Dual modulation of GIP and glucagon action by the low molecular weight compound 4-hydroxybenzoic acid 2-bromobenzylidene hydrazide

Diabetes, Obesity and Metabolism

Volumn 13, Issue 8, 2011, Pages 742-749

  Franklin, Z J ^a   Mcdonnell, B ^a   Montgomery, I A ^a   Flatt, P R ^a   Irwin, N ^a  

^a UNIVERSITY OF ULSTER   (United Kingdom)

Author keywords

Gastric inhibitory polypeptide; Glucagon; Glucagon like peptide 1; Glucose homeostasis; Insulin secretion; Type 2 diabetes

Indexed keywords

4 HYDROXYBENZOIC ACID; 4 HYDROXYBENZOIC ACID 2 BROMOBENZYLIDENE HYDRAZIDE; CYCLIC AMP; GASTRIC INHIBITORY POLYPEPTIDE; GLUCAGON; GLUCAGON LIKE PEPTIDE 1; GLUCOSE; HORMONE RECEPTOR; UNCLASSIFIED DRUG;

ADIPOCYTE; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; GLUCOSE BLOOD LEVEL; IN VITRO STUDY; IN VIVO STUDY; INSULIN BLOOD LEVEL; INSULIN RELEASE; INSULIN RESISTANCE; LIPID STORAGE; MALE; MODULATION; MOLECULAR WEIGHT; MOUSE; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; OBESITY;

EID: 79959415632     PISSN: 14628902     EISSN: 14631326     Source Type: Journal    
DOI: 10.1111/j.1463-1326.2011.01401.x     Document Type: Article

References (37)

1. Irwin N, Gault V, Flatt PR. Therapeutic potential of the original incretin hormone glucose-dependent insulinotropic polypeptide: diabetes, obesity, osteoporosis and Alzheimer's disease? Expert Opin Investig Drugs 2010; 19: 1039-1048.
2. Irwin N, Flatt PR. Therapeutic potential for GIP receptor agonists and antagonists. Best Pract Res Clin Endocrinol Metab 2009; 23: 499-512.
3. Yip RG, Boylan MO, Kieffer TJ, Wolfe MM. Functional GIP receptors are present on adipocytes. Endocrinology 1998; 139: 4004-4007.
4. Ross SA, Dupre J. Effects of ingestion of triglyceride or galactose on secretion of gastric inhibitory polypeptide and on responses to intravenous glucose in normal and diabetic subjects. Diabetes 1978; 27: 327-333.
5. Gniuli D, Calcagno A, Dalla Libera L et al. High-fat feeding stimulates endocrine, glucose-dependent insulinotropic polypeptide (GIP)-expressing cell hyperplasia in the duodenum of Wistar rats. Diabetologia 2010; 53: 2233-2240.
6. Kim SJ, Nian C, McIntosh CH. GIP increases human adipocyte LPL expression through CREB and TORC2-mediated trans-activation of the LPL gene. J Lipid Res 2010; 51: 3145-3157.
7. Flatt PR. Dorothy Hodgkin Lecture 2008. Gastric inhibitory polypeptide (GIP) revisited: a new therapeutic target for obesity-diabetes? Diabet Med 2008; 25: 759-764.
8. Althage MC, Ford EL, Wang S, Tso P, Polonsky KS, Wice BM. 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 2008; 283: 18365-18376.
9. 3)GIP improves metabolic status in high-fat-fed mice. Diabetes Obes Metab 2010; 12: 744-751.
10. Miyawaki K, Yamada Y, Ban N et al. Inhibition of gastric inhibitory polypeptide signaling prevents obesity. Nat Med 2002; 8: 738-742.
11. 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: 1420-1426.
12. 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.
13. McClean PL, Irwin N, Hunter K, Gault VA, Flatt PR. (Pro(3))GIP[mPEG]: novel, long-acting, mPEGylated antagonist of gastric inhibitory polypeptide for obesity-diabetes (diabesity) therapy. Br J Pharmacol 2008; 155: 690-701.
14. Irwin N, Flatt PR, Patterson S, Green BD. Insulin-releasing and metabolic effects of small molecule GLP-1 receptor agonist 6, 7-dichloro-2-methylsulfonyl-3-N-tert-butylaminoquinoxaline. Eur J Pharmacol 2010; 628: 268-273.
15. Sloop KW, Willard FS, Brenner MB et al. Novel small molecule glucagon-like peptide-1 receptor agonist stimulates insulin secretion in rodents and from human islets. Diabetes 2010; 59: 3099-3107.
16. Coopman K, Huang Y, Johnston N, Bradley SJ, Wilkinson GF, Willars GB. Comparative effects of the endogenous agonist glucagon-like peptide-1 (GLP-1)-(7-36) amide and the small-molecule ago-allosteric agent "compound 2" at the GLP-1 receptor. J Pharmacol Exp Ther 2010; 334: 795-808.
17. Flatt PR, Bailey CJ, Green BD. Dipeptidyl peptidase IV (DPP IV) and related molecules in type 2 diabetes. Front Biosci 2008; 13: 3648-3660.
18. McClenaghan NH, Barnett CR, Ah-Sing E et al. Characterization of a novel glucose-responsive insulin-secreting cell line, BRIN-BD11, produced by electrofusion. Diabetes 1996; 45: 1132-1140.
19. Hamid M, McCluskey JT, McClenaghan NH, Flatt PR. Comparison of the secretory properties of four insulin-secreting cell lines. Endocr Res 2002; 28: 35-47.
20. Flatt PR, Bailey CJ. Abnormal plasma glucose and insulin responses in heterozygous lean (ob/+) mice. Diabetologia 1981; 20: 573-577.
21. Yip RG, Wolfe MM. GIP biology and fat metabolism. Life Sci 2000; 66: 91-103.
22. Gault VA, Irwin N, Green BD et al. Chemical ablation of gastric inhibitory polypeptide receptor action by daily (Pro3)GIP administration improves glucose tolerance and ameliorates insulin resistance and abnormalities of islet structure in obesity-related diabetes. Diabetes 2005; 54: 2436-2446.
23. Tseng CC, Kieffer TJ, Jarboe LA, Usdin TB, Wolfe MM. Postprandial stimulation of insulin release by glucose-dependent insulinotropic polypeptide (GIP). Effect of a specific glucose-dependent insulinotropic polypeptide receptor antagonist in the rat. J Clin Invest 1996; 98: 2440-2445.
24. McIntosh CH, Widenmaier S, Kim SJ. Glucose-dependent insulinotropic polypeptide (gastric inhibitory polypeptide; GIP). Vitam Horm 2009; 80: 409-471.
25. 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.
26. Brubaker PL, Drucker DJ. Structure-function of the glucagon receptor family of G protein-coupled receptors: the glucagon, GIP, GLP-1, and GLP-2 receptors. Receptors Channels 2002; 8: 179-188.
27. Nauck MA, Vardarli I, Deacon CF, Holst JJ, Meier JJ. Secretion of glucagon-like peptide-1 (GLP-1) in type 2 diabetes: what is up, what is down? Diabetologia 2011; 54: 10-18.
28. Ling A, Plewe M, Gonzalez J et al. Human glucagon receptor antagonists based on alkylidene hydrazides. Bioorg Med Chem Lett 2002; 12: 663-666.
29. Madsen P, Ling A, Plewe M et al. Optimization of alkylidene hydrazide based human glucagon receptor antagonists. Discovery of the highly potent and orally available 3-cyano-4-hydroxybenzoic acid [1-(2, 3, 5, 6-tetramethylbenzyl)-1H-indol-4-ylmethylene]hydrazide. J Med Chem 2002; 45: 5755-5775.
30. Irwin N, Green BD, Gault VA et al. Degradation, insulin secretion, and antihyperglycemic actions of two palmitate-derivitized N-terminal pyroglutamyl analogues of glucose-dependent insulinotropic polypeptide. J Med Chem 2005; 48: 1244-1250.
31. Pocai A, Carrington PE, Adams JR et al. Glucagon-like peptide 1/glucagon receptor dual agonism reverses obesity in mice. Diabetes 2009; 58: 2258-2266.
32. Pan CQ, Buxton JM, Yung SL et al. Design of a long acting peptide functioning as both a glucagon-like peptide-1 receptor agonist and a glucagon receptor antagonist. J Biol Chem 2006; 281: 12506-12515.
33. Claus TH, Pan CQ, Buxton JM et al. 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 2007; 192: 371-380.
34. Gromada J, Rorsman P. New insights into the regulation of glucagon secretion by glucagon-like peptide-1. Horm Metab Res 2004; 36: 822-829.
35. Gromada J, Franklin I, Wollheim CB. Alpha-cells of the endocrine pancreas: 35 years of research but the enigma remains. Endocr Rev 2007; 28: 84-116.
36. 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.
37. Knudsen LB, Kiel D, Teng M et al. Small-molecule agonists for the glucagon-like peptide 1 receptor. Proc Natl Acad Sci USA 2007; 104: 937-942.