αvβ6 peptide ligands and their uses

摘要

AVβ6 peptide ligands, functional variants thereof and their nucleic acids encoding them are disclosed with their uses in the treatment and imaging of AVβ6 mediated diseases.

主权项

1. A peptide the amino acid sequence of which consists of BnRGDLX5X6LX8X9X10ZmXi, wherein LX5X6L has an alpha helical structure, Bn is a sequence of n amino acids each of which is any amino acid, X5, X6, X8, X9 and X10 each independently represent any amino acid, each Z is a helix promoting residue independently selected from the group consisting of Glu, Ala, Leu, Met, Gln, Lys, Arg, Val, Ile, Trp, Phe and Asp, Xi, is a sequence of i amino acids each of which is any amino acid, m is at least 1, n is 6 to 7, and n, m and i are selected to make the maximum length of said peptide 20 amino acids, said peptide having a modification selected from the group consisting of:
(i) linkage to at least one non-peptide therapeutically active moiety; (ii) linkage to at least one readily detectable moiety; (iii) linkage to at least one nanoparticle; (iv) linkage to at least one lipid-based vesicle; (v) linkage to at least one capping residue; and (vi) replacement of at least one amino acid residue of said peptide with at least one of a halide derivative thereof or a N or C alkyl substituted form thereof or a combination of said derivative and said substituted form.