GPR119
From Self-sufficiency
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| G protein-coupled receptor 119 | |||||||||||||
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| Identifiers | |||||||||||||
| Symbols | GPR119; GPCR2; MGC119957; hGPCR2 | ||||||||||||
| External IDs | OMIM: 300513 MGI: 2668412 HomoloGene: 18670 IUPHAR: GPR119 GeneCards: GPR119 Gene | ||||||||||||
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| RNA expression pattern | |||||||||||||
| 250px | |||||||||||||
| More reference expression data | |||||||||||||
| Orthologs | |||||||||||||
| Species | Human | Mouse | |||||||||||
| Entrez | 139760 | 236781 | |||||||||||
| Ensembl | ENSG00000147262 | ENSMUSG00000051209 | |||||||||||
| UniProt | Q8TDV5 | Q2ABS2 | |||||||||||
| RefSeq (mRNA) | NM_178471 | NM_181751 | |||||||||||
| RefSeq (protein) | NP_848566 | NP_861416 | |||||||||||
| Location (UCSC) | Chr X: 129.35 - 129.35 Mb | Chr X: 44.92 - 44.92 Mb | |||||||||||
| PubMed search | [1] | [2] | |||||||||||
G protein-coupled receptor 119 also known as GPR119 is a G protein-coupled receptor that in humans is encoded by the GPR119 gene.[1]
GPR119, along with GPR55 and GPR18, have been implicated as novel cannabinoid receptors.[2][3][4]
Pharmacology
GPR119 is expressed predominantly in the pancreas and gastrointestinal tract in rodents and humans, as well as in the brain in rodents.[5] Activation of the receptor has been shown to cause a reduction in food intake and body weight gain in rats.[5] GPR119 has also been shown to regulate incretin and insulin hormone secretion.[6][7][8] As a result, new drugs acting on the receptor have been suggested as novel treatments for obesity and diabetes.[5][7][9]
Ligands
A number of endogenous and synthetic ligands for this receptor have been identified:[10][11][12]
- Anandamide[9]
- AR-231,453[13]
- MBX-2982[14]
- Oleoylethanolamide[2][9][5]
- PSN-375,963[5][6]
- PSN-632,408[5][6]
- Palmitoylethanolamide[15]
References
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- Takeda S, Kadowaki S, Haga T; et al. (2002). "Identification of G protein-coupled receptor genes from the human genome sequence". FEBS Lett. 520 (1-3): 97–101. doi:10.1016/S0014-5793(02)02775-8. PMID 12044878.
- 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 Freely accessible. PMID 12477932.
- Fredriksson R, Höglund PJ, Gloriam DE; et al. (2003). "Seven evolutionarily conserved human rhodopsin G protein-coupled receptors lacking close relatives". FEBS Lett. 554 (3): 381–8. doi:10.1016/S0014-5793(03)01196-7. PMID 14623098.
- Gerhard DS, Wagner L, Feingold EA; et al. (2004). "The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC)". Genome Res. 14 (10B): 2121–7. doi:10.1101/gr.2596504. PMC 528928 Freely accessible. PMID 15489334.
- Ross MT, Grafham DV, Coffey AJ; et al. (2005). "The DNA sequence of the human X chromosome". Nature. 434 (7031): 325–37. doi:10.1038/nature03440. PMC 2665286 Freely accessible. PMID 15772651.
- Overton HA, Babbs AJ, Doel SM; et al. (2006). "Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents". Cell Metab. 3 (3): 167–75. doi:10.1016/j.cmet.2006.02.004. PMID 16517404.
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- ↑ "Entrez Gene: GPR119 G protein-coupled receptor 119".
- ↑ 2.0 2.1 Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ 5.0 5.1 5.2 5.3 5.4 5.5 Overton HA, Babbs AJ, Doel SM, Fyfe MC, Gardner LS, Griffin G, Jackson HC, Procter MJ, Rasamison CM, Tang-Christensen M, Widdowson PS, Williams GM, Reynet C. (2006). "Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents". Cell Metab. 3 (3): 167–175. doi:10.1016/j.cmet.2006.02.004. PMID 16517404.
- ↑ 6.0 6.1 6.2 Ning Y, O'Neill K, Lan H, Pang L, Shan LX, Hawes BE, Hedrick JA. (2008). "Endogenous and synthetic agonists of GPR119 differ in signalling pathways and their effects on insulin secretion in MIN6c4 insulinoma cells". Br J Pharmacol. 155 (7): 1056–65. doi:10.1038/bjp.2008.337. PMC 2528830 Freely accessible. PMID 18724386.
- ↑ 7.0 7.1 Swaminath G. (2008). "Fatty acid binding receptors and their physiological role in type 2 diabetes". Arch Pharm (Weinheim). 341 (12): 753–761. doi:10.1002/ardp.200800096. PMID 19009545.
- ↑ Lan H, Vassileva G, Corona A, Liu L, Baker H, Golovko A, Abbondanzo SJ, Hu W, Yang S, Ning Y, Del Vecchio RA, Poulet F, Laverty M, Gustafson EL, Hedrick JA, Kowalski TJ. (2009). "GPR119 is required for physiological regulation of glucagon-like peptide-1 secretion but not for metabolic homeostasis". J Endocrinol. 201 (2): 219–230. doi:10.1677/JOE-08-0453. PMID 19282326.
- ↑ 9.0 9.1 9.2 Overton HA, Fyfe MC, Reynet C. (2007). "GPR119, a novel G protein-coupled receptor target for the treatment of type 2 diabetes and obesity". Br J Pharmacol. 153 (Suppl 1): S76–81. doi:10.1038/sj.bjp.0707529. PMC 2268073 Freely accessible. PMID 18037923.
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ Semple G, Fioravanti B, Pereira G, Calderon I, Uy J, Choi K, Xiong Y, Ren A, Morgan M, Dave V, Thomsen W, Unett DJ, Xing C, Bossie S, Carroll C, Chu ZL, Grottick AJ, Hauser EK, Leonard J, Jones RM. (2008). "Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119". J Med Chem. 51 (17): 5172–5175. doi:10.1021/jm8006867. PMID 18698756.
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ Godlewski, G.; Offertáler, L.; Wagner, J. A.; Kunos, G. (2009). "Receptors for acylethanolamides—GPR55 and GPR119". Prostaglandins & Other Lipid Mediators. 89 (3-4): 105–297. doi:10.1016/j.prostaglandins.2009.07.001. PMC 2751869 Freely accessible. PMID 19615459.
