Low level cyclic adenosine 3',5'-monophosphate accumulation analysis of [des-His1,des-Phe6,Glu9]glucagon-NH2 identifies glucagon antagonists from weak partial agonists/antagonists

Endocrinology

Volumn 137, Issue 8, 1996, Pages 3316-3322

  Van Tine, Brian A ^a   Azizeh, Bassem Y ^a   Trivedi, Dev ^a   Phelps, Jason R ^a   Houslay, Miles D ^c   Johnson, David G ^b   Hruby, Victor J ^a  

^a University of Arizona   (United States)

^b UNIVERSITY OF ARIZONA   (United States)

^c UNIVERSITY OF GLASGOW   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

CYCLIC AMP; ISOBUTYLMETHYLXANTHINE; PHOSPHODIESTERASE INHIBITOR; ROLIPRAM;

ANIMAL CELL; ARTICLE; DRUG ACCUMULATION; DRUG ANTAGONISM; ENZYME ACTIVITY; ENZYME INHIBITION; GLUCAGON RELEASE; GLUCOSE HOMEOSTASIS; GLYCOLYSIS; HORMONAL REGULATION; MULTIGENE FAMILY; NONHUMAN; PRIORITY JOURNAL; PROTEIN PHOSPHORYLATION; RAT; SIGNAL TRANSDUCTION;

EID: 0029891226     PISSN: 00137227     EISSN: None     Source Type: Journal    
DOI: 10.1210/endo.137.8.8754757     Document Type: Article

References (39)

1. Unger RH 1978 Role of glucagon in the pathogenesis of diabetes: the status of the controversy. Metab Clin Exp 27:1691-1709
2. Bressler R, Johnson D 1992 New pharmacological approaches to therapy of NIDDM. Diabetes Care 15:792-805
3. Bygrave FL, Bendetti A 1993 Calcium: its modulation in liver by cross-talk between the actions of glucagon and mobilizing agonists. Biochem J 296:1-14
4. Bregman MD, Trivedi D, Hruby VJ 1980 Glucagon amino groups. Evaluation of modifications leading to antagonism and agonism. J Biol Chem 255:11725-11731
5. Tang EKY, Houslay MD 1992 Glucagon, vasopressin and angiotensin all elicit a rapid, transient increase in hepatocyte protein kinase C activity. Biochem J 283:341-346
6. +2-mobilizing hormones in cultured hepatocytes. Role of phosphatidylinositol and phosphatidylcholine hydrolysis. Biochem J 257:371-378
7. Wakelam MJO, Murphy GJ, Hruby VJ, Houslay MD 1986 Activation of two signal-transduction systems in hepatocytes by glucagon. Nature 323:68-71
8. Beavo JA, Conti M, Heaslip RJ 1994 Multiple cyclic nucleotide phosphodiesterases. Mol Pharmacol 46:399-405
9. Lavan BE, Lakey T, Houslay MD 1989 Resolution of soluble cyclic nucleotide phosphodiesterase isoenzymes, from liver and hepatocytes, identities a novel IBMX-insensitive form. Biochem Pharmacol 38:4123-4136
10. Houslay MD 1990 The use of selective inhibitors and computer modeling to evaluate the role of specific high affinity cyclic AMP phosphodiesterases in the hormonal regulation of hepatocyte intracellular cyclic AMP concentrations. Cell Signal 2:85-98
11. Pyne NJ, Cooper ME, Houslay MD 1987 The insulin- and glucagon-stimulated 'dense-vesicle' high-affinity cyclic AMP phosphodiesterase from rat liver. Biochem J 242:33-42
12. Marchmont RJ, Houslay MD 1980 Insulin triggers cyclic AMP-dependent activation and phosphorylation of a plasma membrane cyclic AMP phosphodiesterase. Nature 286:904-906
13. Heyworth CM, Wallace AV, Houslay MD 1983 Insulin and glucagon regulate the activation of two distinct membrane bound cyclic AMP phosphodiesterases in hepatocytes. Biochem J 214:99-110
14. Kilgour E, Anderson NG, Houslay MD 1989 Activation and phosphorylation of the 'dense-vesicle' high-affinity cyclic AMP phosphodiesterase by cyclic AMP-dependent protein kinase. Biochem J 260:27-36
15. Wilson SR, Wallace AV, Houslay MD 1983 Insulin activates the plasma membrane and dense vesicle cyclic AMP phosphodiesterase in hepatocytes by distinct routes. Biochem J 216:245-248
16. Johnson DG, Goebel CU, Hruby VJ, Bregman MD, Trivedi D 1982 Hyperglycemia of diabetic rats decreased by a glucagon receptor antagonist. Science 215:1115-1116
17. 9]glucagon amide, a glucagon antagonist. Peptides 10:1171-1177
18. Hruby VJ 1982 Structure-conformation-activity studies of glucagon and semi-synthetic glucagon analogs. Mol Cell Biochem 44:49-64
19. Zechel C, Trivedi D, Hruby VJ 1991 Synthetic glucagon antagonists and partial agonists. Int J Peptide Protein Res 38:131-138
20. Unson CG, Andreu D, Gurzenda EM, Merrifield RB 1987 Synthetic peptide antagonists of glucagon. Proc Natl Acad Sci USA 84:4083-4087
21. Heyworth CM, Wallace AV, Wilson SR, Houslay MD 1984 An assessment of the ability of insulin-stimulated cyclic AMP phosphodiesterase to decrease hepatocyte intracellular cyclic AMP concentrations. Biochem J 222:183-187
22. Wilson M, Sullivan M, Brown N, Houslay MD 1994 Purification, characterization and analysis of rolipram inhibition of a human type-IVA cyclic AMP-specific phosphodiesterase expressed in yeast. Biochem J 304:407-415
23. Weishaar RE, Cain MH, Bristol JA 1985 A new generation of phosphodiesterase inhibitors: multiple forms of phosphodiesterase and the potential for drug selectivity. J Med Chem 28:537-545
24. nv rolipram-sensitive, cAMP-specific phosphodiesterase from human brain. cloning and expression of cDNA, biochemical characterization of recombinant protein and tissue distribution of mRNA. J Biol Chem 268:6470-6476
25. Nicholson CD, Challiss RAJ, Shahid M 1991 Differential modulation of tissue function and therapeutic potential of selective inhibitors of cyclic nucleotide phosphodiesterase isoenzymes. Trends Pharmacol Sci 12:19-27
26. 9]glucagon amide: a newly designed "pure" glucagon antagonist. Bioorg Med Chem Lett 5:1849-1852
27. Neville Jr DM 1968 Isolation of an organ specific protein antigen from cell surface membrane of rat liver. Biochim Biophys Acta 154:540-552
28. Pohl SL, Birnbaumer L, Rodbell M 1971 The glucagon-sensitive adenylate cyclase system in membranes of rat liver. Comparison between glucagon- and fluoride-stimulated activities. J Biol Chem 246:1857-1860
29. Lowry OH, Rosebrough NJ, Farr AL, Randall RJ 1951 Protein measurement with the Polin phenol reagent. J Biol Chem 193:265-275
30. Markwell MAK, Haas SM, Bieleer LL, Tolbert NE 1978 A modification of the Lowry procedure to simplify protein determination in membrane and lipoprotein samples. Anal Biochem 87:206-210
31. Lin ME, Wright DE, Hruby VJ, Rodbell M 1975 Structure-function relationships in glucagon: properties of highly purified des-His-1-, monoiodo-, and (des-Asn-28,Thr29)(homoserine lactone-27)glucagon. Biochemistry 14: 1559-1563
32. Salomon Y, Londos G, Rodbell M 1974 A high sensitivity adenylate cyclase assay. Anal Biochem 58: 541-548
33. Berry MN, Friend DS 1969 High-yield preparation of isolated rat liver parenchymal cells: a biochemical and fine structural study. J Biol Chem 43:506-520
34. Heyworth CM, Houslay MD 1983 Challenge of hepatocytes by glucagon triggers a rapid modulation of adenylate cyclase activity in isolated membranes. Biochem J 214:93-98
35. Brown BL, Ekins RP, Albano JMP 1972 Saturation assay tor cyclic AMP using endogenous binding protein. Adv Cyclic Nucleotide Res 2:25-40
36. Joseph SK, Williamson JR 1983 The origin, quantitation, and kinetics of intracellular calcium mobilization by vasopressin and phenylephrine in hepatocytes. J Biol Chem 258:10425-10432
37. Stalmans W, Hers H 1975 The stimulation of liver phosphorylase b by AMP, fluoride and sulfate. Eur J Biochem 54:341-350
38. Rajab AA, Ahren B 1993 Long-term diabetogenic effect of streptozotocin in rats. Pancreas 8:50-57
39. Korn AP, Ottensmeyer FP 1983 A model for the three-dimensional structure of glucagon. J Theor Biol 105:403-425