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Cytotoxic Peptide Conjugates: Anticancer Therapeutic Strategies

Qian Xiao, Bo Feng, Wei Luo3 and Lichun Sun

Traditional chemotherapeutic agents exhibit potent anticancer efficacy. However, in clinical applications, they also exhibit severely toxic side effects, and result in multidrug resistance (MDR) of cancer cells. So, receptor-targeted therapy is catching more attention of scientists from both academic and industry and recently is coming to the central stage of drug development. Certain peptides, due to their advantages like, easy synthesis and low cost, less or no immunogenicity, stability and high affinity, have been used as drug delivery vehicles. For example, cell-targeting peptides and cell-penetrating peptides (CPPs) in conjugation with cytotoxic agents have elicited remarkable effects. Luteinizing hormone-releasing hormone, somatostatin, and bombesin/gastrinreleasing peptide are the cell-targeting peptides that interact with their cognate surface receptors aberrantly expressed in many cancer cells, so these hormone peptides can be incorporated into cytotoxic agents for cell-specific targeting in cancer chemotherapy. Due to their cell-penetrating ability, CPPs also serve as cytotoxic drug delivery vehicles to carry drugs across the plasma membrane and overcome MDR of cancer cells. Cytotoxic agents linked to cell-targeting peptides and CPPs have been considered as an effective and reliable method in cancer chemotherapy. In this review, we address the applications of these peptides as drug delivery vehicles in targeted anticancer drug development.