Novel GPR119 agonist AS1669058 potentiates insulin secretion from rat islets and has potent anti-diabetic effects in ICR and diabetic db/db mice

Life Sciences

Volumn 92, Issue 2, 2013, Pages 167-173

  Oshima, Hiroyuki ^a   Yoshida, Shigeru ^a   Ohishi, Takahide ^a   Matsui, Tetsuo ^a   Tanaka, Hirotsugu ^a   Yonetoku, Yasuhiro ^a   Shibasaki, Masayuki ^a   Uchiyama, Yasuo ^b  

^a ASTELLAS PHARMA INC   (Japan)

^b JUNTENDO UNIVERSITY   (Japan)

Author keywords

cAMP; GPR119; Insulin secretion; Pancreatic cell; Type 2 diabetes

Indexed keywords

2 (4 BROMO 2,5 DIFLUOROPHENYL) 6 METHYL N [2 (1 OXIDOPYRIDIN 3 YL)ETHYL]PYRIMIDIN 4 AMINE ETHANEDIOATE; ANTIDIABETIC AGENT; G PROTEIN COUPLED RECEPTOR; G PROTEIN COUPLED RECEPTOR 119; GLUCOSE; INSULIN; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIDIABETIC ACTIVITY; ARTICLE; BLOOD SAMPLING; CELL LINE; CONTROLLED STUDY; DRUG BLOOD LEVEL; GLUCOSE BLOOD LEVEL; HUMAN; HUMAN CELL; HYPERGLYCEMIA; IN VIVO STUDY; INSULIN BLOOD LEVEL; INSULIN RELEASE; MALE; MOUSE; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; ORAL GLUCOSE TOLERANCE TEST; PANCREAS ISLET BETA CELL; RAT; SINGLE DRUG DOSE; TREATMENT DURATION;

ANIMALS; BLOOD GLUCOSE; DISEASE MODELS, ANIMAL; DOSE-RESPONSE RELATIONSHIP, DRUG; HYPOGLYCEMIC AGENTS; INSULIN; INSULIN-SECRETING CELLS; MALE; MICE; MICE, INBRED ICR; PYRIDINES; PYRIMIDINES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, G-PROTEIN-COUPLED;

CRICETINAE; MUS; RATTUS;

EID: 84872340261     PISSN: 00243205     EISSN: 18790631     Source Type: Journal    
DOI: 10.1016/j.lfs.2012.11.015     Document Type: Article

References (31)

1. S.A. Amiel, T. Dixon, R. Mann, and K. Jameson Hypoglycaemia in type 2 diabetes Diabet Med 25 2008 245 254
2. P.L. Brubaker, and D.J. Drucker Minireview: glucagon-like peptides regulate cell proliferation and apoptosis in the pancreas, gut, and central nervous system Endocrinology 145 2004 2653 2659
3. Z.L. Chu, R.M. Jones, H. He, C. Carroll, V. Gutierrez, and A. Lucman A role for beta-cell-expressed G protein-coupled receptor 119 in glycemic control by enhancing glucose-dependent insulin release Endocrinology 148 2007 2601 2609
4. Z.L. Chu, C. Carroll, J. Alfonso, V. Gutierrez, H. He, and A. Lucman A role for intestinal endocrine cell-expressed g protein-coupled receptor 119 in glycemic control by enhancing glucagon-like peptide-1 and glucose-dependent insulinotropic peptide release Endocrinology 149 2008 2038 2047
5. R.A. DeFronzo, R.C. Bonadonna, and E. Ferrannini Pathogenesis of NIDDM. A balanced overview Diabetes Care 15 1992 318 368
6. M.E. Doyle, and J.M. Egan Mechanisms of action of glucagon-like peptide 1 in the pancreas Pharmacol Ther 113 2007 546 593
7. D.J. Drucker The biology of incretin hormones Cell Metab 3 2006 153 165
8. L. Eliasson, X. Ma, E. Renstrom, S. Barg, P.O. Berggren, and J. Galvanovskis SUR1 regulates PKA-independent cAMP-induced granule priming in mouse pancreatic B-cells J Gen Physiol 121 2003 181 197
9. G.G. Holz Epac: a new cAMP-binding protein in support of glucagon-like peptide-1 receptor-mediated signal transduction in the pancreatic beta-cell Diabetes 53 2004 5 13
10. G.G. Holz New insights concerning the glucose-dependent insulin secretagogue action of glucagon-like peptide-1 in pancreatic beta-cells Horm Metab Res 36 2004 787 794
11. A.M. Jennings, R.M. Wilson, and J.D. Ward Symptomatic hypoglycemia in NIDDM patients treated with oral hypoglycemic agents Diabetes Care 12 1989 203 208
12. R.M. Jones, J.N. Leonard, D.J. Buzard, and J. Lehmann GPR119 agonists for the treatment of type 2 diabetes Expert Opin Ther Pat 19 2009 1339 1359
13. Y. Kashima, T. Miki, T. Shibasaki, N. Ozaki, M. Miyazaki, and H. Yano Critical role of cAMP-GEFII-Rim2 complex in incretin-potentiated insulin secretion J Biol Chem 276 2001 46046 46053
14. D. Kawamori, and H. Kaneto Effects of incretins on the regulation of beta-cell mass, proliferation and survival Nihon Rinsho 69 2011 821 825
15. M.A. Nauck, T. Vilsboll, B. Gallwitz, A. Garber, and S. Madsbad Incretin-based therapies: viewpoints on the way to consensus Diabetes Care 32 Suppl. 2 2009 S223 S231
16. T. Okeda, J. Ono, R. Takaki, and S. Todo Simple method for the collection of pancreatic islets by the use of Ficoll-Conray gradient Endocrinol Jpn 26 1979 495 499
17. H.A. Overton, A.J. Babbs, S.M. Doel, M.C. Fyfe, L.S. Gardner, and G. Griffin Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents Cell Metab 3 2006 167 175
18. N. Ozaki, T. Shibasaki, Y. Kashima, T. Miki, K. Takahashi, and H. Ueno cAMP-GEFII is a direct target of cAMP in regulated exocytosis Nat Cell Biol 2 2000 805 811
19. R. Perfetti, J. Zhou, M.E. Doyle, and J.M. Egan Glucagon-like peptide-1 induces cell proliferation and pancreatic-duodenum homeobox-1 expression and increases endocrine cell mass in the pancreas of old, glucose-intolerant rats Endocrinology 141 2000 4600 4605
20. M.L. Peyot, J.P. Gray, J. Lamontagne, P.J. Smith, G.G. Holz, and S.R. Madiraju Glucagon-like peptide-1 induced signaling and insulin secretion do not drive fuel and energy metabolism in primary rodent pancreatic beta-cells PLoS One 4 2009 e6221
21. H. Safayhi, H. Haase, U. Kramer, A. Bihlmayer, M. Roenfeldt, and H.P. Ammon L-type calcium channels in insulin-secreting cells: biochemical characterization and phosphorylation in RINm5F cells Mol Endocrinol 11 1997 619 629
22. Y. Sakamoto, H. Inoue, S. Kawakami, K. Miyawaki, T. Miyamoto, and K. Mizuta Expression and distribution of Gpr119 in the pancreatic islets of mice and rats: predominant localization in pancreatic polypeptide-secreting PP-cells Biochem Biophys Res Commun 351 2006 474 480
23. R.F. Santerre, R.A. Cook, R.M. Crisel, J.D. Sharp, R.J. Schmidt, and D.C. Williams Insulin synthesis in a clonal cell line of simian virus 40-transformed hamster pancreatic beta cells Proc Natl Acad Sci U S A 78 1981 4339 4343
24. J.E. Shaw, R.A. Sicree, and P.Z. Zimmet Global estimates of the prevalence of diabetes for 2010 and 2030 Diabetes Res Clin Pract 87 2010 4 14
25. T. Shibasaki, H. Takahashi, T. Miki, Y. Sunaga, K. Matsumura, and M. Yamanaka Essential role of Epac2/Rap1 signaling in regulation of insulin granule dynamics by cAMP Proc Natl Acad Sci U S A 104 2007 19333 19338
26. T. Soga, T. Ohishi, T. Matsui, T. Saito, M. Matsumoto, and J. Takasaki Lysophosphatidylcholine enhances glucose-dependent insulin secretion via an orphan G-protein-coupled receptor Biochem Biophys Res Commun 326 2005 744 751
27. S.I. Taylor, D. Accili, and Y. Imai Insulin resistance or insulin deficiency. Which is the primary cause of NIDDM? Diabetes 43 1994 735 740
28. S. Yoshida, T. Ohishi, T. Matsui, and M. Shibasaki Identification of a novel GPR119 agonist, AS1269574, with in vitro and in vivo glucose-stimulated insulin secretion Biochem Biophys Res Commun 400 2010 437 441
29. S. Yoshida, T. Ohishi, T. Matsui, H. Tanaka, H. Oshima, and Y. Yonetoku Novel GPR119 agonist AS1535907 contributes to first-phase insulin secretion in rat perfused pancreas and diabetic db/db mice Biochem Biophys Res Commun 402 2010 280 285
30. S. Yoshida, H. Tanaka, H. Oshima, T. Yamazaki, Y. Yonetoku, and T. Ohishi AS1907417, a novel GPR119 agonist, as an insulinotropic and beta-cell preservative agent for the treatment of type 2 diabetes Biochem Biophys Res Commun 400 2010 745 751
31. S. Yoshida, T. Ohishi, T. Matsui, H. Tanaka, H. Oshima, and Y. Yonetoku The role of small molecule GPR119 agonist, AS1535907, in glucose-stimulated insulin secretion and pancreatic beta-cell function Diabetes Obes Metab 13 2011 34 41