MAC-545496 is a potent and selective inhibitor of glycopeptide-resistance-associated protein R (GraR) that displays antivirulence and antimicrobial adjuvant properties. MAC-545496 reverses β-lactam resistance in Methicillin-resistant strains (MRSA) and synergizes with cationic antimicrobial peptides (CAMPs). It also potentiates the effects of Cefuroxime and Oxacillin MRSA strains. MAC-545496 has no effect on commensal S. epidermidis and Gram-negative bacteria such as P. aeruginosa.
potent and selective inhibitor of glycopeptide-resistance-associated protein R (GraR); antivirulent, antibacterial
Nature chemical biology, 16(2), 143-149 (2019-11-27)
Staphylococcus aureus is the leading cause of infections worldwide, and methicillin-resistant strains (MRSA) are emerging. New strategies are urgently needed to overcome this threat. Using a cell-based screen of ~45,000 diverse synthetic compounds, we discovered a potent bioactive, MAC-545496, that
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