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Novel Antimicrobial Peptides with High Anticancer Activity and Selectivity

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posted on 2015-05-13, 04:28 authored by Hung-Lun Chu, Bak-Sau Yip, Kuan-Hao Chen, Hui-Yuan Yu, Ya-Han Chih, Hsi-Tsung Cheng, Yu-Ting Chou, Jya-Wei Cheng

We describe a strategy to boost anticancer activity and reduce normal cell toxicity of short antimicrobial peptides by adding positive charge amino acids and non-nature bulky amino acid β-naphthylalanine residues to their termini. Among the designed peptides, K4R2-Nal2-S1 displayed better salt resistance and less toxicity to hRBCs and human fibroblast than Nal2-S1 and K6-Nal2-S1. Fluorescence microscopic studies indicated that the FITC-labeled K4R2-Nal2-S1 preferentially binds cancer cells and causes apoptotic cell death. Moreover, a significant inhibition in human lung tumor growth was observed in the xenograft mice treated with K4R2-Nal2-S1. Our strategy provides new opportunities in the development of highly effective and selective antimicrobial and anticancer peptide-based therapeutics.