Polypeptide ligands specific for plasma kallikrein
AssigneeBicycleRD Limited
InventorsDaniel Teufel, Catherine Stace, Edward Walker
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Abstract
The present invention relates to polypeptides which are covalently bound to molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold. In particular, the invention describes peptides which are specific for the human and rat protease plasma kallikrein and are modified in one or two peptide loops to enhance potency and/or protease resistance.
Claims42
A peptide ligand specific for plasma kallikrein comprising a polypeptide comprising at least three cysteine residues, separated by at least two loop sequences, and a molecular scaffold which forms covalent bonds with the cysteine residues of the polypeptide such that at least two polypeptide loops are formed on the molecular scaffold, wherein the peptide ligand comprises a peptide sequence of:
- (SEQ ID NO:
- 6)
- -Ci-(N)a-U-J-P-J-R-Cii-V-Y-Y-P-D-I-Ciii-,
- or a modified derivative, or pharmaceutically acceptable salt, thereof;
- wherein:
- Ci, Cii and Ciii represent first, second and third cysteine residues, respectively;
- subscript “a” represents an integer selected from 0 or 1;
- J represents a non-polar aromatic amino acid residue selected from F, W and Y;
- U represents a polar, uncharged amino acid residue selected from N, C, Q, M, S and T.
Dependencies are inferred from the claim text.