GPR30

G protein-spregnuti estrogenski receptor 1
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
Vrsta	Čovek
Entrez	2852
Ensembl	ENSG00000164850
UniProt	Q99527
RefSeq (mRNA)	NM_001039966
RefSeq (protein)	NP_001035055
Lokacija (UCSC)	Chr 7:; 1.09 - 1.1 Mb
PubMed pretraga	[1]

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 (1998). „Discovery of three novel G-protein-coupled receptor genes”. Genomics. 47 (2): 310—3. PMID 9479505. doi:10.1006/geno.1998.5095.
^ 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.
^ 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.
^ 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.
^ 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.
^ „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. PMID 19911269. doi:10.1007/s10549-009-0624-6.

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. 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.

Spoljašnje veze

„Estrogen (G protein coupled) Receptor”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Архивирано из оригинала 03. 03. 2016. г.
GPER+protein на US National Library of Medicine Medical Subject Headings (MeSH)

[pmid9479505-1] O'Dowd BF, Nguyen T, Marchese A, Cheng R, Lynch KR, Heng HH, Kolakowski LF, George SR (1998). „Discovery of three novel G-protein-coupled receptor genes”. Genomics. 47 (2): 310—3. PMID 9479505. doi:10.1006/geno.1998.5095.

[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. PMID 15705806. doi:10.1126/science.1106943.

[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. PMID 16125968. doi:10.1016/j.tem.2005.08.005.

[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. PMID 16270355. doi:10.1002/jcp.20551.

[pmid17222505-5] 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.

[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. PMID 19911269. doi:10.1007/s10549-009-0624-6.

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