Mitochondria-Penetrating Peptide (MPP) for Hydrophobic Drug or dye Conjugate (MPDC) for efficient antitumor therapy

Abstract

Recently, targeting mitochondria is a promising strategy to improve chemotherapy efficiency by reducing side effects. Mitochondria penetrating peptide (MPP) has been worked to offer highly efficient gene or drug delivery. Most MPPs consist of alternative positive charged amino acids such as arginine (R) and lysine (K) and liphophilic amino acids such as phenylalanine (F) or cyclohexylalanine.(Fx). In here, mitochondria targeting peptide can be achieved with hydrophobic drug or dye acted as liphophilic amino acids. These mitochondria targeting peptides which are short and highly positive peptides with anticancer drug, camptothecin (CPT) and IR-780 has been synthesized in which the CPT and IR-780 are conjugated to peptide via thiol functional group of cysteine in peptide. It can self-assemble into nanostructure in water. First, the mitochondria targeting peptide containing IR-780 can be used for NIR imaging and photothermal therapy with laser irradiation and mitochondria targeting drug can be released via disulfide bond based on intracellular GSH concentration. These short peptides conjugated to drug exhibited target specific toxicity with antitumor efficiency also the dye conjugated peptides showed target tumor toxicity with photothermal therapy.