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Therapeutic potential of the original incretin hormone glucose-dependent insulinotropic polypeptide: diabetes, obesity, osteoporosis and Alzheimer's disease?

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Pages 1039-1048 | Published online: 11 Aug 2010

Bibliography

  • Jornvall H, Carlquist M, Kwauk S, Amino acid sequence and heterogeneity of gastric inhibitory polypeptide (GIP). FEBS Lett 1981;123:205-10
  • Pederson RA, Schubert HE, Brown JC. Gastric inhibitory polypeptide. Its physiological release and insulinotropic action in the dog. Diabetes 1975;24:1050-6
  • Nauck M, Stockmann F, Ebert R, Creutzfeldt W. Reduced incretin effect in type 2 (non-insulin-dependent) diabetes. Diabetologia 1986;29:46-52
  • Madsbad S. Exenatide and liraglutide: different approaches to develop GLP-1 receptor agonists (incretin mimetics) – preclinical and clinical results. Best Pract Res Clin Endocrinol Metab 2009;23:463-77
  • Brown JC, Pederson RA, Jorpes E, Mutt V. Preparation of a highly active enterogastrone. Can J Physiol Pharmacol 1969;47:113-14
  • Pederson RA, Brown JC. The insulinotropic action of gastric inhibitory polypeptide in the perfused isolated rat pancreas. Endocrinology 1976;99:780-5
  • Lund PK, Goodman RH, Dee PC, Habener JF. Pancreatic preproglucagon cDNA contains two glucagon-related coding sequences arranged in tandem. Proc Natl Acad Sci 1982;79:345-9
  • Baggio LL, Drucker DJ. Biology of incretins: GLP-1 and GIP. Gastroenterology 2007;132:2131-57
  • McIntosh CH, Widenmaier S, Kim SJ. Glucose-dependent insulinotropic polypeptide (Gastric Inhibitory Polypeptide; GIP). Vitam Horm 2009;80:409-71
  • Irwin N, Flatt PR, Gault VA. GIP-based therapeutics for diabetes and obesity. Curr Chem Biol 2007;2:61-8
  • Usdin TB, Mezey E, Button DC, 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;133:2861-70
  • Bollag RJ, Zhong Q, Ding KH, Glucose-dependent insulinotropic peptide is an integrative hormone with osteotropic effects. Mol Cell Endocrinol 2001;177:35-41
  • Nyberg J, Anderson MF, Meister B, Glucose-dependent insulinotropic polypeptide is expressed in adult hippocampus and induces progenitor cell proliferation. J Neurosci 2005;25:1816-25
  • Irwin N, Flatt PR. Evidence for beneficial effects of compromised gastric inhibitory polypeptide action in obesity-related diabetes and possible therapeutic implications. Diabetologia 2009;52:1724-231
  • Mentlein R, Gallwitz B, Schmidt WE. Dipeptidyl-peptidase IV hydrolyses gastric inhibitory polypeptide, glucagon-like peptide-1 (7-36)amide, peptide histadine methionine and is responsible for their degradation in human serum. Eur J Biochem 1993;214:829-35
  • Marguet D, Baggio L, Kobayashi T, Enhanced insulin secretion and improved glucose tolerance in mice lacking CD26. Proc Natl Acad Sci USA 2000;97:6874-9
  • Deacon CF, Holst JJ. Linagliptin, a xanthine-based dipeptidyl peptidase-4 inhibitor with an unusual profile for the treatment of type 2 diabetes. Expert Opin Investig Drugs 2010;19:133-40
  • Irwin N, Flatt PR. Therapeutic potential for GIP receptor agonists and antagonists. Best Pract Res Clin Endocrinol Metab 2009;23:499-512
  • Ehses JA, Pellech SL, Pederson RA, McIntosh CH. Glucose-dependent insulinotropic polypeptide (GIP) activates the Raf-Mek 1/2-ERK 1/2 module via a cyclic AMP/PKA/Rap1-mediated pathway. J Biol Chem 2002;277:37088-97
  • Trumper A, Trumper K, Horsch D. Mechanisms of mitogenic and anti-apoptotic signaling by glucose-dependent insulinotropic polypeptide in beta(INS-1)-cells. J Endocrinol 2002;174:233-45
  • Trumper A, Trumper K, Trusheim H, Glucose-dependent insulinotropic polypeptide is a growth factor for beta (INS-1) cells by pleiotropic signaling. Mol Endocrinol 2001;15:1559-70
  • Renner S, Fehlings C, Herbach N, Glucose intolerance and reduced proliferation of pancreatic {beta}-cells in transgenic pigs with impaired GIP function. Diabetes 2010. [Epub ahead of print]
  • Gault VA, Flatt PR, O'Harte FPM. Glucose-dependent insulinotropic polypeptide (GIP): anti-diabetic and anti-obesity potential. Neuropeptides 2003;37:253-63
  • Vella A, Rizza RA. Extrapancreatic effects of GIP and GLP-1. Horm Metab Res 2004;36:830-6
  • Fujita Y, Asadi A, Yang GK, Differential Processing of Pro Glucose-Dependent Insulinotropic Polypeptide (ProGIP) in Gut. Am J Physiol Gastrointest Liver Physiol 2010. [Epub ahead of print]
  • Fujita Y, Wideman RD, Asadi A, Glucose-dependent insulinotropic polypeptide is expressed in pancreatic islet alpha-cells and promotes insulin secretion. Gastroenterology 2010. [Epub ahead of print]
  • Nauck MA, Heimesaat MM, Orskov C, 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;91:301-7
  • Ward WK, Bolgiano DC, McKnight B, Diminished B cell secretory capacity in patients with noninsulin-dependent diabetes mellitus. J Clin Invest 1984;74:1318-28
  • Kjems LL, Holst JJ, 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 2003;52:380-6
  • Kozawa J, Okita K, Imagawa A, Similar incretin secretion in obese and non-obese Japanese subjects with type 2 diabetes. Biochem Biophys Res Commun 2010;393:410-13
  • Aaboe K, Knop FK, Vilsboll T, KATP channel closure ameliorates the impaired insulinotropic effect of glucose-dependent insulinotropic polypeptide in patients with type 2 diabetes. J Clin Endocrinol Metab 2009;4:603-8
  • Hojberg PV, Vilsboll T, Rabol R, 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
  • Solomon TP, Haus JM, Kelly KR, Improved pancreatic beta-cell function in type 2 diabetics following lifestyle-induced weight loss is related to glucose-dependent insulinotropic polypeptide. Diabetes Care 2010. [Epub ahead of print]
  • Piteau S, Olver A, Kim SJ, Reversal of islet GIP receptor down-regulation and resistance to GIP by reducing hyperglycemia in the Zucker rat. Biochem Biophys Res Commun 2007;362:1007-12
  • Parks M, Rosebraugh C. Weighing risks and benefits of liraglutide – the FDA's review of a new antidiabetic therapy. N Engl J Med 2010;362:774-7
  • Irwin N, Gault VA, Green BD, Antidiabetic potential of two novel fatty acid derivatised, N-terminally modified analogues of glucose-dependent insulinotropic polypeptide (GIP): N-AcGIP(LysPAL16) and N-AcGIP(LysPAL37). Biol Chem 2005;386:679-87
  • Irwin N, Green BD, Gault VA, Degradation, insulin secretion, and antihyperglycemic actions of two palmitate-derivitized N-terminal pyroglutamyl analogues of glucose-dependent insulinotropic polypeptide. J Med Chem 2005;48:1244-50
  • Irwin N, O'Harte FP, Gault VA, GIP(Lys16PAL) and GIP(Lys37PAL): novel long-acting acylated analogues of glucose-dependent insulinotropic polypeptide with improved antidiabetic potential. J Med Chem 2006;49:1047-54
  • Irwin N, Green BD, Mooney MH, A novel, long-acting agonist of glucose-dependent insulinotropic polypeptide suitable for once-daily administration in type 2 diabetes. J Pharmacol Exp Ther 2005;314:1187-94
  • Irwin N, Clarke GC, Green BD, Evaluation of the antidiabetic activity of DPP IV resistant N-terminally modified versus mid-chain acylated analogues of glucose-dependent insulinotropic polypeptide. Biochem Pharmacol 2006;72:719-28
  • Kerr BD, Irwin N, O'Harte FP, Fatty acid derivatised analogues of glucose-dependent insulinotropic polypeptide with improved antihyperglycaemic and insulinotropic properties. Biochem Pharmacol 2009;78:1008-16
  • Madsen K, Knudsen LB, Agersoe H, Structure-activity and protraction relationship of long-acting glucagon-like peptide-1 derivatives: importance of fatty acid length, polarity, and bulkiness. J Med Chem 2007;50:6126-232
  • Gault VA, Kerr BD, Irwin N, Flatt PR. C-terminal mini-PEGylation of glucose-dependent insulinotropic polypeptide exhibits metabolic stability and improved glucose homeostasis in dietary-induced diabetes. Biochem Pharmacol 2008;75:2325-33
  • Kerr BD, Irwin N, Flatt PR, Gault VA. Prolonged GIP receptor activation using stable mini-PEGylated GIP improves glucose homeostasis and beta-cell function in age-related glucose intolerance. Peptides 2009;30:219-25
  • Salhanick AI, Clairmont KB, Buckholz TM, Contribution of site-specific PEGylation to the dipeptidyl peptidase IV stability of glucose-dependent insulinotropic polypeptide. Bioorg Med Chem Lett 2005;15:4114-17
  • Parker HE, Reimann F, Gribble FM. Molecular mechanisms underlying nutrient-stimulated incretin secretion. Expert Rev Mol Med 2010;12:e1
  • Chu ZL, Carroll C, Alfonso J, A role for intestinal endocrine cell-expressed g protein-coupled receptor 119 in glycemic control by enhancing glucagon-like peptide-1 and glucose-dependent insulinotropic peptide release. Endocrinology 2008;149:2038-47
  • Edfalk S, Steneberg P, Edlund H. Gpr40 is expressed in enteroendocrine cells and mediates free fatty acid stimulation of incretin secretion. Diabetes 2008;57:2280-7
  • Parker HE, Habib AM, Rogers GJ, Nutrient-dependent secretion of glucose-dependent insulinotropic polypeptide from primary murine K cells. Diabetologia 2009;52:289-98
  • Reimann F. Molecular mechanisms underlying nutrient detection by incretin-secreting cells. Int Dairy J 2010;20:236-42
  • Moriya R, Shirakura T, Ito J, Activation of sodium-glucose cotransporter 1 ameliorates hyperglycemia by mediating incretin secretion in mice. Am J Physiol Endocrinol Metab 2009;29:E1358-1365
  • Bollag RJ, Zhong Q, Phillips P, Osteoblast-derived cells express functional glucose-dependent insulinotropic peptide receptors. Endocrinology 2000;141:1228-35
  • Zhong Q, Ding KH, Mulloy AL, Glucose-dependent insulinotropic peptide stimulates proliferation and TGF-beta release from MG-63 cells. Peptides 2003;24:611-16
  • Zhong Q, Itokawa T, Sridhar S, Effects of glucose-dependent insulinotropic peptide on osteoclast function. Am J Physiol Endocrinol Metab 2007;292:E543-8
  • Xie D, Zhong Q, Ding KH, Glucose-dependent insulinotropic peptide-overexpressing transgenic mice have increased bone mass. Bone 2007;40:1352-60
  • Xie D, Cheng H, Hamrick M, Glucose-dependent insulinotropic polypeptide receptor knockout mice have altered bone turnover. Bone 2005;37:759-69
  • Tsukiyama K, Yamada Y, Yamada C, Gastric inhibitory polypeptide as an endogenous factor promoting new bone formation after food ingestion. Mol Endocrinol 2006;20:1644-51
  • Ding KH, Shi XM, Zhong Q, Impact of glucose-dependent insulinotropic peptide on age-induced bone loss. J Bone Miner Res 2008;23:536-43
  • Kaplan AM, Vigna SR. Gastric inhibitory polypeptide (GIP) binding sites in rat brain. Peptides 1994;15:297-302
  • Nyberg J, Jacobsson C, Anderson MF, Eriksson PS. Immunohistochemical distribution of glucose-dependent insulinotropic polypeptide in the adult rat brain. J Neurosci Res 2007;85:2099-119
  • Ding KH, Zhong Q, Xie D, Effects of glucose-dependent insulinotropic polypeptide on behavior. Peptides 2006;27:2750-5
  • Gault VA, Holscher C. Protease-resistant glucose-dependent insulinotropic polypeptide agonists facilitate hippocampal LTP and reverse the impairment of LTP induced by beta-amyloid. J Neurophysiol 2008;99:1590-5
  • Yip RG, Wolfe MM. GIP biology and fat metabolism. Life Sci 2000;66:91-103
  • Salera M, Giacomoni P, Pironi L, Gastric inhibitory polypeptide release after oral glucose: relationship to glucose intolerance, diabetes mellitus, and obesity. J Clin Endocrinol Metab 1982;55:329-36
  • Marks V. GIP – The obesity hormone. In: James WPT, Parker SW, editors. Current approaches: obesity. Duphar Medical Publications, Southampton, UK;1988. p. 13-19
  • Flatt PR, Bailey CJ, Kwasowski P, Abnormalities of GIP in spontaneous syndromes of obesity and diabetes in mice. Diabetes 1983;32:433-5
  • Bailey CJ, Flatt PR, Kwasowski P, Immunoreactive gastric inhibitory polypeptide and K cell hyperplasia in obese hyperglycaemic (ob/ob) mice fed high fat and high carbohydrate cafeteria diets. Acta Endocrinologica 1986;112:224-9
  • Enc FY, Ones T, Akin HL, Orlistat accelerates gastric emptying and attenuates GIP release in healthy subjects. Am J Physiol Gastrointest Liver Physiol 2009;296:G482-9
  • Hansotia T, Maida A, Flock G, Extrapancreatic incretin receptors modulate glucose homeostasis, body weight and energy expenditure. J Clin Invest 2007;117:143-52
  • Miyawaki K, Yamada Y, Ban N, Inhibition of gastric inhibitory polypeptide signaling prevents obesity. Nat Med 2002;8:738-42
  • Gault VA, O'Harte FP, Harriott P, Flatt PR. Characterization of the cellular and metabolic effects of a novel enzyme-resistant antagonist of glucose-dependent insulinotropic polypeptide. Biochem Biophys Res Commun 2002;290:1420-6
  • Gault VA, Irwin N, Green BD, Chemical ablation of gastric inhibitory polypeptide receptor action by daily (Pro3)GIP administration improves glucose tolerance and ameliorates insulin resistance and abnormalitities of islet structure in obestity-diabetes. Diabetes 2005;54:2436-46
  • Gault VA, McClean PL, Cassidy RC, Chemical GIP receptor antagonism protects against obesity, insulin resistance, glucose intolerance and associated disturbances in mice fed high fat and cafeteria diets. Diabetologia 2007;50:1752-62
  • Irwin N, McClean PL, O'Harte FPM, Early administration of the glucose-dependent insulinotropic polypeptide receptor antagonist, (Pro3)GIP, prevents the development of diabetes and related metabolic abnormalities associated with genetically-inherited obesity in ob/ob mice. Diabetologia 2007;50:1532-40
  • McClean PL, Irwin N, Cassidy RS, GIP receptor antagonism reverses obesity, insulin resistance and associated metabolic disturbances in mice by prolonged consumption of high fat diet. Am J Physiol Endocrinol Metab 2007;293:E1746-55
  • Tsubamoto Y, Nakamura T, Kinoshita H, A novel low-molecular weight antagonist of glucose-dependent insulinotropic polypeptide receptor, SKL14959, prevents obesity and insulin resistance. Diabetologia 2008;51:S373
  • Fulurija A, Lutz TA, Sladko K, Vaccination against GIP for the treatment of obesity. PLoS ONE 2008;3:e3163
  • Irwin N, McClean PL, Patterson S, Active immunisation against gastric inhibitory polypeptide (GIP) improves blood glucose control in an animal model of obesity-diabetes. Biol Chem 2009;390:75-80
  • Althage MC, Ford EL, Wang S, Targeted ablation of GIP-producing cells in transgenic mice reduces obesity and insulin resistance induced by a high fat diet. J Biol Chem 2008;283:18365-76
  • Shimotoyodome A, Suzuki J, Fukuoka D, RS4-type resistant starch prevents high-fat diet-induced obesity via increased hepatic fatty acid oxidation and decreased postprandial GIP in C57BL/6J mice. Am J Physiol Endocrinol Metab 2010;298:E652-2
  • Flatt PR. Effective surgical treatment of obesity may be mediated by ablation of the lipogenic gut hormone gastric inhibitory polypeptide (GIP): evidence and clinical opportunity for development of new obesity-diabetes drugs? Diab Vasc Dis Res 2007;4:151-3
  • Lindsay JR, Au STB, Kelly CMN, A novel amino-terminally glycated analogue of glucose-dependent insulinotropic polypeptide (GIP), with a prolonged insulinotropic activity in type 2 diabetes mellitus. Diabetes 2002;S5:1394

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