Article
Disruption of allosteric response as an unprecedented mechanism of resistance to antibiotics.
Journal of the American Chemical Society - 16 Jul 2014
Fishovitz Jennifer, Rojas-Altuve Alzoray, Otero Lisandro H, Dawley Matthew, Carrasco-López Cesar, Chang Mayland, Hermoso Juan A, Mobashery Shahriar
Abstract excerpt
Ceftaroline, a recently approved β-lactam antibiotic for treatment of infections by methicillin-resistant Staphylococcus aureus (MRSA), is able to inhibit penicillin-binding protein 2a (PBP2a) by triggering an allosteric conformational change that leads to the opening of the active site. The opened active site is now vulnerable to inhibition by a second molecule of ceftaroline, an event that impairs cell-wall...
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