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US 12,187,773 B2Granted
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.
Claims16
A glucose-dependent insulinotropic peptide (GIP) analogue selected from the group consisting of:
- (a) a GIP analogue consisting of the amino acid sequence of SEQ ID NO:
- 1:
- 3 4 5 6 7 8 9 10 11 12 13 14
- X1 - G - T - F - I - S - D - Y - S - I - A - M -
- 15 16 17
- D - R - I
- 18 19 20 21 22 23 24 25 26 27 28 29 30
- X2 - Q - Q - D - F - V - N - W - L - L - A - Q - X3
- wherein said amino acid residue X1 is P, G, A, S, or pyroE (pyroglutamic acid),
- wherein said amino acid X2 is K or Orn, and
- wherein said amino acid X3 is R or E,
- or a functional variant thereof, wherein said functional variant has 1 to 4 individual amino acid substitutions at any one of the amino acid residues at positions 4 to 15, 17 and 19 to 29 of SEQ ID NO:
- 1,
- wherein said amino acid sequence is modified by attaching a fatty acid molecule at the amino acid at position 18 of SEQ ID NO:
- 1 or said functional variant thereof, and wherein said GIP analogue is an antagonist of GIP receptor (GIPR);
- and
- (b) a GIP analogue consisting of the amino acid sequence of SEQ ID NO:
- 11:
- 3 4 5 6 7 8 9 10 11 12 13 14
- X1 - G - T - F - I - S - D - Y - S - I - A - M -
- 15 16 17
- D - R - I
- 18 19 20 21 22 23 24 25 26 27 28 29 30
- X2 - Q - Q - D - F - V - N - W - L - L - A - Q - X3
- wherein said amino acid X2 is K or Orn, and
- wherein said amino acid X3 is R or E,
- or a functional variant thereof having 1 to 4 individual amino acid substitutions at any one of the amino acid residues at positions 4 to 17 and 19 to 29 of SEQ ID NO:
- 11,
- wherein said peptide amino acid sequence is modified by attaching a fatty acid molecule at the amino acid at position 18 of SEQ ID NO:
- 11, or a functional variant thereof, and wherein said GIP analogue is an antagonist of GIPR;
- and
- (c) a GIP analogue consisting of the amino acid sequence of SEQ ID NO:
- 12:
- 3 4 5 6 7 8 9 10 11 12 13 14
- E - G - T - F - I - S - E - Y - S - I - A - M -
- 15 16 17
- E - K - I
- 18 19 20 21 22 23 24 25 26 27 28 29 30
- X2 - Q - Q - E - F - V - Q - W - L - L - A - Q - K
- wherein said amino acid X2 is K or Orn,
- or a functional variant thereof having 1 to 4 individual amino acid substitutions at any one of positions 3 to 30 of SEQ ID NO:
- 12,
- wherein said amino acid sequence is modified by attaching a fatty acid molecule at the amino acid at position 18 of SEQ ID NO:
- 12, or said functional variant thereof, and wherein said GIP analogue is an antagonist of GIPR.
41 more elements
Dependencies are inferred from the claim text.