A novel long-acting glucose-dependent insulinotropic peptide analogue: Enhanced efficacy in normal and diabetic rodents

Diabetes, Obesity and Metabolism

Volumn 16, Issue 1, 2014, Pages 75-85

  Tatarkiewicz, K ^a   Hargrove, D M ^a   Jodka, C M ^a   Gedulin, B R ^a   Smith, P A ^a   Hoyt, J A ^a   Lwin, A ^a   Collins, L ^a   Mamedova, L ^a   Levy, O E ^a   D'Souza, L ^a   Janssen, S ^a   Srivastava, V ^a   Ghosh, S S ^a   Parkes, D G ^a  

^a AMYLIN PHARMACEUTICALS INC   (United States)

Author keywords

Diabetes; DPP IV resistant; GIP; Rodents; Trp cage

Indexed keywords

AC 163794; AC 3174; AMINO ACID; ANTIDIABETIC AGENT; DIPEPTIDYL PEPTIDASE IV; EXENDIN 4; GASTRIC INHIBITORY POLYPEPTIDE; STREPTOZOCIN; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTIDIABETIC ACTIVITY; ARTICLE; BIOLOGICAL ACTIVITY; CARBOXY TERMINAL SEQUENCE; CONTINUOUS INFUSION; CONTROLLED STUDY; DRUG BINDING; DRUG BLOOD LEVEL; DRUG DETERMINATION; DRUG POTENCY; INSULIN LIKE ACTIVITY; MOUSE; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; PEPTIDE SYNTHESIS; RAT; ZUCKER DIABETIC FATTY RAT;

DIABETES; DPP-IV RESISTANT; GIP; RODENTS; TRP-CAGE;

ANIMALS; BLOOD GLUCOSE; CHEMISTRY, PHARMACEUTICAL; DIABETES MELLITUS, EXPERIMENTAL; FEMALE; GASTRIC INHIBITORY POLYPEPTIDE; HYPOGLYCEMIC AGENTS; INCRETINS; MALE; MICE; MICE, OBESE; OBESITY; RATS; RATS, SPRAGUE-DAWLEY; RATS, ZUCKER;

EID: 84890562831     PISSN: 14628902     EISSN: 14631326     Source Type: Journal    
DOI: 10.1111/dom.12181     Document Type: Article

References (39)

1. Elliott RM, Morgan LM, Tredger JA, Deacon S, Wright J, Marks V. Glucagon-like peptide-1 (7-36)amide and glucose-dependent insulinotropic polypeptide secretion in response to nutrient ingestion in man: acute post-prandial and 24-h secretion patterns. J Endocrinol 1993; 138: 159-166.
2. Jorde R, Burhol PG, Waldum HL, Schulz TB, Lygren I, Florholmen J. Diurnal variation of plasma gastric inhibitory polypeptide in man. Scand J Gastroenterol 1980; 15: 617-619.
3. Dupre J, Ross SA, Watson D, Brown JC. Stimulation of insulin secretion by gastric inhibitory polypeptide in man. J Clin Endocrinol Metabol 1973; 37: 826-828.
4. Pederson RA, Schubert HE, Brown JC. Gastric inhibitory polypeptide. Its physiologic release and insulinotropic action in the dog. Diabetes 1975; 24: 1050-1056.
5. Andersen DK, Elahi D, Brown JC, Tobin JD, Andres R. Oral glucose augmentation of insulin secretion. Interactions of gastric inhibitory polypeptide with ambient glucose and insulin levels. J Clin Invest 1978; 62: 152-161.
6. Ehses JA, Casilla VR, Doty T et al. Glucose-dependent insulinotropic polypeptide promotes β-(INS-1) cell survival via cyclic adenosine monophosphate-mediated caspase-3 inhibition and regulation of p38 mitogen-activated protein kinase. Endocrinology 2003; 144: 4433-4445.
7. Trümper A, Trümper K, Hörsch D. Mechanisms of mitogenic and anti-apoptotic signaling by glucose-dependent insulinotropic polypeptide in β(INS-1)-cells. J Endocrinol 2002; 174: 233-246.
8. Trümper A, Trümper K, Trusheim H, Arnold R, Göke B, Hörsch D. Glucose-dependent insulinotropic polypeptide is a growth factor for β (INS-1) cells by pleiotropic signaling. Mol Endocrinol 2001; 15: 1559-1570.
9. Kim SJ, Nian C, Widenmaier S, McIntosh CH. Glucose-dependent insulinotropic polypeptide-mediated up-regulation of beta-cell antiapoptotic Bcl-2 gene expression is coordinated by cyclic AMP (cAMP) response element binding protein (CREB) and cAMP-responsive CREB coactivator 2. Mol Cell Biol 2008; 28: 1644-1656.
10. Usdin TB, Mezey E, Button DC, Brownstein MJ, Bonner TI. Gastric inhibitory polypeptide receptor, a member of the secretin-vasoactive intestinal peptide receptor family, is widely distributed in peripheral organs and the brain. Endocrinology 1993; 133: 2861-2870.
11. Yip RG, Boylan MO, Kieffer TJ, Wolfe MM. Functional GIP receptors are present on adipocytes. Endocrinology 1998; 139: 4004-4007.
12. Flatt PR. Dorothy Hodgkin Lecture 2008. Gastric inhibitory polypeptide (GIP) revisited: a new therapeutic target for obesity-diabetes? Diabet Med 2008; 25: 759-764.
13. Nauck MA, Heimesaat MM, Orskov C, Holst JJ, Ebert R, Creutzfeldt W. Preserved incretin activity of glucagon-like peptide 1 [7-36 amide] but not of synthetic human gastric inhibitory polypeptide in patients with type-2 diabetes mellitus. J Clin Invest 1993; 91: 301-307.
14. Mingrone G. Role of the incretin system in the remission of type 2 diabetes following bariatric surgery. Nutr Metab Cardiovasc Dis 2008; 18: 574-579.
15. Hojberg PV, Vilsboll T, Rabol R et al. Four weeks of near-normalisation of blood glucose improves the insulin response to glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide in patients with type 2 diabetes. Diabetologia 2009; 52: 199-207.
16. Aaboe K, Knop FK, Vilsboll T et al. KATP channel closure ameliorates the impaired insulinotropic effect of glucose-dependent insulinotropic polypeptide in patients with type 2 diabetes. J Clin Endocrinol Metab 2009; 94: 603-608.
17. Meneilly GS, Bryer-Ash M, Elahi D. The effect of glyburide on beta-cell sensitivity to glucose-dependent insulinotropic polypeptide. Diabetes Care 1993; 16: 110-114.
18. Gault VA, Kerr BD, Harriott P, Flatt PR. Administration of an acylated GLP-1 and GIP preparation provides added beneficial glucose-lowering and insulinotropic actions over single incretins in mice with Type 2 diabetes and obesity. Clin Sci (Lond) 2011; 121: 107-117.
19. Piteau S, Olver A, Kim SJ 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: 1007-1012.
20. Pospisilik JA, Hinke SA, Pederson RA et al. Metabolism of glucagon by dipeptidyl peptidase IV (CD26). Regul Pept 2001; 96: 133-141.
21. Kieffer TJ, McIntosh CH, Pederson RA. Degradation of glucose-dependent insulinotropic polypeptide and truncated glucagon-like peptide 1 in vitro and in vivo by dipeptidyl peptidase IV. Endocrinology 1995; 136: 3585-3596.
22. Ahren B, Foley JE. The islet enhancer vildagliptin: mechanisms of improved glucose metabolism. Int J Clin Pract Suppl 2008; 159: 8-14.
23. Gault VA, Flatt PR, O'Harte FP. Glucose-dependent insulinotropic polypeptide analogues and their therapeutic potential for the treatment of obesity-diabetes. Biochem Biophys Res Commun 2003; 308: 207-213.
24. Hinke SA, Gelling RW, Pederson RA et al. Dipeptidyl peptidase IV-resistant [d-Ala(2)]glucose-dependent insulinotropic polypeptide (GIP) improves glucose tolerance in normal and obese diabetic rats. Diabetes 2002; 51: 652-661.
25. Alana I, Hewage CM, Malthouse JP, Parker JC, Gault VA, O'Harte FP. NMR structure of the glucose-dependent insulinotropic polypeptide fragment, GIP(1-30)amide. Biochem Biophys Res Commun 2004; 325: 281-286.
26. Gault VA, Porter DW, Irwin N, Flatt PR. Comparison of sub-chronic metabolic effects of stable forms of naturally occurring GIP(1-30) and GIP(1-42) in high-fat fed mice. J Endocrinol 2011; 208: 265-271.
27. Neidigh JW, Fesinmeyer RM, Prickett KS, Andersen NH. Exendin-4 and glucagon-like-peptide-1: NMR structural comparisons in the solution and micelle-associated states. Biochemistry 2001; 40: 13188-13200.
28. Li Y, Xu W, Tang L, Gong M, Zhang J. A novel GLP-1 analog exhibits potent utility in the treatment of type 2 diabetes with an extended half-life and efficient glucose clearance in vivo. Peptides 2011; 32: 1408-1414.
29. Doyle ME, Theodorakis MJ, Holloway HW, Bernier M, Greig NH, Egan JM. The importance of the nine-amino acid C-terminal sequence of exendin-4 for binding to the GLP-1 receptor and for biological activity. Regul Pept 2003; 114: 153-158.
30. Gallwitz B, Witt M, Folsch UR, Creutzfeldt W, Schmidt WE. Binding specificity and signal transduction of receptors for glucagon-like peptide-1(7-36)amide and gastric inhibitory polypeptide on RINm5F insulinoma cells. J Mol Endocrinol 1993; 10: 259-268.
31. Gotoh M, Maki T, Kiyoizumi T, Satomi S, Monaco AP. An improved method for isolation of mouse pancreatic islets. Transplantation 1985; 40: 437-438.
32. Tatarkiewicz K, Garcia M, Omer A, Van Schilfgaarde R, Weir GC, De Vos P. C-peptide responses after meal challenge in mice transplanted with microencapsulated rat islets. Diabetologia 2001; 44: 646-653.
33. Hargrove DM, Kendall ES, Reynolds JM et al. Biological activity of AC3174, a peptide analog of exendin-4. Regul Pept 2007; 141: 113-119.
34. Roth JD, Hughes H, Kendall E, Baron AD, Anderson CM. Anti-obesity effects of the β-cell hormone amylin in diet induced obese rats: effects on food intake, body weight, composition, energy expenditure and gene expression. Endocrinology 2006; 147: 5855-5864.
35. Venneti KC, Malthouse JP, O'Harte FP, Hewage CM. Conformational, receptor interaction and alanine scan studies of glucose-dependent insulinotropic polypeptide. Biochim Biophys Acta 1814; 2011: 882-888.
36. Widenmaier SB, Kim SJ, Yang GK et al. A GIP receptor agonist exhibits beta-cell anti-apoptotic actions in rat models of diabetes resulting in improved beta-cell function and glycemic control. PLoS One 2010; 5: e9590.
37. Irwin N, Flatt PR. Therapeutic potential for GIP receptor agonists and antagonists. Best Pract Res Clin Endocrinol Metab 2009; 23: 499-512.
38. Lynn FC, Pamir N, Ng EH, McIntosh CH, Kieffer TJ, Pederson RA. Defective glucose-dependent insulinotropic polypeptide receptor expression in diabetic fatty Zucker rats. Diabetes 2001; 50: 1004-1011.
39. Martin CM, Irwin N, Flatt PR, Gault VA. A novel acylated form of (d-Ala(2))GIP with improved antidiabetic potential, lacking effect on body fat stores. Biochim Biophys Acta 1830; 2013: 3407-3413.