Enteroendocrine hormone mimetics for the treatment of obesity and diabetes

Current Opinion in Pharmacology

Volumn 13, Issue 6, 2013, Pages 989-995

  Irwin, Nigel ^a   Flatt, Peter R ^a  

^a UNIVERSITY OF ULSTER   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIDIABETIC AGENT; ANTIOBESITY AGENT; CHOLECYSTOKININ; CHOLECYSTOKININ A RECEPTOR; CHOLECYSTOKININ DERIVATIVE; CHOLECYSTOKININ RECEPTOR STIMULATING AGENT; GASTRIC INHIBITORY POLYPEPTIDE; GASTRIC INHIBITORY POLYPEPTIDE RECEPTOR; GASTRIC INHIBITORY POLYPEPTIDE RECEPTOR ANTAGONIST; GASTROINTESTINAL HORMONE; GLUCAGON LIKE PEPTIDE 1; GLUCAGON LIKE PEPTIDE 1 DERIVATIVE; GLUCAGON LIKE PEPTIDE 1 RECEPTOR AGONIST; GLUCAGON RECEPTOR; HORMONE RECEPTOR; INCRETIN; INSULIN; LEPTIN RECEPTOR; ORAL ANTIDIABETIC AGENT; OXYNTOMODULIN; OXYNTOMODULIN RECEPTOR; PALMITIC ACID DERIVATIVE; PHOSPHODIESTERASE IV INHIBITOR; RECEPTOR BLOCKING AGENT; SULFONYLUREA DERIVATIVE; UNCLASSIFIED DRUG;

ANTIDIABETIC ACTIVITY; ARTICLE; DIABETES MELLITUS; DISEASE ASSOCIATION; DISEASE SEVERITY; DRUG EFFICACY; DRUG MECHANISM; DRUG SAFETY; DRUG TARGETING; DRUG TREATMENT FAILURE; HORMONE ACTION; HUMAN; HYPERGLYCEMIA; INSULIN RESISTANCE; METABOLIC REGULATION; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; OBESITY; PANCREAS ISLET BETA CELL; PATHOPHYSIOLOGY; PRIORITY JOURNAL; TREATMENT RESPONSE;

ANIMALS; DIABETES MELLITUS; ENTEROENDOCRINE CELLS; GASTROINTESTINAL HORMONES; HUMANS; OBESITY; RECEPTORS, GLUCAGON;

EID: 84888197265     PISSN: 14714892     EISSN: 14714973     Source Type: Journal    
DOI: 10.1016/j.coph.2013.09.009     Document Type: Review

References (72)

1. M.J. Perley, and D.M. Kipnis Plasma insulin responses to oral and intravenous glucose: studies in normal and diabetic subjects J Clin Invest 46 1967 1954 1962
2. N. McIntyre, C.D. Holdsworth, and D.S. Turner Intestinal factors in the control of insulin secretion J Clin Endocrinol Metab 25 1965 1317 1324
3. G.J. Dockray Cholecystokinin Curr Opin Endocrinol Diabetes Obes 19 2012 8 12
4. A. Pocai Unraveling oxyntomodulin, GLP1's enigmatic brother J Endocrinol 215 2012 335 346
5. F.M. Gribble The gut endocrine system as a coordinator of postprandial nutrient homoeostasis Proc Nutr Soc 71 2012 456 462
6. P.R. Flatt 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 4 2007 151 153
7. V.A. Gault, F.P. O'Harte, and P.R. Flatt Glucose-dependent insulinotropic polypeptide (GIP): anti-diabetic and anti-obesity potential? Neuropeptides 37 2003 253 263 (Pubitemid 37464028)
8. R.A. Pederson, and J.C. Brown The insulinotropic action of gastric inhibitory polypeptide in the perfused isolated rat pancreas Endocrinology 99 1976 780 785
9. C.F. Deacon, and B. Ahrén Physiology of incretins in health and disease Rev Diabet Stud 8 2011 293 306
10. M.A. Nauck, M.M. Heimesaat, C. Orskov, J.J. Holst, R. Ebert, and W. Creutzfeldt 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 91 1993 301 307 (Pubitemid 23037285)
11. N. Irwin, V. Gault, and P.R. Flatt Therapeutic potential of the original incretin hormone glucose-dependent insulinotropic polypeptide: diabetes, obesity, osteoporosis and Alzheimer's disease? Expert Opin Investig Drugs 19 2010 1039 1048
12. C.M. Martin, N. Irwin, P.R. Flatt, and V.A. Gault 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
13. K. Aaboe, F.K. Knop, T. Vilsboll, A. Vølund, U. Simonsen, C.F. Deacon, S. Madsbad, J.J. Holst, and T. Krarup KATP channel closure ameliorates the impaired insulinotropic effect of glucose-dependent insulinotropic polypeptide in patients with type 2 diabetes J Clin Endocrinol Metab 94 2009 603 608
14. P.V. Højberg, T. Vilsbøll, R. Rabøl, F.K. Knop, M. Bache, T. Krarup, J.J. Holst, and S. Madsbad 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 52 2009 199 207
15. A.I. Taylor, N. Irwin, A.M. McKillop, S. Patterson, P.R. Flatt, and V.A. Gault Evaluation of the degradation and metabolic effects of the gut peptide xenin on insulin secretion, glycaemic control and satiety J Endocrinol 207 2010 87 93
16. B.M. Wice, S. Wang, D.L. Crimmins, K.A. Diggs-Andrews, M.C. Althage, E.L. Ford, H. Tran, M. Ohlendorf, T.A. Griest, and Q. Wang Xenin-25 potentiates glucose-dependent insulinotropic polypeptide action via a novel cholinergic relay mechanism J Biol Chem 285 2010 19842 19853
17. C.M. Martin, V.A. Gault, S. McClean, P.R. Flatt, and N. Irwin Degradation, insulin secretion, glucose-lowering and GIP additive actions of a palmitate-derivatised analogue of xenin-25 Biochem Pharmacol 84 2012 312 319
18. N. Irwin, and P.R. Flatt Evidence for beneficial effects of compromised gastric inhibitory polypeptide action in obesity-related diabetes and possible therapeutic implications Diabetologia 52 2009 1724 1731
19. K. Miyawaki, Y. Yamada, N. Ban, Y. Ihara, K. Tsukiyama, H. Zhou, S. Fujimoto, A. Oku, K. Tsuda, and S. Toyokuni Inhibition of gastric inhibitory polypeptide signaling prevents obesity Nat Med 8 2002 738 742 (Pubitemid 34778728)
20. M.C. Althage, E.L. Ford, S. Wang, P. Tso, K.S. Polonsky, and B.M. Wice Targeted ablation of glucose-dependent insulinotropic polypeptide-producing cells in transgenic mice reduces obesity and insulin resistance induced by a high fat diet J Biol Chem 283 2008 18365 18376
21. 3)GIP improves metabolic status in high-fat-fed mice Diabetes Obes Metab 12 2010 744 751
22. P.L. McClean, N. Irwin, R.S. Cassidy, J.J. Holst, V.A. Gault, and P.R. Flatt 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 293 2007 E1746 E1755
23. T. Nakamura, H. Tanimoto, Y. Mizuno, Y. Tsubamoto, and H. Noda Biological and functional characteristics of a novel low-molecular weight antagonist of glucose-dependent insulinotropic polypeptide receptor, SKL-14959, in vitro and in vivo Diabetes Obes Metab 14 2012 511 517
24. P. Ravn, C. Madhurantakam, S. Kunze, E. Matthews, C. Priest, S. O'Brien, A. Collinson, M. Papworth, M. Fritsch-Fredin, and L. Jermutus Structural and pharmacological characterization of novel potent and selective monoclonal antibody antagonists of glucose-dependent insulinotropic polypeptide receptor J Biol Chem 288 2013 19760 19772
25. D.A. Scott, K.S. Boye, L. Timlin, J.F. Clark, and J.H. Best A network meta-analysis to compare glycaemic control in patients with type 2 diabetes treated with exenatide once weekly or liraglutide once daily in comparison with insulin glargine, exenatide twice daily or placebo Diabetes Obes Metab 15 2013 213 223
26. R. Balena, I.E. Hensley, S. Miller, and A.H. Barnett Combination therapy with GLP-1 receptor agonists and basal insulin: a systematic review of the literature Diabetes Obes Metab 15 2013 485 502
27. C. Edwards Glucagon-like peptide-1 agonists in the treatment of type 2 diabetes Br J Hosp Med (Lond) 74 2013 198 201
28. B. Gier, P.C. Butler, C.K. Lai, D. Kirakossian, M.M. DeNicola, and M.W. Yeh Glucagon like peptide-1 receptor expression in the human thyroid gland J Clin Endocrinol Metab 97 2012 121 131
29. A.E. Butler, M. Campbell-Thompson, T. Gurlo, D.W. Dawson, M. Atkinson, and P.C. Butler Marked expansion of exocrine and endocrine pancreas with incretin therapy in humans with increased exocrine pancreas dysplasia and the potential for glucagon-producing neuroendocrine tumors Diabetes 2013 [Epub ahead of print]
30. J.S. Nachnani, D.G. Bulchandani, A. Nookala, B. Herndon, A. Molteni, P. Pandya, R. Taylor, T. Quinn, L. Weide, and L.M. Alba Biochemical and histological effects of exendin-4 (exenatide) on the rat pancreas Diabetologia 53 2010 153 159
31. P.S. Denker, and P.E. Dimarco Exenatide (exendin-4)-induced pancreatitis: a case report Diabetes Care 29 2006 471 (Pubitemid 44106551)
32. P.C. Butler, M. Elashoff, R. Elashoff, and E.A. Gale A critical analysis of the clinical use of incretin-based therapies: are the GLP-1 therapies safe? Diabetes Care 2013 [Epub ahead of print]
33. C. Alves, F. Batel-Marques, and A.F. Macedo A meta-analysis of serious adverse events reported with exenatide and liraglutide: acute pancreatitis and cancer Diabetes Res Clin Pract 98 2012 271 284
34. L. Bjerre Knudsen, L.W. Madsen, S. Andersen, K. Almholt, A.S. de Boer, D.J. Drucker, C. Gotfredsen, F.L. Egerod, A.C. Hegelund, and H. Jacobsen Glucagon-like peptide-1 receptor agonists activate rodent thyroid C-cells causing calcitonin release and C-cell proliferation Endocrinology 151 2010 1473 1486
35. M.A. Nauck A critical analysis of the clinical use of incretin-based therapies: the benefits by far outweigh the potential risks Diabetes Care 2013 [Epub ahead of print]
36. D.E. Cummings, and J. Overduin Gastrointestinal regulation of food intake J Clin Invest 117 2007 13 23 (Pubitemid 46048445)
37. N. Irwin, P. Frizelle, I.A. Montgomery, R.C. Moffett, F.P.M. O'Harte, and P.R. Flatt Beneficial effects of the novel choleycystokinin agonist (pGlu-Gln)-CCK-8 in animal models of obesity-diabetes Diabetologia 55 2012 2747 2758
38. F.P. O'Harte, M.H. Mooney, C.M. Kelly, and P.R. Flatt Glycated cholecystokinin-8 has an enhanced satiating activity and is protected against enzymatic degradation Diabetes 47 1998 1619 1624 (Pubitemid 28445351)
39. J.A. Lavine, P.W. Raess, D.S. Stapleton, M.E. Rabaglia, J.I. Suhonen, K.L. Schueler, J.E. Koltes, J.A. Dawson, B.S. Yandell, and L.C. Samuelson Cholecystokinin is up-regulated in obese mouse islets and expands beta-cell mass by increasing beta-cell survival Endocrinology 151 2010 3577 3588
40. R.J. Lieverse, J.B. Jansen, A.A. Masclee, and C.B. Lamers Satiety effects of a physiological dose of cholecystokinin in humans Gut 36 1995 176 179
41. I. Verbaeys, F. León-Tamariz, J. Buyse, E. Decuypere, H. Pottel, and M. Cokelaere Lack of tolerance development with long-term administration of PEGylated cholecystokinin Peptides 30 2009 699 704
42. J.N. Crawley, and M.C. Beinfeld Rapid development of tolerance to the behavioural actions of cholecystokinin Nature 302 1983 703 706 (Pubitemid 13120271)
43. A.D. Roses Stimulation of cholecystokinin-A receptors with Gl181771X a failed clinical trial that did not test the pharmacogenetic hypothesis for reduction of food intake Clin Pharmacol Ther 85 2009 362 365
44. N. Irwin, I.A. Montgomery, R.C. Moffett, and P.R. Flatt Chemical cholecystokinin receptor activation protects against obesity-diabetes in high fat fed mice and has sustainable beneficial effects in genetic ob/ob mice Biochem Pharmacol 85 2013 81 91
45. N. Irwin, P. Frizelle, F.P. O'Harte, and P.R. Flatt Metabolic effects of activation of CCK receptor signaling pathways by twice-daily administration of the enzyme-resistant CCK-8 analog, (pGlu-Gln)-CCK-8, in normal mice J Endocrinol 216 2013 53 59
46. M.J. Berna, J.A. Tapia, V. Sancho, and R.T. Jensen Progress in developing cholecystokinin (CCK)/gastrin receptor ligands that have therapeutic potential Curr Opin Pharmacol 7 2007 583 592 (Pubitemid 350177555)
47. N. Irwin, P. Frizelle, F.P. O'Harte, and P.R. Flatt (pGlu-Gln)-CCK- 8[mPEG]: a novel, long-acting, mini-PEGylated cholecystokinin (CCK) agonist that improves metabolic status in dietary-induced diabetes Biochim Biophys Acta 1830 2013 4009 4016
48. I.A. Montgomery, N. Irwin, and P.R. Flatt Beneficial effects of (pGlu-Gln)-CCK-8 on energy intake and metabolism in high fat fed mice are associated with alterations of hypothalamic gene expression Horm Metab Res 45 2013 471 473
49. A.M. Wren, and S.R. Bloom Gut hormones and appetite control Gastroenterology 132 2007 2116 2130 (Pubitemid 46693747)
50. E. Karra, and R.L. Batterham The role of gut hormones in the regulation of body weight and energy homeostasis Mol Cell Endocrinol 316 2010 120 128
51. M.A. Cohen, S.M. Ellis, C.W. Le Roux, R.L. Batterham, A. Park, M. Patterson, G.S. Frost, M.A. Ghatei, and S.R. Bloom Oxyntomodulin suppresses appetite and reduces food intake in humans J Clin Endocrinol Metab 88 2003 4696 4701 (Pubitemid 37357514)
52. K. Wynne, A.J. Park, C.J. Small, M. Patterson, S.M. Ellis, K.G. Murphy, A.M. Wren, G.S. Frost, K. Meeran, M.A. Ghatei, and S.R. Bloom Subcutaneous oxyntomodulin reduces body weight in overweight and obese subjects: a double-blind, randomized, controlled trial Diabetes 54 2005 2390 2395 (Pubitemid 41134267)
53. M.R. Druce, J.S. Minnion, B.C. Field, S.R. Patel, J.C. Shillito, M. Tilby, K.E. Beale, K.G. Murphy, M.A. Ghatei, and S.R. Bloom Investigation of structure-activity relationships of Oxyntomodulin (Oxm) using Oxm analogs Endocrinology 150 2009 1712 1722
54. Y.L. Liu, H.E. Ford, M.R. Druce, J.S. Minnion, B.C. Field, J.C. Shillito, J. Baxter, K.G. Murphy, M.A. Ghatei, and S.R. Bloom Subcutaneous oxyntomodulin analogue administration reduces body weight in lean and obese rodents Int J Obes (Lond) 34 2010 1715 1725
55. B.D. Kerr, P.R. Flatt, and V.A. Gault (d-Ser2)Oxm[mPEG-PAL]: a novel chemically modified analogue of oxyntomodulin with antihyperglycaemic, insulinotropic and anorexigenic actions Biochem Pharmacol 80 2010 1727 1735
56. K.L. Egerod, M.S. Engelstoft, K.V. Grunddal, M.K. Nøhr, A. Secher, I. Sakata, J. Pedersen, J.A. Windeløv, E.M. Füchtbauer, and J. Olsen A major lineage of enteroendocrine cells coexpress CCK, secretin, GIP, GLP-1, PYY, and neurotensin but not somatostatin Endocrinology 153 2012 5782 5795
57. B. Gallwitz, M. Witt, C. Morys-Wortmann, U.R. Fölsch, and W.E. Schmidt GLP-1/GIP chimeric peptides define the structural requirements for specific ligand-receptor interaction of GLP-1 Regul Pept 63 1996 17 22 (Pubitemid 26189051)
58. N. Irwin, K. Hunter, N. Frizzell, and P.R. Flatt Antidiabetic effects of sub-chronic activation of the GIP receptor alone and in combination with background exendin-4 therapy in high fat fed mice Regul Pept 153 2009 70 76
59. B. Gallwitz Emerging DPP-4 inhibitors: focus on linagliptin for type 2 diabetes Diabetes Metab Syndr Obes 6 2013 1 9
60. C.Q. Pan, J.M. Buxton, S.L. Yung, I. Tom, L. Yang, H. Chen, M. MacDougall, A. Bell, T.H. Claus, K.B. Clairmont, and J.P. Whelan Design of a long acting peptide functioning as both a glucagon-like peptide-1 receptor agonist and a glucagon receptor antagonist J Biol Chem 281 2006 12506 12515 (Pubitemid 43855337)
61. E.M. Sinclair, and D.J. Drucker Proglucagon-derived peptides: mechanisms of action and therapeutic potential Physiology (Bethesda) 20 2005 357 365 (Pubitemid 41457401)
62. T.H. Claus, C.Q. Pan, J.M. Buxton, L. Yang, J.C. Reynolds, N. Barucci, M. Burns, A.A. Ortiz, S. Roczniak, and J.N. Livingston Dual-acting peptide with prolonged glucagon-like peptide-1 receptor agonist and glucagon receptor antagonist activity for the treatment of type 2 diabetes J Endocrinol 192 2007 371 380 (Pubitemid 46444438)
63. A. Pocai, P.E. Carrington, J.R. Adams, M. Wright, G. Eiermann, L. Zhu, X. Du, A. Petrov, M.E. Lassman, and G. Jiang Glucagon-like peptide 1/glucagon receptor dual agonism reverses obesity in mice Diabetes 58 2009 2258 2266
64. J.W. Day, V. Gelfanov, D. Smiley, P.E. Carrington, G. Eiermann, G. Chicchi, M.D. Erion, J. Gidda, N.A. Thornberry, and M.H. Tschöp Optimization of co-agonism at GLP-1 and glucagon receptors to safely maximize weight reduction in DIO-rodents Biopolymers 98 2012 443 450
65. K. Fosgerau, L. Jessen, J. Lind Tolborg, T. ∅sterlund, K. Schæffer Larsen, K. Rolsted, M. Brorson, J. Jelsing, and T. Skovlund Ryge Neerup The novel GLP-1-gastrin dual agonist, ZP3022, increases β-cell mass and prevents diabetes in db/db mice Diabetes Obes Metab 15 2013 62 71
66. N. Irwin, K. Hunter, I.A. Montgomery, and P.R. Flatt Comparison of independent and combined metabolic effects of chronic treatment with (pGlu-Gln)-CCK-8 and long-acting GLP-1 and GIP mimetics in high fat-fed mice Diabetes Obes Metab 2013 [Epub ahead of print]
67. J.D. Roth, M.R. Erickson, S. Chen, and D.G. Parkes GLP-1R and amylin agonism in metabolic disease: complementary mechanisms and future opportunities Br J Pharmacol 166 2012 121 136
68. N. Irwin, I.A. Montgomery, and P.R. Flatt Comparison of the metabolic effects of sustained CCK1 receptor activation alone and in combination with upregulated leptin signalling in high-fat-fed mice Diabetologia 56 2013 1425 1435
69. S.A. Sadry, and D.J. Drucker Emerging combinatorial hormone therapies for the treatment of obesity and T2DM Nat Rev Endocrinol 2013 [Epub ahead of print]
70. P.R. Flatt Dorothy Hodgkin Lecture 2008, Gastric inhibitory polypeptide (GIP) revisited: a new therapeutic target for obesity-diabetes? Diabet Med 25 2008 759 764
71. V.K. Bhat, B.D. Kerr, P.R. Flatt, and V.A. Gault A novel GIP-oxyntomodulin hybrid peptide acting through GIP, glucagon and GLP-1 receptors exhibits weight reducing and anti-diabetic properties Biochem Pharmacol 85 2013 1655 1662
72. V.K. Bhat, B.D. Kerr, S. Vasu, P.R. Flatt, and V.A. Gault A DPP-IV-resistant triple-acting agonist of GIP, GLP-1 and glucagon receptors with potent glucose-lowering and insulinotropic actions in high-fat-fed mice Diabetologia 56 2013 1417 1424