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Issue 6, 2019
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Rational design of novel amphipathic antimicrobial peptides focused on the distribution of cationic amino acid residues

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Abstract

Antimicrobial peptides (AMPs) have garnered much attention as novel therapeutic agents against infectious diseases. They exhibit antimicrobial activity through microbial membrane disruption based on their amphipathic properties. In this study, we rationally designed and synthesized a series of novel AMPs Block, Stripe, and Random, and revealed that Stripe exhibits potent antimicrobial activity against Gram-positive and Gram-negative microbes. Moreover, we also demonstrated that Stripe disrupts both Gram-positive and Gram-negative mimetic bacterial membranes. Finally, we investigated the hemolytic activity and cytotoxicity in human blood cells and human cell lines, and found that Stripe exhibited neither. These data indicated that Stripe is a promising antimicrobial reagent that does not display significant cytotoxicity.

Graphical abstract: Rational design of novel amphipathic antimicrobial peptides focused on the distribution of cationic amino acid residues

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Supplementary files

Article information


Submitted
19 Mar 2019
Accepted
03 Apr 2019
First published
04 Apr 2019

Med. Chem. Commun., 2019,10, 896-900
Article type
Research Article

Rational design of novel amphipathic antimicrobial peptides focused on the distribution of cationic amino acid residues

T. Misawa, C. Goto, N. Shibata, M. Hirano, Y. Kikuchi, M. Naito and Y. Demizu, Med. Chem. Commun., 2019, 10, 896
DOI: 10.1039/C9MD00166B

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