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Gene and Protein Information  |
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| class A G protein-coupled receptor | ||||||
| Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
| Human | 7 | 375 | 7p22.3 | GPER1 | G protein-coupled estrogen receptor 1 | 10-11 |
| Mouse | 7 | 375 | 5 G2 | Gper1 | G protein-coupled estrogen receptor 1 | |
| Rat | 7 | 375 | 12q11 | Gper1 | G protein-coupled estrogen receptor 1 | 2 |
| Previous and Unofficial Names |
| CEPR | CMKRL2 | DRY12 | FEG-1 | Gpr41 | LERGU | LERGU2 | chemokine receptor-like 2 | Flow-induced endothelial G-protein coupled receptor 1 | GPGR | LYGPR | Lymphocyte-derived G-protein coupled receptor | Membrane estrogen receptor | mER | GPCR-BR | GPR30 | IL8-related receptor DRY12 |
| Database Links |
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| Specialist databases | |
| GPCRdb | gper1_human (Hs), gper1_mouse (Mm), gper1_rat (Rn) |
| Other databases | |
| Alphafold | Q99527 (Hs), Q8BMP4 (Mm), O08878 (Rn) |
| ChEMBL Target | CHEMBL5872 (Hs), CHEMBL3309103 (Rn) |
| Ensembl Gene | ENSG00000164850 (Hs), ENSMUSG00000053647 (Mm), ENSRNOG00000001287 (Rn) |
| Entrez Gene | 2852 (Hs), 76854 (Mm), 171104 (Rn) |
| Human Protein Atlas | ENSG00000164850 (Hs) |
| KEGG Gene | hsa:2852 (Hs), mmu:76854 (Mm), rno:171104 (Rn) |
| OMIM | 601805 (Hs) |
| Pharos | Q99527 (Hs) |
| RefSeq Nucleotide | NM_001505 (Hs), NM_029771 (Mm), NM_133573 (Rn) |
| RefSeq Protein | NP_001496 (Hs), NP_084047 (Mm), NP_598257 (Rn) |
| UniProtKB | Q99527 (Hs), Q8BMP4 (Mm), O08878 (Rn) |
| Wikipedia | GPER1 (Hs) |
| Natural/Endogenous Ligands |
| 17β-estradiol |
| Comments: Southern et al. (2013) were unable to detect 17β-estradiol-GPER engagement using the PathHunter™ β-Arrestin recruitment assay [14]. |
Download all structure-activity data for this target as a CSV file 
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| Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Antagonists | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Immuno Process Associations | ||
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| Primary Transduction Mechanisms
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| Transducer | Effector/Response |
| Gi/Go family | Phospholipase C stimulation |
| References: 6,9,13 | |
| Secondary Transduction Mechanisms |
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| Transducer | Effector/Response |
| Gs family | Adenylyl cyclase stimulation |
| References: 7,15 | |
| Tissue Distribution
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| Expression Datasets |
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| Functional Assays
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| Phenotypes, Alleles and Disease Models
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Mouse data from MGI | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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1. Bologa CG, Revankar CM, Young SM, Edwards BS, Arterburn JB, Kiselyov AS, Parker MA, Tkachenko SE, Savchuck NP, Sklar LA et al.. (2006) Virtual and biomolecular screening converge on a selective agonist for GPR30. Nat Chem Biol, 2 (4): 207-12. [PMID:16520733]
2. Bonini JA, Anderson SM, Steiner DF. (1997) Molecular cloning and tissue expression of a novel orphan G protein-coupled receptor from rat lung. Biochem Biophys Res Commun, 234 (1): 190-3. [PMID:9168987]
3. Carmeci C, Thompson DA, Ring HZ, Francke U, Weigel RJ. (1997) 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]
4. Dennis MK, Burai R, Ramesh C, Petrie WK, Alcon SN, Nayak TK, Bologa CG, Leitao A, Brailoiu E, Deliu E et al.. (2009) In vivo effects of a GPR30 antagonist. Nat Chem Biol, 5 (6): 421-7. [PMID:19430488]
5. Dennis MK, Field AS, Burai R, Ramesh C, Petrie WK, Bologa CG, Oprea TI, Yamaguchi Y, Hayashi S, Sklar LA et al.. (2011) Identification of a GPER/GPR30 antagonist with improved estrogen receptor counterselectivity. J Steroid Biochem Mol Biol, 127 (3-5): 358-66. [PMID:21782022]
6. Filardo EJ, Quinn JA, Bland KI, Frackelton Jr AR. (2000) 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]
7. Filardo EJ, Quinn JA, Frackelton Jr 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]
8. Koganti S, Snyder R, Gumaste U, Karamyan VT, Thekkumkara T. (2014) 2-methoxyestradiol binding of GPR30 down-regulates angiotensin AT(1) receptor. Eur J Pharmacol, 723: 131-40. [PMID:24262995]
9. Maggiolini M, Vivacqua A, Fasanella G, Recchia AG, Sisci D, Pezzi V, Montanaro D, Musti AM, Picard D, Andò S. (2004) The G protein-coupled receptor GPR30 mediates c-fos up-regulation by 17beta-estradiol and phytoestrogens in breast cancer cells. J Biol Chem, 279 (26): 27008-16. [PMID:15090535]
10. O'Dowd BF, Nguyen T, Marchese A, Cheng R, Lynch KR, Heng HH, Kolakowski Jr LF, George SR. (1998) Discovery of three novel G-protein-coupled receptor genes. Genomics, 47 (2): 310-3. [PMID:9479505]
11. 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]
12. Petrie WK, Dennis MK, Hu C, Dai D, Arterburn JB, Smith HO, Hathaway HJ, Prossnitz ER. (2013) G protein-coupled estrogen receptor-selective ligands modulate endometrial tumor growth. Obstet Gynecol Int, 2013: 472720. [PMID:24379833]
13. 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]
14. Southern C, Cook JM, Neetoo-Isseljee Z, Taylor DL, Kettleborough CA, Merritt A, Bassoni DL, Raab WJ, Quinn E, Wehrman TS et al.. (2013) Screening β-Arrestin Recruitment for the Identification of Natural Ligands for Orphan G-Protein-Coupled Receptors. J Biomol Screen, 18 (5): 599-609. [PMID:23396314]
15. Thomas P, Pang Y, Filardo EJ, Dong J. (2005) Identity of an estrogen membrane receptor coupled to a G protein in human breast cancer cells. Endocrinology, 146 (2): 624-32. [PMID:15539556]
