Preliminary investigations into developing all-D Omiganan for treating Mupirocin-resistant MRSA skin infections

Preliminary investigations into developing all-D Omiganan for treating Mupirocin-resistant MRSA skin infections
Title:
Preliminary investigations into developing all-D Omiganan for treating Mupirocin-resistant MRSA skin infections
Other Titles:
Chemical Biology and Drug Design
Publication Date:
11 July 2017
Citation:
Ng SMS, Teo SW, Yong YE, et al. Preliminary investigations into developing all-D Omiganan for treating Mupirocin-resistant MRSA skin infections. Chem Biol Drug Des. 2017;00:1–6. https://doi.org/10.1111/cbdd.13035
Abstract:
Staphylococcus aureus is the primary pathogen responsible for the majority of human skin infections and meticillin-resistant Staphylococcus aureus (MRSA) currently presents a major clinical concern. The overuse of Mupirocin, the first-line topical antibacterial drug over 30 years has led to the emergence of Mupirocin-resistant MRSA, creating a clinical concern. The antimicrobial peptide Omiganan was touted to be a promising antibacterial drug candidate due to its rapid membrane-disrupting bactericidal mode of action, entering clinical trials in 2005 as a topical gel to prevent catheter site infections. However, drug development ceased in 2009 due to a lack of efficacy. We postulate this to be due to proteolytic degradation caused by endogenous human skin proteases. Herein, we tested our hypothesis using Omiganan and its all-D enantiomer in a human skin protease stability assay, followed by anti-MRSA activity assay against of a panel of clinical MRSA isolates, a bactericidal/static determination and a time-kill assay to gauge all-D Omiganan's potential for further topical antibacterial drug development.
License type:
PublisherCopyrights
Funding Info:
Agency for Science, Technology and Research (A*STAR) Biomedical Research Council.
Description:
ISSN:
1747-0285
1747-0277
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