RGD-mediated delivery of small-molecule drugs.

Conjugates of cytotoxic agents with RGD peptides (Arg-Gly-Asp) addressed to αβ, αβ and αβ integrin receptors overexpressed by cancer cells, have recently gained attention as potential selective anticancer chemotherapeutics. In this review, the design and the development of RGD conjugates coupled to different small molecules including known cytotoxic drugs and natural products will be discussed.