Modified GIP peptide analogues
AssigneeAntag Therapeutics ApS
InventorsAlexander Hovard Sparre-Ulrich, Bjørn Behrens Sivertsen, Ditte Riber, Mette Marie Rosenkilde
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Abstract
Disclosed are glucose-dependent insulinotropic peptide (GIP)-derived peptide analogues which are antagonists of the GIP receptor. These GIP peptide analogues are modified by comprising one or more individual amino acid substitutions and are fatty acid conjugated with/without a linker, so to have improved antagonistic activity and improved pharmacokinetic profile.
Claims17
A glucose-dependent insulinotropic peptide (GIP) analogue consisting of the amino acid sequence of SEQ ID NO:
- 81:
- (SEQ ID NO:
- 81)
- 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17
- E - G - T - F - I - S - E - Y - S - I - Aib - L - E - K - I
- 18 19 20 21 22 23 24 25 26 27 28 29 30
- K - Q - Q - E - F - V - E - W - L - L - A - Q - K - Z,
- wherein said amino acid sequence is modified by attaching a fatty acid molecule at one or more amino acid residue, directly or via a linker, at any one of positions 3 to 29 of SEQ ID NO:
- 81,
- wherein Z is a peptide of one or more amino acid residues of GIP(31-42) (GKKNDWKHNITQ;
- SEQ ID NO:
- 2) or wherein Z is a peptide of one or more amino acid residues of Exendin-4 (HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS;
- SEQ ID NO:
- 3),
- wherein said amino acid sequence is optionally C-terminally amidated (—NH2) or C-terminally carboxylated (—COOH), and
- wherein said GIP analogue is an antagonist of GIPR.
A method of treating obesity in a subject, wherein said method comprises administering to the subject the GIP analogue
- EGTFISEYSIAibLEKIKQQEFVEWLLAQKPSSGAPPPS-C16-diacid/18K;
- SEQ ID NO:
- 174 GIP(3-30)+Cex(31-39), wherein said GIP analogue is C-terminally carboxylated.
Dependencies are inferred from the claim text.