Description
MAC-545496 (838810-96-1) is an inhibitor of glycopeptide-resistance-associated protein R (GraR, also known as ApsR).? GraR and its regulatory system are important for virulence of S. aureus.? MAC-545496 is able to reverse ?-lactam resistance in S. aureus in a G. Mellonella larvae model.? 0.06 μg/mL MAC-545496? lowered the minimum inhibitory concentration (MIC) for oxacillin against S. aureus below the CLSI clinical breakpoint. It lowered the ?-lactam MIC from 512 to 8 μg/mL against S. aureus USA300.
References
El-Halfawy et al. (2020), Discovery of an antivirulence compound that reverses ?-lactam resistance in MRSA; Nat. Chem. Biol., 16 143
