Glucagon analogs exhibiting GIP receptor activity
First Claim
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1. A peptide comprising(a) the sequence of SEQ ID NO:
- 28(b) SEQ ID NO;
28 with up to 3 amino acid modifications relative to SEQ ID NO;
28, wherein the peptide exhibits agonist activity at each of the human GIP receptor, the human GLP-1 receptor and the human glucagon receptor.
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Abstract
Provided herein are glucagon analogs which exhibit potent activity at the GIP receptor, and, as such are contemplated for use in treating diabetes and obesity. In exemplary embodiments, the glucagon analog of the present disclosures exhibit an EC50 at the GIP receptor which is within the nanomolar or picomolar range.
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11 Claims
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1. A peptide comprising
(a) the sequence of SEQ ID NO: - 28
(b) SEQ ID NO;
28 with up to 3 amino acid modifications relative to SEQ ID NO;
28, wherein the peptide exhibits agonist activity at each of the human GIP receptor, the human GLP-1 receptor and the human glucagon receptor. - View Dependent Claims (2, 3, 4, 5, 6)
- 28
- 7. A peptide comprising the sequence of SEQ ID NO:
-
11. An analog comprising a parent sequence with a total of up to 3 amino acid modifications relative to the parent sequence, wherein the parent sequence is SEQ ID NO:
- 28, wherein the amino acid modifications are selected from the group consisting of;
a DPP-IV protective amino acid at position 2;
other than AIB, optionally D-Ser;b. a large, aliphatic, nonpolar amino acid at position 12, optionally Ile; c. an amino acid other than Arg at position 17, optionally Gln; d. a small aliphatic amino acid at position 18, other than Ala; e. an amino acid other than Asp at position 21, optionally Glu; f. an amino acid other than Gln at position 24, optionally Asn or Ala; g. an amino acid other than Leu at position 27; h. an amino acid other than Asp at position 28, optionally Ala; and i. an amino acid other than Gly at position 29.
- 28, wherein the amino acid modifications are selected from the group consisting of;
Specification