Scheme 1.

Cooperation of a targeting moiety known for a highly selective interaction with the target of interest and the anti-tumor effect of a therapeutic moiety is the basis of active targeting in cancer therapy. Thus, maximal efficiency and minimal off-targeting of such systems can be achieved. Examples of targets involved in the development of such anti-cancer formulations and their targeting ligands are partially described in this review and are given in the left part of the scheme. Examples of small-molecule cancer drugs, therapeutic nanoparticles, and bioactive proteins are given in the right part of the scheme. This review is mainly focused on integrin-binding peptides in combination with liposomes, gold and magnetic nanoparticles as the therapeutic agent of choice.