Glucagon analogs exhibiting physiological solubility and stability
First Claim
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1. A derivative of native glucagon (SEQ ID NO:
- 1) comprising a hydrophilic moiety covalently bound to the amino acid residue at position 24 of the derivative, wherein the amino acid residue at position 24 is an amino acid selected from the group consisting of lysine, cysteine, ornithine, homocysteine, and acetyl phenylalanine, wherein the derivative stimulates activity at the glucagon receptor, and pharmaceutically acceptable salts of said derivative.
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Abstract
Modified glucagon peptides are disclosed having improved solubility and stability, wherein the native glucagon peptide has been modified by pegylation, or the addition of a carboxy terminal peptide selected from the group consisting of SEQ ID NO: 19, SEQ ID NO: 20, SEQ ID NO: 21, or both.
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Citations
19 Claims
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1. A derivative of native glucagon (SEQ ID NO:
- 1) comprising a hydrophilic moiety covalently bound to the amino acid residue at position 24 of the derivative, wherein the amino acid residue at position 24 is an amino acid selected from the group consisting of lysine, cysteine, ornithine, homocysteine, and acetyl phenylalanine, wherein the derivative stimulates activity at the glucagon receptor, and pharmaceutically acceptable salts of said derivative.
- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13)
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14. A derivative of native glucagon (SEQ ID NO:
- 1) comprising a hydrophilic moiety covalently bound to the amino acid residue at position 24 of the derivative, wherein the derivative comprises SEQ ID NO;
1 with an amino acid substitution at position 12 and/or position 27, optionally, wherein the derivative comprises an Arg at position 12 and/or a Leu or Norleucine at position 27, wherein the derivative stimulates activity at the glucagon receptor, and pharmaceutically acceptable salts of said derivative, optionally, wherein the hydrophilic moiety is polyethylene glycol (PEG). - View Dependent Claims (15, 16, 17, 18, 19)
- 1) comprising a hydrophilic moiety covalently bound to the amino acid residue at position 24 of the derivative, wherein the derivative comprises SEQ ID NO;
Specification