1,450
Views
131
CrossRef citations to date
0
Altmetric
Reviews

GPR119 agonists for the treatment of type 2 diabetes

, , &
Pages 1339-1359 | Published online: 28 Sep 2009

Bibliography

  • Stumvoll M, Goldstein BJ, van Haeften TW. Type 2 diabetes: principles of pathogenesis and therapy. Lancet 2005;365(9467):1333-46
  • Prokopenko I, McCarthy MI, Lindgren CM. Type 2 diabetes: new genes, new understanding. Trends Genet 2008;24:613-21
  • Diabetes report: developments and opportunities in drugs and devices. BioWorld and Medical Device Daily; 2008
  • Wild S, Roglic G, Green A, et al. Global prevalence of diabetes: estimates for the year 2000 and projections for 2030. Diabetes Care 2004;27:1047-53
  • Felber JP, Golay A. Pathways from obesity to diabetes. Int J Obes Relat Metab Disord 2002;26:S39-45
  • Weir GC, Bonner-Weir S. Five stages of evolving beta-cell dysfunction during progression to diabetes. Diabetes 2004;53:S16-21
  • Weyer C, Bogardus C, Mott DM, Pratley RE. The natural history of insulin secretory dysfunction and insulin resistance in the pathogenesis of type 2 diabetes mellitus. J Clin Invest 1999;104:787-94
  • Jarrett RJ. Epidemiology and public health aspects of non-insulin-dependent diabetes mellitus. Epidemiol Rev 1989;11:151-71
  • Davis MD. Diabetic retinopathy. A clinical overview. Diabetes Care 1992;15:1844-74
  • Ritz E, Orth SR. Nephropathy in patients with type 2 diabetes mellitus. N Engl J Med 1999;341:1127-33
  • Haffner SM, Lehto S, Rönnemaa T, et al. Mortality from coronary heart disease in subjects with type 2 diabetes and in nondiabetic subjects with and without prior myocardial infarction. N Engl J Med 1998;339:229-34
  • American Diabetes Association; Standards of Medical Care in Diabetes – 2009. Diabetes Care 2009;32(S1):S13-61
  • Cefalu WT. Pharmacotherapy for the treatment of patients with type 2 diabetes mellitus: rationale and specific agents. Clin Pharmacol Ther 2007;81:636-49
  • UK Prospective Diabetes Study (UKPDS) Group. Effect of intensive blood-glucose control with metformin on complications in overweight patients with type 2 diabetes (UKPDS 34). Lancet 1998;352:854-65
  • Agius L. New hepatic targets for glycaemic control in diabetes. Best Pract Res Clin Endocrinol Metab 2007;21:587-605
  • Dunning BE, Gerich JE. The role of alpha-cell dysregulation in fasting and postprandial hyperglycemia in type 2 diabetes and therapeutic implications. Endocr Rev 2007;28:253-83
  • Erion MD, van Poelje PD, Dang Q, et al. MB06322 (CS-917): a potent and selective inhibitor of fructose 1,6-bisphosphatase for controlling gluconeogenesis in type 2 diabetes. Proc Natl Acad Sci USA 2005;102:7970-5
  • Koren S, Fantus IG. Inhibition of the protein tyrosine phosphatase PTP1B: Potential Therapy for Obesity, Insulin Resistance and Type-2 Diabetes Mellitus. Best Pract Res Clin Endocrinol Metab 2007;21:621-40
  • Tomlinson JW, Peterson PM. Modulation of glucocorticoid action and the treatment of type-2 diabetes. Best Pract Res Clin Endocrinol Metab 2007;21:607-19
  • Foster-Schubert KE, Cummings DE. Emerging therapeutic strategies for obesity. Endocr Rev 2006;27(7):779-93
  • Han S, Hagan DL, Taylor JR, et al. Dapagliflozin, a selective SGLT2 inhibitor, improves glucose homeostasis in normal and diabetic rats. Diabetes 2008;57:1723-9
  • Drucker DJ, Nauck MA. The Incretin System: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes. Lancet 2006;368:1696-705
  • Baggio LL, Drucker DJ. Biology of incretins: GLP-1 and GIP. Gastroenterology 2007;132:2131-57
  • Habener JF. The incretin notion and its relevance to diabetes. Endocrinol Clin Metab North Am 1993;22:775-94
  • Leech CA, Holz GG, Habener JF. Signal transduction of PACAP and GLP-1 in pancreatic beta cells. Ann NY Acad Sci 1996;805:81-92
  • Fehmann HC, Habener JF. Insulinotropic hormone glucagon-like peptide-I(7-37) stimulation of proinsulin gene expression and proinsulin biosynthesis in insulinoma beta TC-1 cells. Endocrinology 1992;130:159-66
  • Fehmann HC, Göke B. Characterization of GIP(1-30) and GIP(1-42) as stimulators of proinsulin gene transcription. Peptides 1995;16:1149-52
  • Nauck MA, Heimesaat MM, Behle K, et al. Effects of glucagon-like peptide 1 on counterregulatory hormone responses, cognitive functions, and insulin secretion during hyperinsulinemic, stepped hypoglycemic clamp experiments in healthy volunteers. J Clin Endocrinol Metab 2002;87:1239-46
  • Wettergren A, Schjoldager B, Mortensen PE, et al. Truncated GLP-1 (proglucagon 78-107-amide) inhibits gastric and pancreatic functions in man. Dig Dis Sci 1993;38:665-73
  • Turton MD, O'Shea D, Gunn I, et al. A role for glucagon-like peptide-1 in the central regulation of feeding. Nature 1996;379(6560):69-72
  • Balkan B, Li X. Portal GLP-1 administration in rats augments the insulin response to glucose via neuronal mechanisms. Am J Physiol Regul Integr Comp Physiol 2000;279:R1449-54
  • Deacon CF, Nauck MA, Toft-Nielsen M, et al. Both subcutaneously and intravenously administered glucagon-like peptide I are rapidly degraded from the NH2-terminus in type II diabetic patients and in healthy subjects. Diabetes 1995;44:1126-31
  • Matthews DR, Cull CA, Stratton IM, et al. UKPDS 26: Sulphonylurea failure in non-insulin-dependent diabetic patients over six years. UK Prospective Diabetes Study (UKPDS) Group. Diabet Med 1998;15:297-303
  • Goldstein BJ, Feinglos MN, Lunceford JK, et al.; Sitagliptin 036 Study Group. Effect of initial combination therapy with sitagliptin, a dipeptidyl peptidase-4 inhibitor, and metformin on glycemic control in patients with type 2 diabetes. Diabetes Care 2007;30:1979-87
  • Madiraju SR, Poitout V. G protein-coupled receptors and insulin secretion: 119 and counting. Endocrinology 2007;148:2598-600
  • Fyfe MC, Overton HA, Procter MJ, et al. Chapter 9 new nonpeptide-binding GPCRs as targets for diabetes and the metabolic syndrome. p. 129-45
  • Lauffer L, Iakoubov R, Brubaker PL. GPR119: “double-dipping” for better glycemic control. Endocrinology 2008;149:2035-7
  • Engelstoft MS, Egerod KL, Holst B, Schwartz TW. A gut feeling for obesity: 7TM sensors on enteroendocrine cells. Cell Metab 2008;8:447-9
  • Fyfe MC, McCormack JG, Overton HA, et al. GPR119 agonists as potential new oral agents for the treatment of type 2 diabetes and obesity. Expert Opin Drug Discov 2008;3:403-13
  • Overton HA, Fyfe MC, Reynet C. GPR119, a novel G protein-coupled receptor target for the treatment of type 2 diabetes and obesity. Br J Pharmacol 2008;153(Suppl 1):S76-81
  • Fredriksson R, Hoglund PJ, Gloriam DEI, et al. Seven Evolutionarily Conserved Human Rhodopsin G Protein-Coupled Receptors Lacking Close Relatives. FEBS Lett 2003;554:381-8
  • Soga T, Ohishi T, Matsui T, et al. Lysophosphatidylcholine enhances glucose-dependent insulin secretion via an orphan G-protein-coupled receptor. Biochem Biophys Res Commun 2005;326:744-51
  • Chu Z, Carroll C, Alfonso J, et al. A role for intestinal endocrine cell-expressed GPR119 in glycemic control by enhancing GLP-1 and GIP release. Endocrinology 2008;149:2038-47
  • Leonard J, Chu ZL, Jones RM, et al. Arena Pharmaceuticals unpublished data
  • Chu Z, Jones RM, He H, et al. A role for β-cell-expressed G protein-coupled receptor 119 in glycemic control by enhancing glucose-dependent insulin release. Endocrinology 2007;148:2601-9
  • Sakamoto Y, Inoue H, Kawakami S, et al. 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;351:474-80
  • Demarest K, Liang Y, Leonard J, et al. Improvement of Blood Glucose Control in Rats and Cynomologous Monkeys by Enhancing Glucose-Stimulated Insulin and GLP-1 Release with a GDIR Agonist. American Diabetes Association – 69th Meeting, New Orleans; 2009
  • Roberts B, Gregoire FM, Karpf DB, et al. MBX-2982, a Novel Oral GPR119 Agonist for the Treatment of Type 2 Diabetes: Results of Single & Multiple Dose Studies. American Diabetes Association – 69th Meeting, New Orleans; 2009
  • James N. Leonard. GPR119 Ligands Regulate Glucose Homeostasis by Multiple Cell-Based Mechanisms. ADA meeting, San Francisco; 2008
  • Arena Pharmaceuticals. Combination Therapy for the Treatment of Diabetes and Conditions related thereto and for the treatment of conditions ameliorated by increasing a blood GLP1 level. WO2006076231; 2006
  • Semple G, Fioravanti B, Pereira G, et al. Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119. J Med Chem 2008;51:5172-5
  • Yamanouchi Pharmaceutical Co. Ltd. Method of screening insulin content enhancer. WO04024943; 2004
  • Yamanouchi Pharmaceutical Co. Ltd. Insulin secretion accelerator and novel pyrimidine derivative. WO03026661; 2003
  • Yamanouchi Pharmaceutical Co. Ltd. (Pyrimidinylamino)propanediols or their salts and pharmaceutical compositions containing them as insulin secretion promoters. JP04269468; 2004
  • Yamanouchi Pharmaceutical Co. Ltd. Aminopyrimidines or their salts and pharmaceutical compositions containing them as insulin secretion promoters. JP04269469; 2004
  • Astellas Pharma, Inc. Aromatic-ring-fused pyrimidine derivative. WO06040966; 2006
  • Astellas Pharma, Inc. Pyrimidine derivative fused with nonaromatic ring. WO06043490; 2006
  • Arena Pharmaceuticals Announces Global Diabetes Collaboration with Ortho-McNeil Pharmaceutical Dec 21, 2004. Arena Pharmaceuticals Announces Selection of Two Arena-Discovered Compounds for Preclinical Development by Ortho-McNeil Dec 23, 2004. Arena Pharmaceuticals, Inc. Announces Initiation of Phase 1 Clinical Trial of Arena Type 2 Diabetes Drug Candidate in Collaboration With Ortho-McNeil Feb 7, 2006. Arena Pharmaceuticals Announces That Ortho-McNeil Extends Research Term Under Partnership to Develop Drugs to Treat Type 2 Diabetes Sep 27, 2006
  • Arena Pharmaceuticals Announces APD668 Initial Clinical Study Results Suggest Glucose-Dependent Insulinotropic Receptors May Improve Glucose Control in Patients With Type 2 Diabetes Jan 7, 2008
  • Arena Pharmaceuticals Announces Initiation of Phase 1 Clinical Trial of Type 2 Diabetes Drug Candidate in Partnership with Ortho-McNeil-Janssen Pharmaceuticals Dec 15, 2008
  • Arena Pharmaceuticals, Inc. 1,2,3-Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia. WO04065380; 2004
  • Arena Pharmaceuticals, Inc. Substituted aryl and heteroaryl derivatives as modulators of glucose metabolism and the prophylaxis and treatment of disorders thereof. WO04076413; 2004
  • Arena Pharmaceuticals, Inc. Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto. WO05007647; 2005
  • Arena Pharmaceuticals, Inc. Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto. WO05007658; 2005
  • Arena Pharmaceuticals, Inc. Substituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto. WO05121121; 2005
  • Arena Pharmaceuticals, Inc. Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto. WO06083491; 2006
  • Arena Pharmaceuticals, Inc. Modulators of metabolism and the treatment of disorders related thereto. WO07035355; 2007
  • Arena Pharmaceuticals, Inc. GPR119 receptor agonists in methods of increasing bone mass and of treating osteoporosis and other conditions characterized by low bone mass, and combination therapy relating thereto. WO07120702; 2007
  • Tsukiyama K, Yamada Y, Yamada C, et al. Gastric inhibitory polypeptide as an endogenous factor promoting new bone formation following food ingestion. Mol Endocrinol 2006;20:1644-51
  • Xie D, Cheng H, Hamrick M, et al. Glucose-dependent insulinotropic polypeptide receptor knockout mice have altered bone turnover. Bone 2005;37:759-69
  • Arena Pharmaceuticals, Inc. Modulators of metabolism and the treatment of disorders related thereto. WO08005576; 2008
  • Arena Pharmaceuticals, Inc. Modulators of metabolism and the treatment of disorders related thereto. WO08005569; 2008
  • Prosidion Ltd. Heterocyclic derivatives as GPCR receptor agonists. WO05061489; 2005
  • Prosidion Ltd. G-Protein coupled receptor (GPR1 16) agonists and use thereof for treating obesity and diabetes. WO06067531; 2006
  • Prosidion Ltd. G-Protein coupled receptor agonists. WO06067532; 2006
  • Prosidion Ltd. Pyrimidine derivatives as GPCR agonists. WO06070208; 2006
  • Prosidion Ltd. GPCR agonists. WO07003960; 2007
  • Prosidion Ltd. GPCR agonists. WO07003962; 2007
  • Prosidion Ltd. GPCR agonists. WO07003961; 2007
  • Prosidion Ltd. G-Protein coupled receptor agonists. WO07003964; 2007
  • Prosidion Ltd. Heterocyclic GPCR agonists. WO07116229; 2007
  • Prosidion Ltd. Azetidine derivatives as G-protein coupled receptor (GPR119) agonists. WO07116230; 2007
  • Prosidion Ltd. Piperidine GPCR agonists. WO08081204; 2008
  • Prosidion Ltd. Piperidine GPCR agonists. WO08081205; 2008
  • Prosidion Ltd. Piperidine GPCR agonists. WO08081206; 2008
  • Prosidion Ltd. Piperidine GPCR agonists. WO08081207; 2008
  • Prosidion Ltd. Piperidine GPCR agonists. WO08081208; 2008
  • Overton HA, Babbs AJ, Doel SM, et al. Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents. Cell Metab 2006;3:167-75
  • Smithkline Beecham Co. Chemical Compounds. WO0800887; 2008
  • Smithkline Beecham Co. GPR119 agonists for treatment of diabetes and related disorders. WO08008895; 2008
  • Smithkline Beecham Co. Chemical compounds and uses. WO08070692; 2008
  • Biovitrum Ab. Pyridine compounds for treating GPR119 related disorders. WO08025798; 2008
  • Biovitrum Ab. Pyridazine compounds for treating GPR119 related disorders WO08025799; 2008
  • Biovitrum Ab. Pyrimidine compounds for treating GPR119 related disorders WO08025800; 2008
  • Merck & Co., Inc. Acyl biperidinyl compounds, compositions containing such compounds and methods of treatment. WO08076243; 2008
  • Merck & Co., Inc. Pipiperininyl compounds, compositions containing such compounds and methods of treatment. WO08085316; 2008
  • Gabriel D, Vernier M, Pfeifer MJ, et al. High throughput screening technologies for direct cyclic AMP measurement. Assay Drug Dev Technol 2003;1:291-303
  • Metabolex, Inc. Heterocyclic receptor agonists for treatment of diabetes and metabolic disorders. WO08083238; 2008
  • Metabolex. N-Linked Heterocyclic Receptor Agonists for the Treatment of Diabetes and Metabolic Disorders. WO09014910; 2009
  • IRM LLC. Compounds and compositions as modulators of GPR119 activity. WO08097428; 2008
  • IRM LLC. Compounds and compositions as modulators of GPR119 activity. WO08109702; 2008
  • Schering Corporation. Spiro-condensed azetidine derivatives useful in treating pain, diabetes and disorders of lipid metabolism. WO08033456; 2008
  • Schering Corporation. Azetidinone derivatives and methods of use thereof. WO08033464; 2008
  • Schering Corporation. Pyrimidinone derivatives and methods of use thereof. WO08130584; 2008
  • Schering Corporation. Pyrimidinone derivatives and methods of use thereof. WO08130581; 2008
  • Bristol-Myers Squibb Company. [6,5]-Bicyclic GPR119 protein-coupled receptor agonists. WO08137436; 2008
  • Bristol-Myers Squibb Company. [6,6] and [6,7]-Bicyclic GPR119 protein-coupled receptor agonists. WO08137435; 2008
  • Bristol-Myers Squibb Company. Method for Modulating GPR119 and selected compounds. WO09012277; 2009
  • Bayer-Aktiengesellschaft. Regulation of Human Dopamine-Like G Protein-Coupled Receptor. WO0187929A2; 2001
  • Takeda S, Kadowakic S, Haga T, et al. Identification of G protein-coupled receptor genes from the human genome sequence. FEBS Lett 2002;520:97-101
  • Pfizer Limited. G-Protein Receptor. EP1092727A2; 2001
  • Synaptic Pharmaceutical Corp. DNA Encoding SNORF25 Receptor. WO200050562; 2000
  • Prosidion Ltd. Methods for identification of modulators of OSGPR116 activity. US7083933; 2006
  • Opposition to the Grant of Australian Patent Application No. 30035/00 (Acceptance No. 777247) in the name of Lundbeck A/S: DNA encoding a SNORF25 Receptor; First Statutory Declaration by James N. Leonard; November 2, 2005
  • Lauffer LM, Iaboukov R, Brubaker PL. GPR119 is essential for oleoylethanolamide-induced glucagon-like peptide-1 secretion from the intestinal enteroendocrine L-cell. Diabetes 2009;58:1058-66
  • Fu J, Astarita G, Gaetani S, et al. Food intake regulates oleoylethanolamide formation and degradation in the proximal small intestine. J Biol Chem 2007;282:1518-28
  • Lan H, Vassileva G, Corona A, et al. GPR119 is required for physiological regulation of glucagon-like peptide-1 secretion but not for metabolic homeostasis. J Endocrinol 2009;201:219-30
  • Ammala C, Bullard S, Kashatus J, et al. GPR119 dependent hormone secretion: insulin, GLP-1 and more. Islet and β-cell biology, Keystone Symposium; 2008
  • Batterham RL, Cowley MA, Small CJ, et al. Gut hormone PYY(3-36) physiologically inhibits food intake. Nature 2002;418:650-4
  • Lovshin JA, Drucker DJ. Incretin-based therapies for type 2 diabetes mellitus. Nat Rev Endocrinol 2009;5:262-9
  • Ning Y, O'Neill K, Lan H, et al. Endogenous and synthetic agonists of GPR119 differ in signalling pathways and their effects on insulin secretion in MIN6c4 insulinoma cells. Br J Pharmacol 2008;155(7):1056-65
  • Arena Pharmaceuticals Unpublished Data.
  • Rubino F, Gagner M, Gentileschi P, et al. The early effect of the Roux-en-Y gastric bypass on hormones involved in body weight regulation and glucose metabolism. Ann Surg 2004;240(2):236-42
  • Laferrere B, Heshka S, Wang K, et al. Incretin levels and effect are markedly enhanced 1 month after roux-en-Y gastric bypass surgery in obese patients with type 2 diabetes. Diabetes Care 2007;30:1709-16
  • Piteau S, Olver A, Kim S, et al. Reversal of islet GIP receptor down-regulation and resistance to GIP by reducing hyperglycemia in the Zucker rat. Biochem Biophys Res Commun 2007;362(4):1007-12
  • OSI Pharmaceuticals Provides Update on Diabetes and Obesity Clinical Programs. Press Release May 11, 2009

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.