Structure-guided design of cell wall biosynthesis inhibitors that overcome β-lactam resistance in Staphylococcus aureus (MRSA).

Journal article

β-Lactam antibiotics have long been a treatment of choice for bacterial infections since they bind irreversibly to Penicillin-Binding Proteins (PBPs), enzymes that are vital for cell wall biosynthesis. Many pathogens express drug-insensitive PBPs rendering β-lactams ineffective, revealing a need for new types of PBP inhibitors active against resistant strains. We have identified alkyl boronic acids that are active against pathogens including methicillin-resistant S. aureus (MRSA). The crystal...

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Authors: Contreras-Martel, C; Amoroso, A; Woon, E; Zervosen, A; Inglis, S

• Publication status: Published
• Journal: ACS chemical biology
• Volume: 6
• Issue: 9
• Pages: 943-951
• Publication date: 2011-09-01
• DOI: 10.1021/cb2001846
• EISSN: 1554-8937
• ISSN: 1554-8929
• Language: English
• Keywords: Dose-Response Relationship, Drug; Stereoisomerism; Models, Molecular; Boronic Acids; Structure-Activity Relationship; Drug Design; Anti-Bacterial Agents; Molecular Structure; Staphylococcus aureus; Penicillin-Binding Proteins; beta-Lactam Resistance; beta-Lactams; Cell Wall