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RefSeq (mRNA)



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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]


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]


A number of endogenous and synthetic ligands for this receptor have been identified:[10][11][12]


  1. "Entrez Gene: GPR119 G protein-coupled receptor 119".
  2. 2.0 2.1 2.2 Brown AJ (Nov 2007). "Novel cannabinoid receptors". British Journal of Pharmacology. 152 (5): 567–75. doi:10.1038/sj.bjp.0707481. PMC 2190013. PMID 17906678.
  3. Izzo AA, Sharkey KA (Apr 2010). "Cannabinoids and the gut: new developments and emerging concepts". Pharmacology & Therapeutics. 126 (1): 21–38. doi:10.1016/j.pharmthera.2009.12.005. PMID 20117132.
  4. McHugh D, Hu SS, Rimmerman N, Juknat A, Vogel Z, Walker JM, Bradshaw HB (March 2010). "N-arachidonoyl glycine, an abundant endogenous lipid, potently drives directed cellular migration through GPR18, the putative abnormal cannabidiol receptor". BMC Neuroscience. 11: 44. doi:10.1186/1471-2202-11-44. PMC 2865488. PMID 20346144.
  5. 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 (Mar 2006). "Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents". Cell Metabolism. 3 (3): 167–75. doi:10.1016/j.cmet.2006.02.004. PMID 16517404.
  6. 6.0 6.1 6.2 Ning Y, O'Neill K, Lan H, Pang L, Shan LX, Hawes BE, Hedrick JA (Dec 2008). "Endogenous and synthetic agonists of GPR119 differ in signalling pathways and their effects on insulin secretion in MIN6c4 insulinoma cells". British Journal of Pharmacology. 155 (7): 1056–65. doi:10.1038/bjp.2008.337. PMC 2528830. PMID 18724386.
  7. 7.0 7.1 Swaminath G (Dec 2008). "Fatty acid binding receptors and their physiological role in type 2 diabetes". Archiv der Pharmazie. 341 (12): 753–61. doi:10.1002/ardp.200800096. PMID 19009545.
  8. 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 (May 2009). "GPR119 is required for physiological regulation of glucagon-like peptide-1 secretion but not for metabolic homeostasis". The Journal of Endocrinology. 201 (2): 219–30. doi:10.1677/JOE-08-0453. PMID 19282326.
  9. 9.0 9.1 9.2 Overton HA, Fyfe MC, Reynet C (March 2008). "GPR119, a novel G protein-coupled receptor target for the treatment of type 2 diabetes and obesity". British Journal of Pharmacology. 153 Suppl 1: S76–81. doi:10.1038/sj.bjp.0707529. PMC 2268073. PMID 18037923.
  10. Shah U (Jul 2009). "GPR119 agonists: a promising new approach for the treatment of type 2 diabetes and related metabolic disorders". Current Opinion in Drug Discovery & Development. 12 (4): 519–32. PMID 19562648.
  11. Godlewski G, Offertáler L, Wagner JA, Kunos G (Sep 2009). "Receptors for acylethanolamides-GPR55 and GPR119". Prostaglandins & Other Lipid Mediators. 89 (3–4): 105–11. doi:10.1016/j.prostaglandins.2009.07.001. PMC 2751869. PMID 19615459.
  12. Wu Y, Kuntz JD, Carpenter AJ, Fang J, Sauls HR, Gomez DJ, Ammala C, Xu Y, Hart S, Tadepalli S (Apr 2010). "2,5-Disubstituted pyridines as potent GPR119 agonists". Bioorganic & Medicinal Chemistry Letters. 20 (8): 2577–81. doi:10.1016/j.bmcl.2010.02.083. PMID 20227877.
  13. Hansen KB, Rosenkilde MM, Knop FK, Wellner N, Diep TA, Rehfeld JF, Andersen UB, Holst JJ, Hansen HS (Sep 2011). "2-Oleoyl glycerol is a GPR119 agonist and signals GLP-1 release in humans". The Journal of Clinical Endocrinology and Metabolism. 96 (9): E1409–E1417. doi:10.1210/jc.2011-0647. PMID 21778222.
  14. 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 (Sep 2008). "Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119". Journal of Medicinal Chemistry. 51 (17): 5172–5. doi:10.1021/jm8006867. PMID 18698756.
  15. Jones RM, Leonard JN, Buzard DJ, Lehmann J (Oct 2009). "GPR119 agonists for the treatment of type 2 diabetes". Expert Opinion on Therapeutic Patents. 19 (10): 1339–59. doi:10.1517/13543770903153878. PMID 19780700.

Further reading

  • Takeda S, Kadowaki S, Haga T, Takaesu H, Mitaku S (Jun 2002). "Identification of G protein-coupled receptor genes from the human genome sequence". FEBS Letters. 520 (1–3): 97–101. doi:10.1016/S0014-5793(02)02775-8. PMID 12044878.
  • Fredriksson R, Höglund PJ, Gloriam DE, Lagerström MC, Schiöth HB (Nov 2003). "Seven evolutionarily conserved human rhodopsin G protein-coupled receptors lacking close relatives". FEBS Letters. 554 (3): 381–8. doi:10.1016/S0014-5793(03)01196-7. PMID 14623098.