Cell-penetrating peptides (CPPs) are a heterogeneous class of peptides with the ability to translocate across the plasma membrane and to carry attached cargos inside the cell. Two main entry pathways are discussed, as direct translocation and endocytosis , whereas the latter is often favored when bulky cargos are added to the CPP. Attachment to the CPP can be achieved by means of covalent coupling or non-covalent complex formation, depending on the chemical nature of the cargo. Owing to their striking abilities the further development and application of CPP-based delivery strategies has steadily emerged during the past years. However, one main pitfall when using CPPs is their non-selective uptake in nearly all types of cells. Thus, one particular interest lies in the design of targeting strategies that help to circumvent this drawback but still benefit from the potent delivery abilities of CPPs. The following review aims to summarize some of these very recent concepts and to highlight the current role of CPPs in cancer therapy.
Keywords: Cancer targeting; Cancer therapy; Cell-penetrating peptides; Drug delivery; Peptide-drug conjugates.