Approaches to glucagon receptor antagonists

Bibliography

• UNGER RH: Role of glucagon in the pathogenesis of diabetes: the status of the controversy. Metabolism (1978) 27:1691–1709.
   PubMed Web of Science ®Google Scholar
• UNGER RH, ORCI L: The essential role of glucagon in the pathogenesis of diabetes mellitus. Lancet (1975) 1:14–26.
   PubMed Web of Science ®Google Scholar
• UNGER RH, ORCI L: Role of glucagon in diabetes. Arch. Intern. Med. (1977) 137:482–491.
   PubMedGoogle Scholar
• AZIZEH BY, AHN JM, CASPARI R, SHENDEROVICH MD, TRIVEDI D, HRUBY VJ: The role of phenylalanine at position 6 in glucagon's mechanism of biological action: multiple replacement analogues of glucagon. .1 Med. Chem. (1997) 40:2555–2562.
   PubMedGoogle Scholar
• UNSON CG, GURZENDA EM, MERRIFIELD RB: Biological activities of des-His1[G1u9]glucagon amide, a glucagon antagonist. Peptides (1989) 10:1171–1177.
   PubMedGoogle Scholar
• TERLECKYJ I, SALZIG M, UNSON C, MERRIFIELD B: The glucagon receptor antagonist ALT3000 lowers fasting hyperglycemia in rat models of diabetes. Diabetes (1996) 45 (Suppl. 2):220A (poster811).
   Google Scholar
• BRAND CL, ROLIN B, JORGENSEN PN, SVENDSEN I, KRISTENSEN JS, HOLST JJ: Immunoneutralization of endogenous glucagon with monoclonal glucagon antibody normalizes hyperglycemia in moderately streptozotocin-diabetic rats. Diabetologia (1994) 37:985–993.
   PubMed Web of Science ®Google Scholar
• BRAND CL, JORGENSEN PN, SVENDSEN I, HOLST JJ: Evidence for a major role for glucagon in regulation of plasma glucose in conscious, nondiabetic, and alloxan-induced diabetic rabbits. Diabetes (1996) 45:1076–1083.
   PubMed Web of Science ®Google Scholar
• BRAND CL, JORGENSEN PN, KNIGGE U et al.: Role of glucagon in maintenance of euglycemia in fed and fasted rats. Am.j Physiol (1995) 269(3):E469–E477.
   Google Scholar
• CHRISTOPHE J: Glucagon receptors: from genetic structure and expression to effector coupling and biological responses. Biochim. Biophys. Acta (1995) 1241:45–57.
   PubMed Web of Science ®Google Scholar
• JELINEK LJ, LOK S, ROSENBERG GB et al.: Expression cloning and signaling properties of the rat glucagon receptor. Science (1993) 259:1614–1616.
   PubMedGoogle Scholar
• UNSON CG, CYPESS AM, KIM HN: Characterization of deletion and truncation mutants of the rat glucagon receptor." Biol. Chem. (1995) 270:27720–27727.
   PubMedGoogle Scholar
• CHICCHI GG, GRAZIANO MP, KOCH G et al.: Alterations in receptor activation and divalent cation activation of agonist binding by deletion of intracellular domains of the glucagon receptor.' Biol. Chem. (1997) 272:7765–7769.
   Google Scholar
• LIVINGSTON JN, SCHOEN WR: Glucagon and glucagon-lipe peptide-1. Ann. Rep. Med. Chem. (1999) 34:189–198.
   Google Scholar
• MADSEN P, BRAND CL, HOLST JJ et at.:Advances in non-peptide glucagon receptor antagonists. Carr: Amin. Design (1999) 5:683–691.
   Google Scholar
• CONNELL RD: Glucagon antagonists for the treatment of Type 2 diabetes. Expert Opin. Tiler: Patents (1999) 9(6):701–709.
   Web of Science ®Google Scholar
• MCCORMACK JG, WESTERGAARD N, KRISTIANSEN M et al.: Pharmacological approaches to inhibit endogenous glucose production as a means of anti-diabetic therapy. Curr. Pharm. Design (2001) 7:1451–1474.
   PubMedGoogle Scholar
• PARKER JC, MCPHERSON RK, ANDREWS KM et al.: Effects of skyrin, a receptor-selective glucagon antagonist, in rat and human hepatocytes. Diabetes (2000) 49:2079–2086.
   PubMed Web of Science ®Google Scholar
• WRIGHT JB, DULIN WE, MARKILLIE JH: The antidiabetic activity of 3,5-dimethylpyrazoles." Med. Chem. (1964) 7:102–107.
   PubMed Web of Science ®Google Scholar
• COLLINS JL, DAMBEK PJ, GOLDSTEIN SW, FARACI WS: CP-99,711: a non-peptide glucagon receptor antagonist. Bioorg. Med. Chem. Lett. (1992) 2(9):915–918.
   Google Scholar
• GUILLON J, DALLEMAGNE P, PFEIFFER B et al.: Synthesis of new pyrrolo [1,2-alquinoxalines: potential non-peptide glucagon receptor antagonists. Ear: .1. Med. Chem. (1998) 33:293–308.
   Google Scholar
• COOK JH, DOHERTY EM, LADOUCEUR G, LIVINGSTON JN, MACDOUGALL ML: Design and synthesis of quinolines as glucagon antagonists. Proceedings of the 2 16thACS National Meeting. Boston, USA (1998):MEDI285.
   Google Scholar
• MADSEN P, KNUDSEN LB, WIBERG FC, CARR RD: Discovery and structure-activity relationship of the first non-peptide competitive human glucagon receptor antagonist. " Med. Chem. (1998) 41:5150–5157.
   PubMed Web of Science ®Google Scholar
• LING A, HONG Y, GONZALEZ J et al.: Identification of alkylidene hydrazides as glucagon receptor antagonists.' Med. Chem. (2001) 44:3141–3149.
   Google Scholar
• LING A, PLEWE M, GONZALEZ Jet al.: Human glucagon receptor antagonists based on alkylidene hydrazides. Biorg. Med. Chem. Lett. (2002) 12:663–666.
   Google Scholar
• 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-indo1-4-ylmethylene] hydrazide. I Med. Chem. (2002) 45:5755–5775.
   Google Scholar
• •Manuscript summarises the programme and includes pharmacokinetic and in vivo model results.
   Google Scholar
• LAU J: Discovery of human glucagon receptor antagonists for treatment of Type 2 diabetes. Cordon Conference, Medicinal Chemistry New London, USA (2002).
   Google Scholar
• DE LASZLO SE, HACKER C, LI B et al: Potent orally absorbed glucagon receptor antagonists. Bioorg. Med. Chem. Lett. (1999) 9:641–646.
   PubMed Web of Science ®Google Scholar
• •This letter contains an extensive SAR table detailing the efect of Mg 2+ on glucagon receptor binding. It also compares glucagon receptor binding affinity versus p38 kinase inhibition.
   Google Scholar
• CHANG L, SIDLER KL, CASCIERI MAet al: Substituted imidazoles as glucagon receptor antagonists. Bioorg. Med. Chem. Lett. (2001) 11:2549–2553.
   PubMed Web of Science ®Google Scholar
• LADOUCEUR GH, COOK JH, DOHERTY EM, SCHOEN WR, MACDOUGALL ML, LIVINGSTON JN: Discovery of 5-hydroxyalky1-4-phenylpyridines as a new class of glucagon receptor antagonists. Bioorg. Med. Chem. Lett. (2002) 12:461–464.
   PubMedGoogle Scholar
• SMITH RA, HERTZOG DL, OSTERHOUT MH et al.: Optimization of the 4-aryl group of 4-aryl-pyridine glucagon antagonists: development of an efficient, alternate synthesis. Bioorg. Med. Chem. Lett. (2002) 12:1303–1306.
   PubMedGoogle Scholar
• LIVINGSTON JN, MACDOUGALL M, LADOUCEUR G, SCHOEN W: BAY-27-9955, a novel, non-peptide antagonist of glucagon binding to the glucagon receptor. Diabetes (1999) 48\(Supp1.1):A199.
   Google Scholar
• BJORGE S, JONES L, MAYS R, HILDING H, BRUBAKER W: BAY-27-9955: plasma pharmacolkinetics in sprague-dawley rats following intravenous and oral administration. Diabetes (1999) 48\(Supp1.1):A452.
   Google Scholar
• PETERSEN KF, SULLIVAN JT: Effects of a novel glucagon receptor antagonist (BAY 27-9955) on glucagon-stimulated glucose production in humans. Diabetologia (2001) 44: 2018-2024.
   Google Scholar
• ••Paper describes the results of clinical trials.
   Google Scholar