The Use of Therapeutic Peptides to Target and to Kill Cancer Cells

R.      J. Boohaker; M.      W. Lee; P.      Vishnubhotla; J.L.      M. Perez; A.      R. Khaled

doi:10.2174/092986712801661004

Abstract

Peptide therapeutics is a promising field for emerging anti-cancer agents. Benefits include the ease and rapid synthesis of peptides and capacity for modifications. An existing and vast knowledge base of protein structure and function can be exploited for novel peptide design. Current research focuses on developing peptides that can (1) serve as tumor targeting moieties and (2) permeabilize membranes with cytotoxic consequences. A survey of recent findings reveals significant trends. Amphiphilic peptides with clusters of hydrophobic and cationic residues are features of anti-microbial peptides that confer the ability to eradicate microbes and show considerable anti-cancer toxicity. Peptides that assemble and form pores can disrupt cell or organelle membranes and cause apoptotic or necrotic death. Cell permeable and tumor-homing peptides can carry biologically active cargo to tumors or tumor vasculature. The challenge lies in developing the clinical application of therapeutic peptides. Improving delivery to tumors, minimizing non-specific toxic effects and discerning pharmacokinetic properties are high among the needs to produce a powerful therapeutic peptide for cancer treatment.

Keywords: Tumor-targeting, membrane, anti-microbial, Bcl-2 family, apoptosis, necrosis, cell-penetrating, mitochondria, cytotoxicity, vasculature