Abstract |
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.
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Authors | Hung-Lun Chu, Bak-Sau Yip, Kuan-Hao Chen, Hui-Yuan Yu, Ya-Han Chih, Hsi-Tsung Cheng, Yu-Ting Chou, Jya-Wei Cheng |
Journal | PloS one
(PLoS One)
Vol. 10
Issue 5
Pg. e0126390
( 2015)
ISSN: 1932-6203 [Electronic] United States |
PMID | 25970292
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Anti-Bacterial Agents
- Antibiotics, Antineoplastic
- Antimicrobial Cationic Peptides
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Topics |
- Animals
- Anti-Bacterial Agents
(pharmacology)
- Antibiotics, Antineoplastic
(pharmacology)
- Antimicrobial Cationic Peptides
(pharmacology)
- Apoptosis
- Cell Line, Tumor
- Escherichia coli
(drug effects)
- Humans
- Lung Neoplasms
(drug therapy)
- Male
- Mice, Inbred BALB C
- Mice, Nude
- Microbial Sensitivity Tests
- Pseudomonas aeruginosa
(drug effects)
- Staphylococcus aureus
(drug effects)
- Xenograft Model Antitumor Assays
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