Antagonism of gastric inhibitory polypeptide (GIP) by palmitoylation of GIP analogues with N- and C-terminal modifications improves obesity and metabolic control in high fat fed mice

Molecular and Cellular Endocrinology

Volumn 401, Issue , 2015, Pages 120-129

  Pathak, V ^a   Gault, V A ^a   Flatt, P R ^a   Irwin, N ^a  

^a UNIVERSITY OF ULSTER   (United Kingdom)

Author keywords

Body weight; Diabetes; GIP; Glucose homeostasis; Insulin secretion; Obesity

Indexed keywords

CYCLIC AMP; DIPEPTIDYL PEPTIDASE IV; GASTRIC INHIBITORY POLYPEPTIDE; GASTRIC INHIBITORY POLYPEPTIDE ANTAGONIST; GLUCOSE; INSULIN; PEPTIDE HORMONE ANTAGONIST; SODIUM CHLORIDE; UNCLASSIFIED DRUG; ANTIOBESITY AGENT; GLUCOSE BLOOD LEVEL;

AMINO ACID SEQUENCE; AMINO TERMINAL SEQUENCE; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CALORIC INTAKE; CARBOXY TERMINAL SEQUENCE; CONTROLLED STUDY; DIABETES MELLITUS; ENZYME DEGRADATION; GLUCOSE BLOOD LEVEL; GLUCOSE TOLERANCE TEST; GLYCEMIC CONTROL; IN VITRO STUDY; INHIBITION KINETICS; INSULIN BLOOD LEVEL; INSULIN RELEASE; INSULIN SENSITIVITY; INTRAPERITONEAL GLUCOSE TOLERANCE TEST; LIPID DIET; LOCOMOTION; MALE; METABOLIC RATE; METABOLIC REGULATION; MOUSE; NONHUMAN; OBESITY; ORAL GLUCOSE TOLERANCE TEST; PALMITOYLATION; PROTEIN MODIFICATION; TREATMENT OUTCOME; WEIGHT REDUCTION; ADVERSE EFFECTS; ANALOGS AND DERIVATIVES; ANIMAL; ANTAGONISTS AND INHIBITORS; BLOOD; BODY WEIGHT; CHEMICALLY INDUCED; CHEMISTRY; DRUG ADMINISTRATION; DRUG EFFECTS; INTRAPERITONEAL DRUG ADMINISTRATION; LIPOYLATION; METABOLISM; ORAL DRUG ADMINISTRATION;

ADMINISTRATION, ORAL; ANIMALS; ANTI-OBESITY AGENTS; BLOOD GLUCOSE; BODY WEIGHT; DIET, HIGH-FAT; DRUG ADMINISTRATION SCHEDULE; GASTRIC INHIBITORY POLYPEPTIDE; GLUCOSE TOLERANCE TEST; INJECTIONS, INTRAPERITONEAL; INSULIN; LIPOYLATION; MICE; OBESITY;

EID: 84919941543     PISSN: 03037207     EISSN: 18728057     Source Type: Journal    
DOI: 10.1016/j.mce.2014.10.025     Document Type: Article

References (36)

1. Bailey C.J., Flatt P.R., Kwasowski P., Powell C.J., Marks V. Immunoreactive gastric inhibitory polypeptide and K cell hyperplasia in obese hyperglycaemic (ob/ob) mice fed high fat and high carbohydrate cafeteria diets. Acta Endocrinol. (Copenh.) 1986, 112:224-229.
2. Brown J.C. Enteroinsular axis. Gut Peptides: Biochemistry and Physiology 1994, 765-784. Raven Press, New York. G.J. Dockray, J.H. Walsh (Eds.).
3. Christensen M., Hansen L.S., Rosenkilde M.M., Holst J.J., Knop F.P. A reappraisal of antagonists for the human glucose-dependent insulinotropic polypeptide (GIP) receptor. Diabetes 2012, 61(S1):A482.
4. Deacon C.F., Plamboeck A., Rosenkilde M.M., De Heer J., Holst J.J. GIP 3-42 does not antagonize the insulinotropic effects of GIP at physiological concentrations. Am. J. Physiol 2006, 291:E468-E475.
5. Doig A.J., Baldwin R.L. N- and C-capping preferences for all 20 amino acids in alpha-helical peptides. Protein Sci 1995, 4:1325-1336.
6. Drucker D.J. The role of gut hormones in glucose homeostasis. J. Clin. Invest 2007, 117:24-32.
7. Flatt P.R., Bailey C.J. Abnormal plasma glucose and insulin responses in heterozygous (ob/+) mice. Diabetologia 1981, 20:573-577.
8. Flatt P.R., Bailey C.J., Kwasowski P., Swanston-Flatt S.K., Marks V. Abnormalities of GIP in spontaneous syndromes of obesity and diabetes in mice. Diabetes 1983, 32:433-435.
9. Flatt P.R., Bailey C.J., Kwasowski P., Swanston-Flatt S.K. Effects of diets rich in sucrose, coconut fat and safflower seed oil on the development of the obese hyperglycaemic (ob/ob) syndrome in mice. Diabetes Res 1990, 13:23-28.
10. Fulurija A., Lutz T.A., Sladko K., Osto M., Wielinga P.Y., Bachmann M.F., et al. Vaccination against GIP for the treatment of obesity. PLoS ONE 2008, 3:e3163.
11. Gault V.A., Flatt P.R., O'Harte F.P.M. Glucose-dependent insulinotropic polypeptide (GIP): anti-diabetic and anti-obesity potential. Neuropeptides 2003, 37:253-263.
12. 3)GIP antagonist and exendin(9-39)amide on GIP- and GLP-1-induced cyclic AMP generation, insulin secretion and postprandial insulin release in obese diabetic (ob/ob) mice: evidence that GIP is the major physiological incretin. Diabetologia 2003, 46:222-230.
13. 3)GIP administration improves glucose tolerance and ameliorates insulin resistance and abnormalities of islet structure in obesity-related diabetes. Diabetes 2005, 54:2436-2446.
14. Gault V.A., McClean P.L., Cassidy R.S., Irwin N., Flatt P.R. Chemical gastric inhibitory polypeptide receptor antagonism protects against obesity, insulin resistance, glucose intolerance and associated disturbances in mice fed high-fat and cafeteria diet. Diabetologia 2007, 50:1752-1762.
15. Gault V.A., Hunter K., Irwin N., Greer B., Green B.D., Harriott P., et al. Characterisation and glucoregulatory actions of a novel acylated form of the (Pro3)GIP receptor antagonist in type 2 diabetes. Biol. Chem 2007, 388:173-179.
16. Gault V.A., Porter D.W., Irwin N., Flatt P.R. 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.
17. Irwin N., Flatt P.R. Evidence for beneficial effects of compromised gastric inhibitory polypeptide action in obesity-related diabetes and possible therapeutic implications. Diabetologia 2009, 52:1724-1731.
18. Irwin N., Flatt P.R. Enteroendocrine hormone mimetics for the treatment of obesity and diabetes. Curr. Opin. Pharmacol 2013, 13:989-995.
19. 3)GIP prevents the development of diabetes and related metabolic abnormalities associated with genetically inherited obesity in ob/ob mice. Diabetologia 2007, 50:1532-1540.
20. Irwin N., McClean P.L., Patterson S., Hunter K., Flatt P.R. Active immunisation against gastric inhibitory polypeptide (GIP) improves blood glucose control in an animal model of obesity-diabetes. Biol. Chem 2009, 390:75-80.
21. Irwin N., Gault V., Flatt P.R. Therapeutic potential of the original incretin hormone glucose-dependent insulinotropic polypeptide: diabetes, obesity, osteoporosis and Alzheimer's disease?. Expert Opin. Investig. Drugs 2010, 9:1039-1048.
22. Kerr B.D., Flatt A.J., Flatt P.R., Gault V.A. Characterization and biological actions of N-terminal truncated forms of glucose-dependent insulinotropic polypeptide. Biochem. Biophys. Res. Commun 2011, 404:870-876.
23. Mabilleau G., Mieczkowska A., Irwin N., Simon Y., Audran M., Flatt P.R., et al. Beneficial effects of a N-terminally modified GIP agonist on tissue-level bone material properties. Bone 2014, 63:61-68.
24. McClean P.L., Irwin N., Cassidy R.S., Holst J.J., Gault V.A., Flatt P.R. GIP receptor antagonism reverses obesity, insulin resistance, and associated metabolic disturbances induced in mice by prolonged consumption of high-fat diet. Am. J. Physiol. Endocrinol. Metab 2007, 293:E1746-E1755.
25. 3)GIP[mPEG]: novel, long-acting, mPEGylated antagonist of gastric inhibitory polypeptide for obesity-diabetes (diabesity) therapy. Br. J. Pharmacol 2008, 155:690-701.
26. McClenaghan N.H., Barnett C.R., O'Harte F.P., Flatt P.R. Mechanisms of amino acid-induced insulin secretion from the glucose-responsive BRIN-BD11 pancreatic B-cell line. J. Endocrinol 1996, 151:349-357.
27. Miyawaki K., Yamada Y., Ban N., Ihara Y., Tsukiyama K., Zhou H., et al. Inhibition of gastric inhibitory polypeptide signaling prevents obesity. Nat. Med 2002, 8:738-742.
28. Naitoh R., Miyawaki K., Harada N., Mizunoya W., Toyoda K., Fushiki T., et al. Inhibition of GIP signaling modulates adiponectin levels under high-fat diet in mice. Biochem. Biophys. Res. Commun 2008, 376:21-25.
29. Nasteska D., Harada N., Suzuki K., Yamane S., Hamasaki A., Joo E., et al. Chronic reduction of GIP secretion alleviates obesity and insulin resistance under high fat diet condition. Diabetes 2014, 63:2332-2343.
30. Ponter A.A., Salter D.N., Morgan L.M., Flatt P.R. The effect of energy source and feeding level on the hormones of the entero-insular axis and plasma glucose in the growing pig. Br. J. Nutr 1991, 66:187-197.
31. Porter D.W., Irwin N., Flatt P.R., Hölscher C., Gault V.A. Prolonged GIP receptor activation improves cognitive function, hippocampal synaptic plasticity and glucose homeostasis in high-fat fed mice. Eur. J. Pharmacol 2011, 15:688-693.
32. Simonsen L., Holst J.J., Madsen K., Deacon C.F. The C-terminal extension of exendin 4 provides additional metabolic stability when added to GLP-1, while there is minimal effect of truncating exendin-4 in anaesthetized pigs. Regul. Pept 2013, 10:17-21.
33. Tartarkiewicz K., Hargrove D.M., Jodka C.M., Gedulin B.R., Smith P.A., Hoyt J.A., et al. A novel long-acting glucose-dependent insulinotropic peptide analogue: enhanced efficacy in normal and diabetic rodents. Diabetes Obes. Metab 2014, 16:75-85.
34. Tschöp M.T., DiMarchi R.D. Outstanding Scientific Achievement Award Lecture 2011: defeating diabesity. The case for personalized combinatorial therapies. Diabetes 2012, 61:1309-1314.
35. Woods S.C., West D.B., Stein L.J., McKay L.D., Lotter E.C., Porte S.G., et al. Peptides and the control of meal size. Diabetologia 1981, 20:305-313.
36. Zhou H., Yamada Y., Tsukiyama K., Miyawaki K., Hosokawa M., Nagashima K., et al. Gastric inhibitory polypeptide modulates adiposity and fat oxidation under diminished insulin action. Biochem. Biophys. Res. Commun 2005, 335:937-942.