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Therapeutic peptides are attracting increasing attention for biomedical applications. Peptides present promising opportunities in targeted drug delivery due to their high specificity, selectivity, small dimensions, ease of modification, and high biocompatibility. During the last decade, the potential of peptides as therapeutics or targeting ligands has been boomed in nanotechnology and cancer research.

This review summarizes various peptides as therapeutics and targeting ligands in cancer therapy. At first, two categories of tumor homing and cell penetrating peptides (CPPs) are introduced and then we will discuss the modification of CPPs. Then various types of tumor targeting peptides and their applications in cancer research are represented.