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G protein-coupled receptor 119
Symbols GPR119 ; GPCR2
External IDs OMIM300513 MGI2668412 HomoloGene18670 IUPHAR: GPR119 ChEMBL: 5652 GeneCards: GPR119 Gene
RNA expression pattern
PBB GE GPR119 gnf1h09789 at tn.png
More reference expression data
Species Human Mouse
Entrez 139760 236781
Ensembl ENSG00000147262 ENSMUSG00000051209
UniProt Q8TDV5 Q7TQP3
RefSeq (mRNA) NM_178471 NM_181751
RefSeq (protein) NP_848566 NP_861416
Location (UCSC) Chr X:
129.52 – 129.52 Mb
Chr X:
48.67 – 48.67 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]


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. ^ a b c Brown A (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 A, Sharkey K (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 S, Rimmerman N, Juknat A, Vogel Z, Walker J et al. (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. ^ a b c d e f Overton H, Babbs A, Doel S, Fyfe M, Gardner L, Griffin G et al. (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. ^ a b c Ning Y, O'Neill K, Lan H, Pang L, Shan L, Hawes B et al. (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. ^ a b 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 et al. (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. ^ a b c Overton H, Fyfe M, Reynet C (Mar 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 (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 J, 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 J, Carpenter A, Fang J, Sauls H, Gomez D et al. (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 K, Rosenkilde M, Knop F, Wellner N, Diep T, Rehfeld J et al. (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 et al. (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 R, Leonard J, Buzard D, 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[edit]

  • 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 P, Gloriam D, Lagerström M, Schiöth H (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. 
  • Overton H, Babbs A, Doel S, Fyfe M, Gardner L, Griffin G et al. (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.