RGD-containing peptidomimetics and uses thereof

摘要

The invention provides RGD-containing cyclic peptidomimetics; conjugates of said peptidomimetics and a moiety of a payload selected from fluorescent probes, photosensitizers, chelating agents, or cytotoxic agents; and pharmaceutical compositions comprising these conjugates. The conjugates of the invention are useful both for diagnostic purposes and treatment of various diseases, disorders and conditions. More specifically, conjugates comprising fluorescent probes can be used for diagnostic purposes, e.g., visualization of organs and tissues, and diagnosis of tumors; conjugates comprising photosensitizers can be used for photodynamic therapy of both tumors and nonneoplastic tissues; conjugates comprising chelating agents can be used in radioimaging or radiotherapy; and conjugates comprising cytotoxic agents can be used for targeted chemotherapy.

主权项

1. An arginine-glycine-aspartic acid (RGD)-containing cyclic peptidomimetic of the general formula II: wherein A1 is a natural or non-natural amino acid residue bearing either an amino or carboxyl group on its side chain, linked via its α- or side chain carboxyl group to the α-amino group of the arginine residue and via its α- or side chain amino group to the backbone C═O; A2 is a natural or non-natural amino acid residue linked via its α-amino group to the backbone C═O and via its α-carboxyl group to the α- or side chain amino group of A3; and A3 is a natural or non-natural amino acid residue bearing an amino group on its side chain and amidated at its C-terminus, linked via one of its α- or side chain amino group to the carboxyl group of A2 and via another of its α- or side chain amino group to the α-carboxyl group of the aspartic acid residue.