Glucose-dependent insulinotropic polypeptide analogues and their therapeutic potential for the treatment of obesity-diabetes

Biochemical and Biophysical Research Communications

Volumn 308, Issue 2, 2003, Pages 207-213

  Gault, Victor A ^a   Flatt, Peter R ^a   O'Harte, Finbarr P M ^a  

^a UNIVERSITY OF ULSTER   (United Kingdom)

Author keywords

Dipeptidylpeptidase IV; GIP analogues; Glucagon like peptide 1; Glucose dependent insulinotropic polypeptide; Insulin secretion; Obesity; Type 2 diabetes

Indexed keywords

ALANINE; ANTIDIABETIC AGENT; DIPEPTIDYL PEPTIDASE IV; GASTRIC INHIBITORY POLYPEPTIDE; GLUTAMIC ACID; GLYCINE; PEPTIDE DERIVATIVE; SERINE; TYROSINE; UNCLASSIFIED DRUG;

AMINO ACID SUBSTITUTION; DIABETIC OBESITY; DRUG ACTIVITY; DRUG HALF LIFE; DRUG INDICATION; DRUG POTENCY; DRUG STABILITY; ENZYME ACTIVITY; FEEDING; HORMONE ACTION; HORMONE RELEASE; HUMAN; INSULIN LIKE ACTIVITY; INSULIN RELEASE; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; PRIORITY JOURNAL; PROTEIN DEGRADATION; PROTEIN MODIFICATION; REVIEW; TREATMENT INDICATION;

EID: 0041592594     PISSN: 0006291X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0006-291X(03)01361-5     Document Type: Article

References (60)

1. Brown J.C. Enteroinsular axis. Dockray G.J., Walsh J.H. Gut Peptides: Biochemistry and Physiology. 1994;765-784 Raven Press, New York.
2. Creutzfeldt W. The entero-insular axis in type 2 diabetes - incretins as therapeutic agents. Exp. Clin. Endocrinol. Diabetes. 109:2001;288-303.
3. D. Elahi, G.S. Meneilly, K.L. Minaker, J.W. Rowe, D.K. Andersen, Regulation of hepatic glucose production by gastric inhibitory polypeptide in man, in: Proceedings of the Sixth International Conference on Gastrointestinal Hormones, Ottawa, 1986, p. 18.
4. O'Harte F.P.M., Gray A.M., Flatt P.R. Gastric inhibitory polypeptide and effects of glycation on glucose transport and metabolism in isolated mouse abdominal muscle. J. Endocrinol. 156:1998;237-243.
5. Yip R.G.-C., Boylan M.O., Kieffer T.J., Wolfe M.M. Functional GIP receptors are present on adipocytes. Endocrinology. 139:1998;4004-4007.
6. Eckel R.H., Fujimoto W.J., Brunzell J.D. Gastric inhibitory polypeptide enhances lipoprotein lipase activity in cultured preadipocytes. Diabetes. 28:1979;1141-1142.
7. Oben J., Morgan L., Fletcher J., Marks V. Effects of the entero-pancreatic hormones, gastric inhibitory polypeptide and glucagon-like polypeptide-1 (7-36) amide on fatty acid synthesis in explants of rat adipose tissue. J. Endocrinol. 130:1991;267-272.
8. Knapper J.M., Puddicombe S.M., Morgan L.M., Fletcher J.M. Investigation into the actions of glucose-dependent insulinotropic polypeptide and glucagon-like peptide-1(7-36)amide on lipoprotein lipase activity in explants of rat tissue. J. Nutr. 125:1995;183-188.
9. Trümper A., Trümper K., Trusheim H., Arnold R., Göke B., Horsch D. Glucose-dependent insulinotropic polypeptide is a growth factor for beta (INS-1) cells by pleiotropic signaling. Mol. Endocrinol. 15:2001;1559-1570.
10. Ehses J., Casilla V., Doty T., Pospisilik J.A., Demuth H.-U., Pederson R.A., McIntosh C.H.S. Glucose-dependent insulinotropic polypeptide (GIP) stimulates cell growth and promotes cell survival in INS-1 cells [abstract]. Diabetes. 51(Suppl. 2):2002;A 339.
11. O'Harte F.P.M., Mooney M.H., Flatt P.R. N-terminally modified gastric inhibitory polypeptide exhibits amino-peptidase resistance and enhanced antihyperglycaemic activity. Diabetes. 48:1999;758-765.
12. Kieffer T.J., McIntosh C.H.S., Pederson R.A. Degradation of glucose-dependent insulinotropic polypeptide and truncated glucagon-like peptide 1 in vitro and in vivo by dipeptidyl peptidase IV. Endocrinology. 136:1995;3585-3596.
13. Brown J.C., Dahl M., Kwauk S., McIntosh C.H.S., Otte S.C., Pederson R.A. Actions of GIP. Peptides. 2:1981;241-245.
14. Gault V.A., Parker J.C., Harriott P., Flatt P.R., O'Harte F.P.M. Evidence that the major degradation product of glucose-dependent insulinotropic polypeptide (GIP), GIP(3-42), is a GIP receptor antagonist in vivo. J. Endocrinol. 175:2002;525-533.
15. Deacon C.F., Danielsen P., Klarskov L., Olesen M., Holst J.J. Dipeptidyl peptidase IV inhibition reduces the degradation and clearance of GIP and potentiates its insulinotropic and antihyperglycemic effects in anesthetized pigs. Diabetes. 50:2001;1588-1597.
16. Pospisilik J.A., Stafford S.G., Demuth H.-U., Brownsey R., Parkhouse W., Finegood D.T., McIntosh C.H.S., Pederson R.A. Long-term treatment with the dipeptidyl peptidase IV inhibitor P32/98 causes sustained improvements in glucose tolerance, insulin sensitivity, hyperinsulinemia, and β-cell glucose responsiveness in VDF (fa/fa) Zucker rats. Diabetes. 51:2002;943-950.
17. Ahren B., Simonsson E., Larsson H., Landin-Olsson M., Torgeirsson H., Jansson P.A., Sandqvist M., Bavenholm P., Efendic S., Eriksson J.W., Dickinson S., Holmes D. Inhibition of dipeptidyl peptidase IV improves metabolic control over a 4-week study period in type 2 diabetes. Diabetes Care. 25:2002;869-875.
18. Mentlein R. Dipeptidyl-peptidase IV (CD26) - role in the inactivation of regulatory peptides. Regul. Pept. 85:1999;9-24.
19. Nauck M.A., Heimesaat M.M., Ørskov C., Holst J.J., Ebert R., Creutzfeldt W. Preserved incretin activity of glucagon-like peptide-1 (7-36amide), but not of synthetic human gastric inhibitory polypeptide in patients with type 2 diabetes mellitus. J. Clin. Invest. 91:1993;301-307.
20. Nauck M., Stockman R., Ebert R., Creutzfeldt W. Reduced incretin effect in type 2 (non-insulin-dependent) diabetes. Diabetologia. 29:1986;46-52.
21. Elahi D., McAloon-Dyke M., Fukagawa N., Meneilly G., Sclater A., Minaker K., Habener J., Andersen D. The insulinotropic actions of glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (7-37) in normal and diabetic subjects. Regul. Pept. 51:1994;63-74.
22. Jones I.R., Owens D.R., Moody A.J., Luzio S.D., Morris T., Hayes T.M. The effects of glucose-dependent insulinotropic polypeptide infused at physiological concentrations in normal subjects and type 2 (non-insulin-dependent) diabetic patients on glucose tolerance and B-cell secretion. Diabetologia. 30:1987;707-712.
23. Kjems L.L., Holst J.J., Volund A., Madsbad S. The influence of GLP-1 on glucose-stimulated insulin secretion: effects on beta-cell sensitivity in type 2 and nondiabetic subjects. Diabetes. 52:2003;380-386.
24. Ward W.K., Bolgiano D.C., McKnight B., Halter J.B., Porte D. Jr. Diminished B cell capacity in patients with noninsulin-dependent diabetes mellitus. J. Clin. Invest. 74:1984;1318-1328.
25. Meneilly G.S., Bryer-Ash M., Elahi D. The effect of glyburide on beta-cell sensitivity to glucose-dependent insulinotropic polypeptide. Diabetes Care. 16:1993;110-114.
26. Almind K., Ambye L., Urhammer S.A., Hansen T., Echwald S.M., Holst J.J., Gromada J., Thorens B., Pedersen O. Discovery of amino acid variants in the human glucose-dependent insulinotropic polypeptide (GIP) receptor: the impact on the pancreatic beta cell responses and functional expression studies in Chinese hamster fibroblast cells. Diabetologia. 41:1998;1194-1198.
27. O'Harte F.P.M., Abdel-Wahab Y.H.A., Conlon J.M., Flatt P.R. Amino-terminal glycation of gastric inhibitory polypeptide enhances its insulinotropic action on clonal pancreatic B-cells. Biochim. Biophys. Acta. 1425:1998;319-327.
28. O'Harte F.P.M., Mooney M.H., Kelly C.M.N., Flatt P.R. Improved glycaemic control in obese diabetic ob/ob mice using N-terminally modified gastric inhibitory polypeptide. J. Endocrinol. 165:2000;639-648.
29. O'Harte F.P.M., Gault V.A., Parker J.C., Harriott P., Mooney M.H., Bailey C.J., Flatt P.R. Improved stability, insulin-releasing activity and antidiabetic potential of two novel N-terminal analogues of glucose-dependent insulinotropic polypeptide: N-acetyl-GIP and pGlu-GIP. Diabetologia. 45:2002;1281-1291.
30. 1-modified enzyme resistant forms of GIP, is associated with significant antihyperglycaemic activity in spontaneous obesity-diabetes. Biochem. J. 367:2002;913-920.
31. 2-substituted analogues of glucose-dependent insulinotropic polypeptide. J. Endocrinol. 176:2003;133-141.
32. 2-substituted analogs of GIP with preserved biological activity in vivo. Metabolism. 52:2003;679-687.
33. 2]glucose-dependent insulinotropic polypeptide (GIP) improves glucose tolerance in normal and obese diabetic rats. Diabetes. 51:2002;656-661.
34. Lindsay J.R., Au S.T.B., Kelly C.M.N., O'Harte F.P.M., Flatt P.R., Bell P.M. A novel amino-terminally glycated analogue of glucose-dependent insulinotropic polypeptide (GIP), with prolonged insulinotropic activity in type 2 diabetes mellitus [abstract]. Diabetes. 51(Suppl. 2):2002;A 85.
35. Meier J.J., Nauck M.A., Schmidt W.E., Gallwitz B. Gastric inhibitory polypeptide: the neglected incretin revisited. Regul. Pept. 107:2002;1-7.
36. Tseng C.-C., Zhang X.-Y., Wolfe M.M. Effect of GIP and GLP-1 antagonists on insulin release in the rat. Am. J. Physiol. 276:1999;1049-1054.
37. 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. 46:2003;222-230.
38. Pederson R.A., Satkunarajah M., McIntosh C.H.S., Scrocchi L.A., Flamez D., Schuit F., Drucker D.J., Wheeler M.B. Enhanced glucose-dependent insulinotropic polypeptide secretion and insulinotropic action in glucagon-like peptide 1 receptor. -/- mice Diabetes. 47:1998;1046-1052.
39. Miyawaki K., Yamada Y., Yano H., Niwa H., Ban N., Ihara Y., Kubota A., Fujimoto S., Kajikawa M., Kuroe A., Tsuda K., Hashimoto H., Yamashita T., Jomori T., Tashiro F., Miyazaki J.I., Seino Y. Glucose tolerance caused by a defect in the enteroinsular axis: a study in gastric inhibitory polypeptide receptor knockout mice. Proc. Natl. Acad. Sci. USA. 96:1999;14843-14847.
40. Burcelin R., Dolci W., Thorens B. Long-lasting antidiabetic effects of a dipeptidyl peptidase IV-resistant analog of glucagon-like peptide-1. Metabolism. 48:1999;252-258.
41. Siegel E.G., Gallwitz B., Scharf G., Mentlein R., Morys-Wortmann C., Folsch U.R., Schrezenmeir J., Drescher K., Schmidt W.E. Biological activity of GLP-1-analogues with N-terminal modifications. Regul. Pept. 79:1999;93-102.
42. Xiao Q., Giguere J., Parisien M., Jeng W., St-Pierre S.A., Brubaker P.L., Wheeler M.B. Biological activities of glucagon-like peptide-1 analogues in vitro and in vivo. Biochemistry. 40:2001;2860-2869.
43. Gallwitz B., Ropeter T., Morys-Wortmann C., Mentlein R., Siegel E.G., Schmidt W.E. GLP-1 analogues resistant to degradation by dipeptidyl-peptidase IV in vitro. Regul. Pept. 86:2000;103-111.
44. Deacon C.F., Knudsen L.B., Madsen K., Wiberg F.C., Jacobsen O., Holst J.J. Dipeptidyl peptidase IV resistant analogues of glucagon-like peptide-1 which have extended metabolic stability and improved biological activity. Diabetologia. 41:1998;271-278.
45. Pederson R.A., Brown J.C. Interaction of gastric inhibitory polypeptide, glucose, and arginine on insulin and glucagon secretion from the perfused rat pancreas. Endocrinology. 103:1978;610-615.
46. Meier J.J., Gallwitz B., Siepmann N., Holst J.J., Deacon C.F., Schmidt W.E., Nauck M.A. Gastric inhibitory polypeptide (GIP) dose-dependently stimulates glucagon secretion in healthy human subjects as euglycaemia. Diabetologia. 46:2003;798-801. DOI 10.1007/s00125-003-1103-y.
47. Kreymann B., Williams G., Ghatei M.A., Bloom S.R. Glucagon-like peptide-1 7-36: a physiological incretin in man. Lancet. 2:1987;1300-1304.
48. Juhl C.B., Hollingdal M., Sturis J., Jakobsen G., Agersø H., Veldhuis J., Pørksen N., Schmitz O. Bedtime administration of NN2211, a long-acting GLP-1 derivative, substantially reduces fasting and postprandial glycemia in type 2 diabetes. Diabetes. 51:2002;424-429.
49. Gault V.A., Harriott P., Flatt P.R., O'Harte F.P.M. Cyclic AMP production and insulin releasing activity of synthetic fragment peptides of glucose-dependent insulinotropic polypeptide. Biosci. Rep. 22:2002;523-528.
50. 13)GIP. Cell Biol. Int. 27:2003;41-46.
51. Kühn-Wache K., Manhart S., Hoffmann T., Hinke S.A., Gelling R., Pederson R.A., McIntosh C.H.S., Demuth H.-U. Synthesis of analogs of glucose-dependent insulinotropic polypeptide with increased dipeptidyl peptidase IV resistance. Adv. Exp. Med. Biol. 477:2000;187-195.
52. Hinke S.A., Gelling R., Manhart S., Lynn F., Pederson R.A., Kühn-Wache K., Rosche F., Demuth H.-U., Coy D., McIntosh C.H.S. Structure-activity relationships of glucose-dependent insulinotropic polypeptide (GIP). Biol. Chem. 384:2003;403-407.
53. Manhart S., Hinke S.A., McIntosh C.H., Pederson R.A., Demuth H.U. Structure-function analysis of a series of novel GIP analogues containing different helical length linkers. Biochemistry. 42:2003;3081-3088.
54. Hinke S.A., Manhart S., Pamir N., Demuth H., Gelling R.W., Pederson R.A., McIntosh C.H. Identification of a bioactive domain in the amino-terminus of glucose-dependent insulinotropic polypeptide (GIP). Biochim. Biophys. Acta. 1547:2001;143-155.
55. Gault V.A., O'Harte F.P.M., Harriott P., Flatt P.R. Characterization of the cellular and metabolic effects of a novel enzyme-resistant antagonist of glucose-dependent insulinotropic polypeptide. Biochem. Biophys. Res. Commun. 290:2002;1420-1426.
56. Gremlich S., Porret A., Hani E.H., Cherif D., Vionnet N., Froguel P., Thorens B. Cloning, functional expression, and chromosomal localization of the human pancreatic islet glucose-dependent insulinotropic polypeptide receptor. Diabetes. 44:1995;1202-1208.
57. McClenaghan N.H., Barnett C.R., Ah-Sing E., Abdel-Wahab Y.H.A., O'Harte F.P.M., Yoon T.-W., Swanston-Flatt S.K., Flatt P.R. Characterization of a novel glucose-responsive insulin-secreting cell line, BRIN-BD11, produced by electrofusion. Diabetes. 45:1996;1132-1140.
58. Miyawaki K., Yamada Y., Ban N., Ihara Y., Tsukiyama K., Zhou K., Fujimoto S., Oku A., Tsuda K., Toyokuni S., Hiai H., Mizunoya W., Fushiki T., Holst J.J., Makino M., Tashita A., Kobara Y., Tsubamoto Y., Jinnouchi T., Jomori T., Seino Y. Inhibition of gastric inhibitory polypeptide signaling prevents obesity. Nat. Med. 8:2002;738-742.
59. 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. 32:1983;433-435.
60. 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 a high fat and high carbohydrate cafeteria diets. Acta Endocrinol. 112:1986;224-229.