Free fatty acid receptor 1: A new drug target for type 2 diabetes?

Canadian Journal of Diabetes

Volumn 36, Issue 5, 2012, Pages 275-280

  Ferdaoussi, Mourad ^a,b   Bergeron, Valérie ^a,b   Kebede, Melkam ^a,b,c   Mancini, Arturo ^a,b   Alquier, Thierry ^a,b   Poitout, Vincent ^a,b  

^a CENTRE HOSPITALIER DE L UNIVERSITÉ DE MONTRÉAL   (Canada)

^b UNIVERSITÉ DE MONTRÉAL   (Canada)

^c UNIVERSITY OF WISCONSIN MADISON   (United States)

Author keywords

Beta cell; Fatty acids; Gpr40; Insulin; Type 2 diabetes

Indexed keywords

ANTIDIABETIC AGENT; CHOLECYSTOKININ; G PROTEIN COUPLED RECEPTOR 40; GASTRIC INHIBITORY POLYPEPTIDE; GLUCAGON LIKE PEPTIDE 1; GLUCOSE; HEMOGLOBIN A1C; INSULIN; LONG CHAIN FATTY ACID; MEDIUM CHAIN FATTY ACID; PHOSPHATIDYLINOSITOL 3 KINASE; PLACEBO; PROTEIN KINASE D; TAK 875; TRANSCRIPTION FACTOR PDX 1; UNCLASSIFIED DRUG;

CHROMOSOME 19; DRUG TARGETING; FATTY ACID METABOLISM; GENE EXPRESSION REGULATION; GLUCOSE INTOLERANCE; GLYCEMIC CONTROL; HUMAN; HYPOGLYCEMIA; INSULIN RELEASE; INSULIN SENSITIVITY; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; PANCREAS ISLET BETA CELL; REVIEW;

EID: 84872652763     PISSN: 14992671     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.jcjd.2012.08.002     Document Type: Review

References (50)

1. Briscoe CP, Tadayyon M, Andrews JL, et al. The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids. J Biol Chem 2003;278:11303-11.
2. Itoh Y, Kawamata Y, Harada M, et al. Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40. Nature 2003;422:173-6.
3. Kotarsky K, Nilsson NE, Flodgren E, et al. A human cell surface receptor activated by free fatty acids and thiazolidinedione drugs. Biochem Biophys Res Commun 2003;301:406-10.
4. Alquier T, Peyot ML, Latour MG, et al. Deletion of GPR40 impairs glucoseinduced insulin secretion in vivo in mice without affecting intracellular fuel metabolism in islets. Diabetes 2009;58:2607-15.
5. Latour MG, Alquier T, Oseid E, et al. GPR40 is necessary but not sufficient for fatty acid stimulation of insulin secretion in vivo. Diabetes 2007;56:1087-94.
6. Burant CF, Viswanathan P, Marcinak J, et al. TAK-875 versus placebo or glimepiride in type 2 diabetes mellitus: a phase 2, randomised, double-blind, placebo-controlled trial. Lancet 2012;379:1403-11.
7. Araki T, Hirayama M, Hiroi S, et al. GPR40-induced insulin secretion by the novel agonist TAK-875: first clinical findings in patients with type 2 diabetes. Diabetes Obes Metab 2012;14:271-8.
8. Brownlie R, Mayers RM, Pierce JA, et al. The long-chain fatty acid receptor, GPR40, and glucolipotoxicity: investigations using GPR40-knockout mice. Biochem Soc Trans 2008;36:950-4.
9. Lan H, Hoos LM, Liu L, et al. Lack of FFAR1/GPR40 does not protect mice from high-fat diet-induced metabolic disease. Diabetes 2008;57:2999-3006.
10. Steneberg P, Rubins N, Bartoov-Shifman R, et al. The FFA receptor GPR40 links hyperinsulinemia, hepatic steatosis, and impaired glucose homeostasis in mouse. Cell Metab 2005;1:245-58.
11. Schnell S, Schaefer M, Schofl C. Free fatty acids increase cytosolic free calcium and stimulate insulin secretion from beta-cells through activation of GPR40. Mol Cell Endocrinol 2007;263:173-80.
12. Zhang Y, Xu M, Zhang S, et al. The role of G protein-coupled receptor 40 in lipoapoptosis in mouse beta-cell line NIT-1. J Mol Endocrinol 2007;38:651-61.
13. Salehi A, Flodgren E, Nilsson NE, et al. Free fatty acid receptor 1 (FFA(1)R/ GPR40) and its involvement in fatty-acid-stimulated insulin secretion. Cell Tissue Res 2005;322:207-15.
14. Tan CP, Feng Y, Zhou YP, et al. Selective small-molecule agonists of G proteincoupled receptor 40 promote glucose-dependent insulin secretion and reduce blood glucose in mice. Diabetes 2008;57:2211-9.
15. Briscoe CP, Peat AJ, McKeown SC, et al. Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules. Br J Pharmacol 2006;148:619-28.
16. Nolan CJ, Madiraju MS, Delghingaro-Augusto V, et al. Fatty acid signaling in the beta-cell and insulin secretion. Diabetes 2006;55(suppl 2):S16-23.
17. Poitout V, Robertson RP. Glucolipotoxicity: fuel excess and beta-cell dysfunction. Endocr Rev 2008;29:351-66.
18. Kebede M, Alquier T, Latour MG, et al. The fatty acid receptor GPR40 plays a role in insulin secretion in vivo after high-fat feeding. Diabetes 2008;57:2432-7.
19. Nagasumi K, Esaki R, Iwachidow K, et al. Overexpression of GPR40 in pancreatic beta-cells augments glucose-stimulated insulin secretion and improves glucose tolerance in normal and diabetic mice. Diabetes 2009;58:1067-76.
20. Lin DC, Zhang J, Zhuang R, et al. AMG 837: a novel GPR40/FFA1 agonist that enhances insulin secretion and lowers glucose levels in rodents. PLoS One 2011;6:e27270.
21. Vettor R, Granzotto M, De Stefani D, et al. Loss-of-function mutation of the GPR40 gene associates with abnormal stimulated insulin secretion by acting on intracellular calcium mobilization. J Clin Endocrinol Metab 2008;93:3541-50.
22. Naik H, Vakilynejad M, Wu J, et al. Safety, tolerability, pharmacokinetics, and pharmacodynamic properties of the GPR40 agonist TAK-875: results from a double-blind, placebo-controlled single oral dose rising study in healthy volunteers. J Clin Pharmacol 2012;52:1007-16.
23. Tsujihata Y, Ito R, Suzuki M, et al. TAK-875, an orally available G proteincoupled receptor 40/free fatty acid receptor 1 agonist, enhances glucosedependent insulin secretion and improves both postprandial and fasting hyperglycemia in type 2 diabetic rats. J Pharmacol Exp Ther 2011;339:228-37.
24. Yashiro H, Tsujihata Y, Takeuchi K, et al. The effects of TAK-875, a selective G protein-coupled receptor 40/free fatty acid 1 agonist, on insulin and glucagon secretion in isolated rat andhuman islets. J Pharmacol Exp Ther 2012;340:483-9.
25. Flodgren E, Olde B, Meidute-Abaraviciene S, et al. GPR40 is expressed in glucagon producing cells and affects glucagon secretion. Biochem Biophys Res Commun 2007;354:240-5.
26. Wang L, Zhao Y, Gui B, et al. Acute stimulation of glucagon secretion by linoleic acid results from GPR40 activation and [Ca2+]i increase in pancreatic islet {alpha}-cells. J Endocrinol 2011;210:173-9.
27. Henquin JC. Triggering and amplifying pathways of regulation of insulin secretion by glucose. Diabetes 2000;49:1751-60.
28. Fujiwara K, Maekawa F, Yada T. Oleic acid interacts with GPR40 to induce Ca2+ signaling in rat islet beta-cells: mediation by PLC and L-type Ca2+ channel and link to insulin release. Am J Physiol Endocrinol Metab 2005;289:E670-7.
29. Shapiro H, Shachar S, Sekler I, et al. Role of GPR40 in fatty acid action on the beta cell line INS-1E. Biochem Biophys Res Commun 2005;335:97-104.
30. Ullrich S, Pfleiderer M, Liebscher K, et al. Effects of small FFA1 receptor agonists in insulin secreting cells. Diabetes 2011;60(suppl 1):2023P.
31. Feng DD, Luo Z, Roh SG, et al. Reduction in voltage-gated K+ currents in primary cultured rat pancreatic beta-cells by linoleic acids. Endocrinology 2006;147:674-82.
32. Ferdaoussi M, Bergeron V, Zarrouki B, et al. G protein-coupled receptor (GPR)40-dependent potentiation of insulin secretion inmouseislets is mediated by protein kinase D1. Diabetologia 2012 http://dx.doi.org/10.1007/s00125-012-2650-x.
33. Kong KC, Butcher AJ, McWilliams P, et al. M3-muscarinic receptor promotes insulin release via receptor phosphorylation/arrestin-dependent activation of protein kinase D1. Proc Natl Acad Sci USA 2010;107:21181-6.
34. Sumara G, Formentini I, Collins S, et al. Regulation of PKD by the MAPK p38delta in insulin secretion and glucose homeostasis. Cell 2009;136:235-48.
35. Kwan EP, Xie L, Sheu L, et al. Munc13-1 deficiency reduces insulin secretion and causes abnormal glucose tolerance. Diabetes 2006;55:1421-9.
36. Wang Z, Thurmond DC. Mechanisms of biphasic insulin-granule exocytosis-roles of the cytoskeleton, small GTPases and SNARE proteins. J Cell Sci 2009;122:893-903.
37. Eiseler T, Hausser A, De Kimpe L, et al. Protein kinase D controls actin polymerization and cell motility through phosphorylation of cortactin. J Biol Chem 2010;285:18672-83.
38. Galandrin S, Oligny-Longpre G, Bouvier M. The evasive nature of drug efficacy: implications for drug discovery. Trends Pharmacol Sci 2007;28:423-30.
39. Bartoov-Shifman R, Ridner G, Bahar K, et al. Regulation of the gene encoding GPR40, a fatty acid receptor expressed selectively in pancreatic beta cells. J Biol Chem 2007;282:23561-71.
40. Kebede M, Ferdaoussi M, Mancini A, et al. Glucose activates free fatty acid receptor 1 gene transcription via phosphatidylinositol-3-kinase-dependent O-GlcNAcylation of pancreas-duodenum homeobox-1. Proc Natl Acad Sci USA 2012;109:2376-81.
41. Hagman DK, Hays LB, Parazzoli SD, et al. Palmitate inhibits insulin gene expression by altering PDX-1 nuclear localization and reducing MafA expression in isolated rat islets of Langerhans. J Biol Chem 2005;280:32413-8.
42. Del GS, Bugliani M, D'Aleo V, et al. G-protein-coupled receptor 40 (GPR40) expression and its regulation in human pancreatic islets: the role of type 2 diabetes and fatty acids. Nutr Metab Cardiovasc Dis 2010;20:22-5.
43. Fontes G, Zarrouki B, Hagman DK, et al. Glucolipotoxicity age-dependently impairs beta cell function in rats despite a marked increase in beta cell mass. Diabetologia 2010;53:2369-79.
44. Edfalk S, Steneberg P, Edlund H. Gpr40 is expressed in enteroendocrine cells and mediates free fatty acid stimulation of incretin secretion. Diabetes 2008; 57:2280-7.
45. Liou AP, Lu X, Sei Y, et al. The G-protein-coupled receptor GPR40 directly mediates long-chain fatty acid-induced secretion of cholecystokinin. Gastroenterology 2011;140:903-12.
46. Cartoni C, Yasumatsu K, Ohkuri T, et al. Taste preference for fatty acids is mediated by GPR40 and GPR120. J Neurosci 2010;30:8376-82.
47. Ma D, Tao B, Warashina S, et al. Expression of free fatty acid receptor GPR40 in the central nervous system of adult monkeys. Neurosci Res 2007;58: 394-401.
48. Nakamoto K, Nishinaka T, Matsumoto K, et al. Involvement of the long-chain fatty acid receptor GPR40 as a novel pain regulatory system. Brain Res 2012; 1432:74-83.
49. Cornish J, MacGibbon A, Lin JM, et al. Modulation of osteoclastogenesis by fatty acids. Endocrinology 2008;149:5688-95.
50. Hardy S, St-Onge GG, Joly E, et al. Oleate promotes the proliferation of breast cancer cells via the G protein-coupled receptor GPR40. J Biol Chem 2005;280: 13285-91.