Novel GPR119 agonist AS1535907 contributes to first-phase insulin secretion in rat perfused pancreas and diabetic db/db mice

Biochemical and Biophysical Research Communications

Volumn 402, Issue 2, 2010, Pages 280-285

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

^a ASTELLAS PHARMA INC   (Japan)

Author keywords

AS1535907; First phase insulin secretion; Glibenclamide; GPR119; Isolated perfused pancreas

Indexed keywords

2 (4 BROMOPHENYL) 6 METHYL N [2 (1-OXIDOPYRIDIN 3 YL) ETHYL]PYRIMIDIN 4 AMINE; ANTIDIABETIC AGENT; AS 1269574; AS 1535907; G PROTEIN COUPLED RECEPTOR; GLIBENCLAMIDE; GLUCOSE; INSULIN; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; DIABETES MELLITUS; DOSE RESPONSE; DRUG ACTIVITY; EMBRYO; HUMAN; HUMAN CELL; HYPOGLYCEMIA; IN VIVO STUDY; INSULIN RELEASE; MALE; MOUSE; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; NUCLEOTIDE SEQUENCE; ORAL GLUCOSE TOLERANCE TEST; PANCREAS PERFUSION; PRIORITY JOURNAL; RAT;

ANIMALS; CELL LINE; CYCLIC N-OXIDES; DIABETES MELLITUS, TYPE 2; GLUCOSE; GLUCOSE TOLERANCE TEST; HUMANS; HYPOGLYCEMIC AGENTS; INSULIN; ISLETS OF LANGERHANS; MALE; MICE; PANCREAS; PERFUSION; PYRIDINES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, G-PROTEIN-COUPLED;

MUS; RATTUS;

EID: 78149470681     PISSN: 0006291X     EISSN: 10902104     Source Type: Journal    
DOI: 10.1016/j.bbrc.2010.10.015     Document Type: Article

References (22)

1. DeFronzo R.A., Bonadonna R.C., Ferrannini E. Pathogenesis of NIDDM. A balanced overview. Diabetes Care 1999, 15:318-368.
2. Taylor S.I., Accili D., Imai Y. Insulin resistance or insulin deficiency. Which is the primary cause of NIDDM?. Diabetes 1994, 43:735-740.
3. Meece J. Pancreatic islet dysfunction in type 2 diabetes: a rational target for incretin-based therapies. Curr. Med. Res. Opin. 2007, 23:933-944.
4. Seino Y., Rasmussen M.F., Nishida T., Kaku K. Efficacy and safety of the once-daily human GLP-1 analogue, liraglutide, vs glibenclamide monotherapy in Japanese patients with type 2 diabetes. Curr. Med. Res. Opin. 2010, 26:1013-1022.
5. Nauck M.A., Vilsbøll T., Gallwitz B., Garber A., Madsbad S. Incretin-based therapies: viewpoints on the way to consensus. Diabetes Care 2009, 32 Suppl 2:S223-S231.
6. Ahrén B. Emerging dipeptidyl peptidase-4 inhibitors for the treatment of diabetes. Expert. Opin. Emerg. Drugs 2008, 13:593-607.
7. Doupis J., Veves A. DPP4 inhibitors: a new approach in diabetes treatment. Adv. Ther. 2008, 25:627-643.
8. Chia C.W., Egan J.M. Incretin-based therapies in type 2 diabetes mellitus. J. Clin. Endocrinol. Metab. 2008, 93:3703-3716.
9. Soga T., Ohishi T., Matsui T., Saito T., Matsumoto M., Takasaki J., Matsumoto S., Kamohara M., Hiyama H., Yoshida S., Momose K., Ueda Y., Matsushime H., Kobori M., Furuichi K. Lysophosphatidylcholine enhances glucose-dependent insulin secretion via an orphan G-protein-coupled receptor. Biochem. Biophys. Res. Commun. 2005, 28:744-751.
10. Sakamoto Y., Inoue H., Kawakami S., Miyawaki K., Miyamoto T., Mizuta K., Itakura M. 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. 2006, 351:474-480.
11. Overton H.A., Babbs A.J., Doel S.M., Fyfe M.C., Gardner L.S., Griffin G., Jackson H.C., Procter M.J., Rasamison C.M., Tang-Christensen M., Widdowson P.S., Williams G.M., Reynet C. Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents. Cell. Metab. 2006, 3:167-175.
12. Chu Z.L., Jones R.M., He H., et al. A role for beta-cell-expressed G protein-coupled receptor 119 in glycemic control by enhancing glucose-dependent insulin release. Endocrinology 2007, 148:2601-2609.
13. Chu Z.L., Jones R.M., He H., Carroll C., Gutierrez V., Lucman A., Moloney M., Gao H., Mondala H., Bagnol D., Unett D., Liang Y., Demarest K., Semple G., Behan D.P., Leonard J. A role for intestinal endocrine cell-expressed GPR119 in glycemic control by enhancing GLP-1 and GIP release. Endocrinology 2008, 149:2038-2047.
14. Jones R.M., Leonard J.N., Buzard D.J., Lehmann J. GPR119 agonists for the treatment of type 2 diabetes. Expert. Opin. Ther. Pat. 2009, 19:1339-1359.
15. Yoshida S., Ohishi T., Matsui T., Shibasaki M. Identification of a novel GPR119 agonist, AS1269574, With in vitro and in vivo glucose-stimulated insulin secretion. Biochem. Biophys. Res. Commun. 2010, 400:437-441.
16. Wollheim C.B., Meda P., Halban P.A. Isolation of pancreatic islets and primary culture of the intact microorgans or of dispersed islet cells. Methods Enzymol. 1990, 192:188-223.
17. Leiter L.A., Ceriello A., Davidson J.A., Hanefeld M., Monnier L., Owens D.R., Tajima N., Tuomilehto J. Postprandial glucose regulation: new data and new implications. Clin. Ther. 2005, 27 Suppl B:S42-S56.
18. Woerle H.J., Neumann C., Zschau S., Tenner S., Irsigler A., Schirra J., Gerich J.E., Göke B. Impact of fasting and postprandial glycemia on overall glycemic control in type 2 diabetes Importance of postprandial glycemia to achieve target HbA1c levels. Diabetes Res. Clin. Pract. 2007, 77:280-285.
19. Ahrén B. Islet G protein-coupled receptors as potential targets for treatment of type 2 diabetes. Nat. Rev. Drug. Discov. 2009, 8:369-385.
20. Winzell M.S., Ahrén B. G-protein-coupled receptors and islet function-implications for treatment of type 2 diabetes. Pharmacol. Ther. 2007, 116:437-448.
21. Morgan N.G., Dhayal S. G-protein coupled receptors mediating long chain fatty acid signalling in the pancreatic beta-cell. Biochem. Pharmacol. 2009, 78:1419-1427.
22. Shah U. GPR119 agonists: a promising new approach for the treatment of type 2 diabetes and related metabolic disorders. Curr. Opin. Drug Discov. Dev. 2009, 12:519-532.