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词条 GPR119
释义

  1. Pharmacology

  2. Ligands

  3. References

  4. Further reading

{{Infobox_gene}}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]

  • 2-Oleoylglycerol [13]
  • Anandamide[9]
  • AR-231,453[14]
  • MBX-2982[15]
  • Oleoylethanolamide[2][5][9] (Endogenous Ligand) [2]
  • PSN-375,963[5][6]
  • PSN-632,408[5][6]
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References

1. ^{{cite web | title = Entrez Gene: GPR119 G protein-coupled receptor 119| url = https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=139760| accessdate = }}
2. ^1 2 {{cite journal | vauthors = Brown AJ | title = Novel cannabinoid receptors | journal = British Journal of Pharmacology | volume = 152 | issue = 5 | pages = 567–75 | date = Nov 2007 | pmid = 17906678 | pmc = 2190013 | doi = 10.1038/sj.bjp.0707481 }}
3. ^{{cite journal | vauthors = Izzo AA, Sharkey KA | title = Cannabinoids and the gut: new developments and emerging concepts | journal = Pharmacology & Therapeutics | volume = 126 | issue = 1 | pages = 21–38 | date = Apr 2010 | pmid = 20117132 | doi = 10.1016/j.pharmthera.2009.12.005 }}
4. ^{{cite journal | vauthors = McHugh D, Hu SS, Rimmerman N, Juknat A, Vogel Z, Walker JM, Bradshaw HB | title = N-arachidonoyl glycine, an abundant endogenous lipid, potently drives directed cellular migration through GPR18, the putative abnormal cannabidiol receptor | journal = BMC Neuroscience | volume = 11 | pages = 44 | date = March 2010 | pmid = 20346144 | pmc = 2865488 | doi = 10.1186/1471-2202-11-44 }}
5. ^1 2 3 4 5 {{cite journal | vauthors = 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 | title = Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents | journal = Cell Metabolism | volume = 3 | issue = 3 | pages = 167–75 | date = Mar 2006 | pmid = 16517404 | doi = 10.1016/j.cmet.2006.02.004 }}
6. ^1 2 {{cite journal | vauthors = Ning Y, O'Neill K, Lan H, Pang L, Shan LX, Hawes BE, Hedrick JA | title = Endogenous and synthetic agonists of GPR119 differ in signalling pathways and their effects on insulin secretion in MIN6c4 insulinoma cells | journal = British Journal of Pharmacology | volume = 155 | issue = 7 | pages = 1056–65 | date = Dec 2008 | pmid = 18724386 | pmc = 2528830 | doi = 10.1038/bjp.2008.337 }}
7. ^1 {{cite journal | vauthors = Swaminath G | title = Fatty acid binding receptors and their physiological role in type 2 diabetes | journal = Archiv der Pharmazie | volume = 341 | issue = 12 | pages = 753–61 | date = Dec 2008 | pmid = 19009545 | doi = 10.1002/ardp.200800096 }}
8. ^{{cite journal | vauthors = 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 | title = GPR119 is required for physiological regulation of glucagon-like peptide-1 secretion but not for metabolic homeostasis | journal = The Journal of Endocrinology | volume = 201 | issue = 2 | pages = 219–30 | date = May 2009 | pmid = 19282326 | doi = 10.1677/JOE-08-0453 }}
9. ^1 2 {{cite journal | vauthors = Overton HA, Fyfe MC, Reynet C | title = GPR119, a novel G protein-coupled receptor target for the treatment of type 2 diabetes and obesity | journal = British Journal of Pharmacology | volume = 153 Suppl 1 | issue = | pages = S76–81 | date = March 2008 | pmid = 18037923 | pmc = 2268073 | doi = 10.1038/sj.bjp.0707529 }}
10. ^{{cite journal | vauthors = Shah U | title = GPR119 agonists: a promising new approach for the treatment of type 2 diabetes and related metabolic disorders | journal = Current Opinion in Drug Discovery & Development | volume = 12 | issue = 4 | pages = 519–32 | date = Jul 2009 | pmid = 19562648 | doi = }}
11. ^{{cite journal | vauthors = Godlewski G, Offertáler L, Wagner JA, Kunos G | title = Receptors for acylethanolamides-GPR55 and GPR119 | journal = Prostaglandins & Other Lipid Mediators | volume = 89 | issue = 3-4 | pages = 105–11 | date = Sep 2009 | pmid = 19615459 | pmc = 2751869 | doi = 10.1016/j.prostaglandins.2009.07.001 }}
12. ^{{cite journal | vauthors = Wu Y, Kuntz JD, Carpenter AJ, Fang J, Sauls HR, Gomez DJ, Ammala C, Xu Y, Hart S, Tadepalli S | title = 2,5-Disubstituted pyridines as potent GPR119 agonists | journal = Bioorganic & Medicinal Chemistry Letters | volume = 20 | issue = 8 | pages = 2577–81 | date = Apr 2010 | pmid = 20227877 | doi = 10.1016/j.bmcl.2010.02.083 }}
13. ^{{cite journal | vauthors = Hansen KB, Rosenkilde MM, Knop FK, Wellner N, Diep TA, Rehfeld JF, Andersen UB, Holst JJ, Hansen HS | title = 2-Oleoyl glycerol is a GPR119 agonist and signals GLP-1 release in humans | journal = The Journal of Clinical Endocrinology and Metabolism | volume = 96 | issue = 9 | pages = E1409–E1417 | date = Sep 2011 | pmid = 21778222 | doi = 10.1210/jc.2011-0647 }}
14. ^{{cite journal | vauthors = 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 | title = Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119 | journal = Journal of Medicinal Chemistry | volume = 51 | issue = 17 | pages = 5172–5 | date = Sep 2008 | pmid = 18698756 | doi = 10.1021/jm8006867 }}
15. ^{{cite journal | vauthors = Jones RM, Leonard JN, Buzard DJ, Lehmann J | title = GPR119 agonists for the treatment of type 2 diabetes | journal = Expert Opinion on Therapeutic Patents | volume = 19 | issue = 10 | pages = 1339–59 | date = Oct 2009 | pmid = 19780700 | doi = 10.1517/13543770903153878 }}

Further reading

{{refbegin|33em}}
  • {{cite journal | vauthors = Takeda S, Kadowaki S, Haga T, Takaesu H, Mitaku S | title = Identification of G protein-coupled receptor genes from the human genome sequence | journal = FEBS Letters | volume = 520 | issue = 1-3 | pages = 97–101 | date = Jun 2002 | pmid = 12044878 | doi = 10.1016/S0014-5793(02)02775-8 }}
  • {{cite journal | vauthors = Fredriksson R, Höglund PJ, Gloriam DE, Lagerström MC, Schiöth HB | title = Seven evolutionarily conserved human rhodopsin G protein-coupled receptors lacking close relatives | journal = FEBS Letters | volume = 554 | issue = 3 | pages = 381–8 | date = Nov 2003 | pmid = 14623098 | doi = 10.1016/S0014-5793(03)01196-7 }}
{{refend}}{{G protein-coupled receptors}}{{Cannabinoidergics}}{{transmembranereceptor-stub}}

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