Targeting of peptide‐binding receptors on cancer cells with peptide‐drug conjugates

Abstract Specifically addressing cell surface molecules on cancer cells facilitates targeted cancer therapies that offer the potential to selectively destroy malignant cells, while sparing healthy tissue. Thus, undesired side‐effects in tumor patients are highly reduced. Peptide‐binding receptors are frequently overexpressed on cancer cells and therefore promising targets for selective tumor therapy. In this review, peptide‐binding receptors for anti‐cancer drug delivery are summarized with a focus on peptide ligands as delivery agents. In the first part, some of the most studied peptide‐binding receptors are presented, and the ghrelin receptor and the Y 1 receptor are introduced as more recent targets for cancer therapy. Furthermore, nonpeptidic small molecules for receptor targeting on cancer cells are outlined. In the second part, peptide conjugates for the delivery of therapeutic cargos in cancer therapy are described. The essential properties of receptor‐targeting peptides are specified, and recent developments in the fields of classical peptide‐drug conjugates with toxic agents, radiolabeled peptides for radionuclide therapy, and boronated peptides for boron neutron capture therapy are presented.