Glucagon analogs with serine replacements

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

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Details

530308, A61K 3826, C07K 1400, C07K 14605

Patent

active

054808677

ABSTRACT:
Glucagon analogs characterized principally by the removal or replacement of the 9-aspartic acid residue or its replacement with another amino acid residue together with replacement of the 16-serine residue and possible replacement of the 11-serine residue and 21-aspartic acid residue with or without a histidine at the amino terminal are useful adjuncts to insulin therapy.

REFERENCES:
patent: 4879273 (1989-11-01), Merrifield
patent: 5143902 (1992-09-01), Merrifield et al.
Unson et al., 1994, "Multiple-site replacement analogs of glucagon. A molecular basis for antagonists design", J. Biol. Chem 269:12548-51.
Unson and Merrifield, 1994, "Identification of an essential serine residue in glucagon: Implication for an active site triad", Proc. Natl. Acad. Sci USA 91:454-58.
Unson et al., 1993, "The role of histidine-1 in glucagon action", Arch. Biochem. Biophys. 300:747-50.
Unson et al., 1991, "Position 9 replacement analogs of glucagon uncouple biological activity and receptor binding", J. Biol. Chem. 266:2763-66.
Unson et al., 1989, "Glucagon antagonists: contribution to binding and activity of the amino-terminal sequence 1-5, position 12, and the putative alpha-helical segment 19-27", J. Biol. Chem. 264:789-94.

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