IMR Press / FBL / Volume 4 / Issue 5 / DOI: 10.2741/A477

Frontiers in Bioscience-Landmark (FBL) is published by IMR Press from Volume 26 Issue 5 (2021). Previous articles were published by another publisher on a subscription basis, and they are hosted by IMR Press on imrpress.com as a courtesy and upon agreement with Frontiers in Bioscience.

Article
Inhibitor resistant class A beta-lactamases
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1 Geriatric CARE Center, Cleveland, OH 44120, USA
2 Department of Medicine, Veterans Affairs Medical Center, Cleveland, Ohio
Front. Biosci. (Landmark Ed) 1999, 4(5), 34–41; https://doi.org/10.2741/A477
Published: 15 May 1999
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.

Keywords
Beta−Lactamase
Suicide Inhibitors
Inhibitor Resistant
TEM (IRT) Beta−Lactamase
Mechanism-Based Inactivators
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