Inhibitor resistant class A beta-lactamases

Front Biosci. 1999 May 15:4:e34-41. doi: 10.2741/A477.

Abstract

Beta-lactamase inhibitors (clavulanic acid, tazobactam, and sulbactam) greatly enhance the therapeutic efficacy of their partner antibiotics (amoxacillin, ampicillin, piperacillin, and ticarcillin) against common enteric and non-enteric organisms possessing class A beta-lactamases. Unfortunately, the number of class A enzymes being discovered that are resistant to these combinations is increasingly rapidly. The TEM and SHV class A beta-lactamases resistant to inhibitors have point mutations in critical amino acids important for catalysis. Compared to the wild type beta-lactamase, inhibitor resistant enzymes are inefficient at hydrolyzing benzylpenicillin, aminopenicillins, and cephalosporins. Nevertheless, hyper-production of these enzymes resulting from mutations in the promoter region can confer substantial levels of resistance. Understanding the microbiologic and kinetic properties of these inhibitor resistant class A beta-lactamases can lead to the design of more potent beta-lactam compounds as well as more effective inhibitors.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.
  • Review

MeSH terms

  • Amino Acid Substitution
  • Cephalosporins / pharmacology
  • Drug Resistance, Microbial / genetics
  • Enzyme Inhibitors / pharmacology*
  • beta-Lactamase Inhibitors
  • beta-Lactamases* / classification
  • beta-Lactamases* / genetics
  • beta-Lactamases* / metabolism

Substances

  • Cephalosporins
  • Enzyme Inhibitors
  • beta-Lactamase Inhibitors
  • beta-Lactamases