptora, G-protein spregnutog;
Celularna komponenta	• integralno sa ćelijskom membranom; • membrana; • integralno sa membranom;
Biološki proces	• prenos signala; • signalni put G-protein spregnutog receptora;
Pregled RNK izražavanja
	podaci
Ortolozi

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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

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

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

Literatura

↑ 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.
↑ 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.
↑ 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.
↑ 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.
↑ 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.
↑ „Entrez Gene: GPR30 G protein-coupled receptor 30”.
↑ 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.
↑ 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

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. 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. 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.

Spoljašnje veze

„Estrogen (G protein coupled) Receptor”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Arhivirano iz originala na datum 2016-03-03.
MeSH GPER+protein

[pmid9479505-1] 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.

[pmid15705806-2] 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.

[pmid16125968-3] 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.

[pmid16270355-4] 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.

[pmid17222505-5] 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.

[entrez-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.

[pmid119911269-8] 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.

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