PMID: 2494991Feb 15, 1989Paper

Clavulanate inactivation of Staphylococcus aureus beta-lactamase

The Biochemical Journal
I RizwiR Virden

Abstract

The interaction of clavulanic acid with beta-lactamase from Staphylococcus aureus was investigated, particularly with a view to determining whether conformational effects are involved. The inactivation at neutral pH is essentially stoichiometric, leading to an inactive species with an enamine chromophore. Two forms of the enamine were observed, the first-formed having a positive ellipticity with a maximum near 290 nm. This species slowly converted into the stable form of the inactivated enzyme that had a negative ellipticity with a minimum at 275 nm. This change in sign of the ellipticity of the enamine is consistent with the previously proposed cis-trans isomerization of the enamine [Cartwright & Coulson (1979) Nature (London) 278, 360-361). Both the far-u.v.c.d. and the intrinsic viscosity of the inactivated enzyme indicated that negligible change in conformation of the enzyme accompanied inactivation. The rates of inactivation and enamine formation were compared at low temperatures, where the initial rates were slow enough to be monitored. The rate of loss of 95% of the catalytic activity was almost 100-fold faster than the rate of formation of the first-formed enamine species. The remaining 5% activity was lost with a rate ...Continue Reading

Citations

Aug 1, 1997·Natural Product Reports·K H BaggaleyC J Schofield
Nov 22, 1993·FEBS Letters·D Monnaie, J M Frere
Jan 12, 2011·Antimicrobial Agents and Chemotherapy·Hilary FraseSergei B Vakulenko
Jan 13, 2010·Clinical Microbiology Reviews·Sarah M Drawz, Robert A Bonomo
Feb 25, 2011·The Journal of Biological Chemistry·Hilary FraseSergei B Vakulenko
Aug 5, 1997·Chemical Reviews·Robert E. Babine, Steven L. Bender
Aug 11, 2001·Drug Resistance Updates : Reviews and Commentaries in Antimicrobial and Anticancer Chemotherapy·Malcolm G. P. Page

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