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  • Title: Inactivation of beta-lactamases from Enterobacter cloacae by monophosphams.
    Author: Bush K, Smith SA, Tanaka SK, Bonner DP.
    Journal: J Antimicrob Chemother; 1988 Dec; 22(6):801-9. PubMed ID: 3266620.
    Abstract:
    Amongst the monocyclic beta-lactam antibiotics, selected monophosphams were potent mechanism-based inactivators of the P99 and E2 cephalosporinases of Enterobacter cloacae. Inhibition of these enzymes was time-dependent with second order rate constants for inactivation of 100,000 to 20,000,000 l/mol/min. After incubation for 24 h at least 99% of the enzymatic activity was inhibited when enzyme was exposed to a ten-fold excess of inactivator. Amongst the monophosphams three classes of inhibitors were seen: irreversible inactivators as described above, transient inactivators and competitive (inhibitory) substrates.
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