Development of potent glucagon antagonists: Structure-activity relationship study of glycine at position 4

Journal of Peptide Research

Volumn 58, Issue 2, 2001, Pages 151-158

  Ahn, J M ^a   Medeiros, M ^a   Trivedi, D ^a   Hruby, Victor J ^a  

^a University of Arizona   (United States)

Author keywords

Alanine; Glucagon antagonists; Glycine; Leucine; Structure activity relationships

Indexed keywords

ALANINE; FUNCTIONAL GROUP; GLUCAGON; GLUCAGON [1 DESHISTIDINE 4 ALANINE 9 GLUTAMIC ACID] AMIDE; GLUCAGON [1 DESHISTIDINE 4 DEXTRO ALANINE 9 GLUTAMIC ACID] AMIDE; GLUCAGON [1 DESHISTIDINE 4 DEXTRO LEUCINE 9 GLUTAMIC ACID] AMIDE; GLUCAGON [1 DESHISTIDINE 4 LEUCINE 9 GLUTAMIC ACID] AMIDE; GLUCAGON [1 DESHISTIDINE 9 GLUTAMIC ACID] AMIDE; GLUCAGON RECEPTOR; GLYCINE; HORMONE ANTAGONIST; LEUCINE; UNCLASSIFIED DRUG;

AMINO ACID SUBSTITUTION; AMINO TERMINAL SEQUENCE; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; CONCENTRATION RESPONSE; ENANTIOMER; HYDROPHOBICITY; MALE; NONHUMAN; PEPTIDE SYNTHESIS; PRIORITY JOURNAL; PROTEIN BINDING; PROTEIN CONFORMATION; RAT; RECEPTOR BINDING; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION;

ADENYLATE CYCLASE; ANIMALS; BINDING, COMPETITIVE; CELL MEMBRANE; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; CHROMATOGRAPHY, THIN LAYER; DOSE-RESPONSE RELATIONSHIP, DRUG; GLUCAGON; GLYCINE; INHIBITORY CONCENTRATION 50; LIVER; MALE; PROTEIN BINDING; RATS; RATS, SPRAGUE-DAWLEY; STRUCTURE-ACTIVITY RELATIONSHIP;

ANIMALIA;

EID: 0034909040     PISSN: 1397002X     EISSN: None     Source Type: Journal    
DOI: 10.1034/j.1399-3011.2001.00880.x     Document Type: Article

References (38)

1. Glucagon: Molecular biology and structure-activity
2. The regulation of gluconeogenesis in isolated rat liver cells by glucagon, insulin, dibutyryl cyclic adenosine monophosphate, and fatty acids
3. Glucagon and the circulation
4. Regulation of hepatic fatty acid oxidation and ketone body production
5. Evidence for interdependent action of glucagon and nucleotides on the hepatic adenytate cyclase system
6. The role of hormone receptors and GTP-regulatory proteins in membrane transduction
7. The essential role of glucagon in the pathogenesis of diabetes mellitus
8. Rote of glucagon in the pathogenesis of diabetes: The status of the controversy
9. Structure-conformation-activity studies of glucagon and semi-synthetic glucagon analogs
10. Conformational considerations in the design of glucagon agonists and antagonists: Examination using synthetic analogs
11. Glucagon amino groups, evaluation of modifications leading to antagonism and agonism
12. Synthetic antagonists of glucagon
13. 9] Glucagon amide: A newly designed 'pure' glucagon antagonist
14. Hyperglycemia of diabetic rats decreased by a glucagon receptor antagonist
15. 9]glucagon amide, a glucagon antagonist
16. 2 identifies glucagon antagonists from weak partial agonists/ antagonists
17. Chain reversals in proteins
18. Analysis and prediction of the different types of beta-tum in proteins
19. Constrained peptides: Models of bioactive peptides and protein substructures
20. X-Ray analysis of glucagon and its relationship to receptor binding
21. 1H nuclear magnetic resonance
22. Empirical predictions of protein conformation
23. A model for the three-dimensional structure of glucagon
24. Glucagon antagonists: Contribution to binding and activity of the amino-terminal sequence 1-5, position 12, and the putative α-helical segment 19-27
25. Synthetic analogs of the hypothalamic luteinizing hormone releasing factor with increased agonist or antagonist properties
26. Analogs of luteinizing hormone-releasing hormone with increased biological activity produced by D-amino acid substitutions in position 6
27. Receptor binding and adenylate cyclase activities of glucagon analogues modified in the N-terminal region
28. The role of phenylalanine at position 6 in glucagon's mechanism of biological action: Multiple replacement analogues of glucagon
29. Isolation of an organ specific protein antigen from cell surface membrane of rat liver
30. The glucagon-sensitive adenylate cyclase system in membranes of rat liver. Comparison between glucagon- and fluoride-stimulated activities
31. Protein measurement with folin phenol reagent
32. A modification of the Lowry procedure to simplify protein determination in membrane and lipoprotein samples
33. 1-6 binds to the glucagon receptor and activates hepatic adenylate cyclase
34. 27)glucagon
35. Highly sensitive adenylate cyclase assay
36. pA, A new scale for the measurement of drug antagonism
37. Solid-phase synthesis of protected peptide fragments using a trialkoxydiphenyl-methylester resin
38. Development of potent truncated glucagon antagonists