RGD-based strategies for selective delivery of therapeutics and imaging agents to the tumour vasculature

This review will summarize the structural requirements for RGD-peptides and RGD-mimetics as ligands for αvβ3. We will show how they have been introduced in the various types of constructs by chemical and recombinant techniques. The importance of multivalent RGD-constructs for high affinity binding and internalization will be highlighted. Furthermore the in vitro and in vivo efficacy of RGD-targeted therapeutics and diagnostics reported in recent years will be reviewed.