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  • Title: Beta-lactamase inactivation by mechanism-based reagents.
    Author: Fisher J, Belasco JG, Charnas RL, Khosla S, Knowles JR.
    Journal: Philos Trans R Soc Lond B Biol Sci; 1980 May 16; 289(1036):309-19. PubMed ID: 6109326.
    Abstract:
    The mechanistic pathway followed by the E. coli RTEM beta-lactamase has been studied with a view to clarifying the mode of action of a number of recently discovered inactivators of the enzyme. There is clear evidence that the beta-lactamase-catalysed hydrolysis of the 7-alpha-methoxycephem, cefoxitin, proceeds via an acyl-enzyme intermediate. An analysis of the inactivation reactions of all the known beta-lactam derivatives that result in irreversible loss of enzyme activity permits the identification of three structural features required for a beta-lactamase inactivator. The application of these principles suggests a new group of mechanism-based inactivators of the enzyme: the sulphones of N-acyl derivatives of 6-beta-aminopenicillanic acid that are themselves poor substrates for the enzyme. These sulphones are powerful inactivators of the beta-lactamase.
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