Designing a leucine‐rich antibacterial nonapeptide with potent activity against mupirocin‐resistant MRSA via a structure–activity relationship study

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Designing a leucine‐rich antibacterial nonapeptide with potent activity against mupirocin‐resistant MRSA via a structure–activity relationship study
Title:
Designing a leucine‐rich antibacterial nonapeptide with potent activity against mupirocin‐resistant MRSA via a structure–activity relationship study
Journal Title:
Chemical Biology & Drug Design
Keywords:
Publication Date:
23 March 2021
Citation:
Ang, Q. A., Arfan, G., Ong, C. Y. F., Ng, F. M., Ong, E. H. Q., & Chia, C. S. B. (2021). Designing a leucine‐rich antibacterial nonapeptide with potent activity against mupirocin‐resistant MRSA via a structure–activity relationship study. Chemical Biology & Drug Design, 97(6), 1185–1193. Portico. https://doi.org/10.1111/cbdd.13840
Abstract:
AbstractStaphylococcus aureus is the main aetiological agent responsible for the majority of human skin infections. Of particular concern is the methicillin‐resistant variety, commonly known as MRSA. The extensive use of the first‐line topical antibiotic of choice, mupirocin, has inevitably resulted in the emergence of resistant strains, signalling an urgent need for the development of new antibacterials with new mechanisms of action. In this work, we describe how we designed a novel cationic nonapeptide, containing only leucine and two lysine residues, with potent anti‐MRSA activity and a rapid bactericidal mode of action. Coupled to a favourable safety profile towards human skin fibroblasts, we believe nonapeptide 11 has high potential for further development as a mupirocin replacement candidate to treat skin infections caused by MRSA.
License type:
Publisher Copyright
Funding Info:
This research is supported by core funding from: Experimental Drug Development Centre (EDDC)
Grant Reference no. : N. A.
Description:
This is the peer reviewed version of the following article: Ang, Q. A., Arfan, G., Ong, C. Y. F., Ng, F. M., Ong, E. H. Q., & Chia, C. S. B. (2021). Designing a leucine‐rich antibacterial nonapeptide with potent activity against mupirocin‐resistant MRSA via a structure–activity relationship study. Chemical Biology & Drug Design, 97(6), 1185–1193. Portico. https://doi.org/10.1111/cbdd.13840, which has been published in final form at 10.1111/cbdd.13840. This article may be used for non-commercial purposes in accordance with Wiley Terms and Conditions for Use of Self-Archived Versions. This article may not be enhanced, enriched or otherwise transformed into a derivative work, without express permission from Wiley or by statutory rights under applicable legislation. Copyright notices must not be removed, obscured or modified. The article must be linked to Wiley’s version of record on Wiley Online Library and any embedding, framing or otherwise making available the article or pages thereof by third parties from platforms, services and websites other than Wiley Online Library must be prohibited.
ISSN:
1747-0285
1747-0277
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