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Updated: Aug 20, 2026

The Use of a β-lactamase-based Conductimetric Biosensor Assay to Detect Biomolecular Interactions
Published on: February 1, 2018
Metallo-beta-lactamase inhibitors: promise for the future?
Jeffrey H Toney1, Joseph G Moloughney
1Montclair State University, Department of Chemistry and Biochemistry, Richardson Hall, Room 352, 1 Normal Avenue, Upper Montclair, NJ 07043, USA. toneyje@mail.montclair.edu
Abstract:
Carbapenem resistance continues to erode the effectiveness of antibiotics such as imipenem and meropenem in the clinic. Resistance mechanisms can include interplay between porin loss (membrane permeability), mutation of penicillin binding proteins necessary for cell division, and expression of class A, B and D beta-lactamases. Bacterial resistance to beta-lactams such as penicillin or amoxicillin has been overcome in the clinic using several strategies, including development of antibiotics not susceptible to hydrolysis by beta-lactamases, or co-administration of the antibiotic with beta-lactamase inhibitors. This overview will focus on progress since 2000 in identifying inhibitors of class B, or metallo-beta-lactamases with the aim of reversing carbapenem resistance.
Insights
Carbapenem resistance threatens antibiotic effectiveness. This review highlights progress in developing metallo-beta-lactamase inhibitors to combat resistance, focusing on advancements since 2000.
Area of Science:
- Microbiology
- Infectious Diseases
- Drug Discovery
Background:
- Carbapenem antibiotics, including imipenem and meropenem, are losing effectiveness due to rising bacterial resistance.
- Resistance mechanisms involve porin loss, penicillin-binding protein mutations, and beta-lactamase enzyme activity (Classes A, B, D).
- Existing strategies to combat beta-lactam resistance include developing hydrolysis-resistant antibiotics and using beta-lactamase inhibitors.
Purpose of the Study:
- To review progress in identifying inhibitors targeting class B metallo-beta-lactamases (MBLs) since 2000.
- To explore strategies for reversing carbapenem resistance mediated by MBLs.
Main Methods:
- Literature review of scientific publications from 2000 onwards.
- Focus on research related to metallo-beta-lactamase inhibitors and carbapenem resistance mechanisms.
Main Results:
- Significant research efforts have been directed towards developing MBL inhibitors.
- Identification of various chemical scaffolds and strategies for MBL inhibition.
Conclusions:
- Developing effective metallo-beta-lactamase inhibitors is crucial for restoring carbapenem efficacy.
- Continued research is needed to translate inhibitor discoveries into clinical applications for combating carbapenem resistance.
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