Chemical Biology & Drug Design · 2018 · 11 citations · 24 references
Staphylococcus aureus is the pathogen responsible for the majority of human skin infections. In particular, the methicillin-resistant variety, MRSA, has become a global clinical concern. The extensive use of mupirocin, the first-line topical antibacterial drug of choice, has led to the emergence of mupirocin-resistant MRSA globally, resulting in the urgent need for a replacement. Antimicrobial peptides are deemed plausible candidates. Herein, we describe a structure-activity relationship approach in the design of an ultra-short peptide with potent anti-MRSA activity with a rapid, bactericidal mode of action. Coupled to a low cytotoxic activity, we believe our lead compound can be developed into a topical antibacterial agent to replace mupirocin as the first-line drug for treating MRSA skin infections.
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Antimicrobial peptides of multicellular organisms
Michael Zasloff · Nature · 2002 · 8.3K citations
Peptoids that mimic the structure, function, and mechanism of helical antimicrobial peptides
Nathaniel P. Chongsiriwatana, James A. Patch, Ann M. Czyzewski et al. · Proceedings of the National Academy of Sciences · 2008 · 632 citations · Full text
Medicinal Chemistry, Antimicrobial Drug Discovery, Biochemistry +15