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 and human islets

Journal of Pharmacology and Experimental Therapeutics

Volumn 340, Issue 2, 2012, Pages 483-489

  Yashiro, Hiroaki ^a,b   Tsujihata, Yoshiyuki ^a,b   Takeuchi, Koji ^a   Hazama, Masatoshi ^a   Johnson, Paul R V ^b   Rorsman, Patrik ^b  

^a TAKEDA PHARMACEUTICAL COMPANY LIMITED   (Japan)

^b UNIVERSITY OF OXFORD   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

CALCIUM ION; G PROTEIN COUPLED RECEPTOR 40; GLUCAGON; GLUCAGON LIKE PEPTIDE 1; GLUCOSE; HORMONE RECEPTOR STIMULATING AGENT; INSULIN; MESSENGER RNA; TAK 875; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; CALCIUM CELL LEVEL; CELL ISOLATION; CELL SPECIFICITY; CONFOCAL MICROSCOPY; CONTROLLED STUDY; FEMALE; GLUCAGON RELEASE; HORMONE RECEPTOR INTERACTION; HUMAN; HUMAN CELL; INSULIN RELEASE; NONHUMAN; PANCREAS ISLET BETA CELL; POLYMERASE CHAIN REACTION; PRIORITY JOURNAL; PROTEIN EXPRESSION; RAT;

ANIMALS; ATP-BINDING CASSETTE TRANSPORTERS; BENZOFURANS; CALCIUM SIGNALING; DRUG SYNERGISM; GENE EXPRESSION; GLUCAGON; GLUCAGON-LIKE PEPTIDE 1; GLUCAGON-SECRETING CELLS; GLUCOSE; HUMANS; INSULIN; INSULIN-SECRETING CELLS; ISLETS OF LANGERHANS; POTASSIUM CHANNELS, INWARDLY RECTIFYING; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, DRUG; RECEPTORS, G-PROTEIN-COUPLED; RECEPTORS, GLUCAGON; SULFONES;

EID: 84856019616     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.111.187708     Document Type: Article

References (40)

1. Barg S, Galvanovskis J, Göpel SO, Rorsman P, and Eliasson L (2000) Tight coupling between electrical activity and exocytosis in mouse glucagon-secreting α-cells. Diabetes 49:1500-1510.
2. 2+ oscillations in pancreatic islet cells secreting glucagon and somatostatin. Biochem Biophys Res Commun 208:644-649.
3. Bharate SB, Nemmani KV, and Vishwakarma RA (2009) Progress in the discovery and development of small-molecule modulators of G-protein-coupled receptor 40 (GPR40/FFA1/FFAR1): an emerging target for type 2 diabetes. Expert Opin Ther Pat 19:237-264.
4. Braun M, Ramracheya R, Bengtsson M, Zhang Q, Karanauskaite J, Partridge C, Johnson PR, and Rorsman P (2008) Voltage-gated ion channels in human pancreatic β-cells: electrophysiological characterization and role in insulin secretion. Diabetes 57:1618-1628.
5. Braun M, Ramracheya R, Johnson PR, and Rorsman P (2009) Exocytotic properties of human pancreatic β-cells. Ann NY Acad Sci 1152:187-193.
6. Briscoe CP, Peat AJ, McKeown SC, Corbett DF, Goetz AS, Littleton TR, McCoy DC, Kenakin TP, Andrews JL, Ammala C, et al. (2006) Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules. Br J Pharmacol 148:619-628. (Pubitemid 43993052)
7. Collins SC, Salehi A, Eliasson L, Olofsson CS, and Rorsman P (2008) Long-term exposure of mouse pancreatic islets to oleate or palmitate results in reduced glucose-induced somatostatin and oversecretion of glucagon. Diabetologia 51:1689-1693.
8. Cryer PE (2008) The barrier of hypoglycemia in diabetes. Diabetes 57:3169-3176.
9. 2+channel-dependent exocytosis. Cell Metab 11:543-553.
10. + currents in primary cultured rat pancreatic β-cells by linoleic acids. Endocrinology 147:674-682.
11. Flodgren E, Olde B, Meidute-Abaraviciene S, Winzell MS, Ahrén B, and Salehi A (2007) GPR40 is expressed in glucagon producing cells and affects glucagon secretion. Biochem Biophys Res Commun 354:240-245. (Pubitemid 46123225)
12. Frayn KN (2003) Metabolic Regulation: A Human Perspective Oxford Blackwell Science, Oxford, UK.
13. 2+channel and link to insulin release. Am J Physiol Endocrinol Metab 289:E670-E677.
14. + channels. J Physiol 528:509-520.
15. Gromada J, Franklin I, and Wollheim CB (2007) α-Cells of the endocrine pancreas: 35 years of research but the enigma remains. Endocr Rev 28:84-116. (Pubitemid 46220851)
16. + channel-dependent regulation of glucagon release and electrical activity by glucose in wild-type and SUR1-/- mouse α-cells. Diabetes 53 (Suppl 3):S181-S189.
17. Hirasawa A, Itsubo C, Sadakane K, Hara T, Shinagawa S, Koga H, Nose H, Koshimizu TA, and Tsujimoto G (2008) Production and characterization of a monoclonal antibody against GPR40 (FFAR1; free fatty acid receptor 1). Biochem Biophys Res Commun 365:22-28. (Pubitemid 350102449)
18. 2+ channels from secretory granules. Cell Metab 10:455-465.
19. Itoh Y, Kawamata Y, Harada M, Kobayashi M, Fujii R, Fukusumi S, Ogi K, Hosoya M, Tanaka Y, Uejima H, et al. (2003) Free fatty acids regulate insulin secretion from pancreatic β cells through GPR40. Nature 422:173-176. (Pubitemid 36362750)
20. Le Marchand SJ and Piston DW (2010) Glucose suppression of glucagon secretion: metabolic and calcium responses from α-cells in intact mouse pancreatic islets. J Biol Chem 285:14389-14398.
21. MacDonald PE, De Marinis YZ, Ramracheya R, Salehi A, Ma X, Johnson PR, Cox R, Eliasson L, and Rorsman P (2007) A K ATP channel-dependent pathway within αcells regulates glucagon release from both rodent and human islets of Langerhans. PLoS Biol 5:e143.
22. MacDonald PE, Joseph JW, and Rorsman P (2005) Glucose-sensing mechanisms in pancreatic β-cells. Philos Trans R Soc Lond B Biol Sci 360:2211-2225.
23. Marchetti P, Dotta F, Lauro D, and Purrello F (2008) An overview of pancreatic β-cell defects in human type 2 diabetes: implications for treatment. Regul Pept 146:4-11.
24. + channels in the hypothalamus are essential for the maintenance of glucose homeostasis. Nat Neurosci 4:507-512.
25. Morgan NG and Dhayal S (2009) G-protein coupled receptors mediating long chain fatty acid signalling in the pancreatic β-cell. Biochem Pharmacol 78:1419-1427.
26. Nadal A, Quesada I, and Soria B (1999) Homologous and heterologous asynchronicity between identified α-, β- and δ-cells within intact islets of Langerhans in the mouse. J Physiol 517:85-93. (Pubitemid 29243473)
27. Negoro N, Sasaki S, Mikami S, Ito M, Suzuki M, Tsujihata Y, Ito R, Takeuchi K, Suzuki N, Miyazaki J, et al. (2010) Discovery of TAK-875: a potent, selective, and orally bioavailable GPR40 agonist. ACS Med Chem Lett 1:290-294.
28. Olofsson CS, Collins S, Bengtsson M, Eliasson L, Salehi A, Shimomura K, Tarasov A, Holm C, Ashcroft F, and Rorsman P (2007) Long-term exposure to glucose and lipids inhibits glucose-induced insulin secretion downstream of granule fusion with plasma membrane. Diabetes 56:1888-1897. (Pubitemid 47025450)
29. Olofsson CS, Salehi A, Göpel SO, Holm C, and Rorsman P (2004a) Palmitate stimulation of glucagon secretion in mouse pancreatic α-cells results from activation of L-type calcium channels and elevation of cytoplasmic calcium. Diabetes 53:2836-2843. (Pubitemid 39425908)
30. 2+ currents and the size of the readily releasable granule pool in mouse pancreatic β-cells. J Physiol 557:935-948.
31. Prentki M, Joly E, El-Assaad W, and Roduit R (2002) Malonyl-CoA signaling, lipid partitioning, and glucolipotoxicity: role in β-cell adaptation and failure in the etiology of diabetes. Diabetes 51 (Suppl 3):S405-S413. (Pubitemid 35403424)
32. Quesada I, Nadal A, and Soria B (1999) Different effects of tolbutamide and diazoxide in α, β-, and δ-cells within intact islets of Langerhans. Diabetes 48:2390-2397. (Pubitemid 30395431)
33. Ramracheya R, Ward C, Shigeto M, Walker JN, Amisten S, Zhang Q, Johnson PR, Rorsman P, and Braun M (2010) Membrane potential-dependent inactivation of voltage-gated ion channels in α-cells inhibits glucagon secretion from human islets. Diabetes 59:2198-2208.
34. Ricordi C, Lacy PE, Finke EH, Olack BJ, and Scharp DW (1988) Automated method for isolation of human pancreatic islets. Diabetes 37:413-420. (Pubitemid 18096377)
35. Shah P, Basu A, Basu R, and Rizza R (1999) Impact of lack of suppression of glucagon on glucose tolerance in humans. Am J Physiol Endocrinol Metab 277:E283-E290. (Pubitemid 29413834)
36. Tan CP, Feng Y, Zhou YP, Eiermann GJ, Petrov A, Zhou C, Lin S, Salituro G, Meinke P, Mosley R, et al. (2008) Selective small-molecule agonists of G protein-coupled receptor 40 promote glucose-dependent insulin secretion and reduce blood glucose in mice. Diabetes 57:2211-2219.
37. Tomita T, Masuzaki H, Iwakura H, Fujikura J, Noguchi M, Tanaka T, Ebihara K, Kawamura J, Komoto I, Kawaguchi Y, et al. (2006) Expression of the gene for a membrane-bound fatty acid receptor in the pancreas and islet cell tumours in humans: evidence for GPR40 expression in pancreatic β cells and implications for insulin secretion. Diabetologia 49:962-968.
38. Tsujihata Y, Ito R, Suzuki M, Harada A, Negoro N, Yasuma T, Momose Y, and Takeuchi K (2011) TAK-875, an orally available G protein-coupled receptor 40/free fatty acid receptor 1 agonist, enhances glucose-dependent insulin secretion and improves both postprandial and fasting hyperglycemia in type 2 diabetic rats. J Pharmacol Exp Ther 339:228-237.
39. Vieira E, Salehi A, and Gylfe E (2007) Glucose inhibits glucagon secretion by a direct effect on mouse pancreatic α cells. Diabetologia 50:370-379.
40. 2+]i increase in pancreatic islet α-cells. J Endocrinol 210:173-179.