Designing a leucine-rich antibacterial nonapeptide with potent activity against mupirocin-resistant MRSA via a structure-activity relationship study
| Autor: | Qi An Ang, Giovinna Arfan, Cheng San Brian Chia, Esther H. Q. Ong, Fui Mee Ng, Chu Yang Fann Ong |
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| Rok vydání: | 2021 |
| Předmět: |
Methicillin-Resistant Staphylococcus aureus
medicine.drug_class Cell Survival Antibiotics Human skin Mupirocin Microbial Sensitivity Tests Skin infection medicine.disease_cause 01 natural sciences Biochemistry Microbiology chemistry.chemical_compound Structure-Activity Relationship Drug Discovery medicine Structure–activity relationship Humans Amino Acid Sequence Mode of action Pharmacology 010405 organic chemistry business.industry Organic Chemistry Fibroblasts medicine.disease 0104 chemical sciences Anti-Bacterial Agents Nanostructures 010404 medicinal & biomolecular chemistry chemistry Staphylococcus aureus Drug Design Molecular Medicine Leucine business Peptides |
| Zdroj: | Chemical biologydrug designREFERENCES. 97(6) |
| ISSN: | 1747-0285 |
| Popis: | Staphylococcus 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. |
| Databáze: | OpenAIRE |
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