An update on β-lactamase inhibitor discovery and development

Antibiotic resistance; Beta-lactamase; Crystal structure; Drug discovery; Inhibitor; Review; Gram negative bacterium; Gram negative infection; Bacterial Proteins; Drug Combinations; Drug Design; Gram-Negative Bacteria; Gram-Negative Bacterial Infections; Molecular Structure; Structure-Activity Relationship

Abstract :

[en] Antibiotic resistance, and the emergence of pan-resistant clinical isolates, seriously threatens our capability to treat bacterial diseases, including potentially deadly hospital-acquired infections. This growing issue certainly requires multiple adequate responses, including the improvement of both diagnosis methods and use of antibacterial agents, and obviously the development of novel antibacterial drugs, especially active against Gram-negative pathogens, which represent an urgent medical need. Considering the clinical relevance of both β-lactam antibiotics and β-lactamase-mediated resistance, the discovery and development of combinations including a β-lactamase inhibitor seems to be particularly attractive, despite being extremely challenging due to the enormous diversity, both structurally and mechanistically, of the potential β-lactamase targets. This review will cover the evolution of currently available β-lactamase inhibitors along with the most recent research leading to new β-lactamase inhibitors of potential clinical interest or already in the stage of clinical development. © 2017 Elsevier Ltd

Disciplines :

Life sciences: Multidisciplinary, general & others
Microbiology
Biochemistry, biophysics & molecular biology

Author, co-author :

Docquier, Jean-Denis ; Université de Liège - ULiège > Département des sciences de la vie > Centre d'ingénierie des protéines

Mangani, S.; Department of Biotechnology, Chemistry and Pharmacy, University of Siena, Via Aldo Moro 2, Siena, 53100, Italy

Language :

English

Title :

An update on β-lactamase inhibitor discovery and development

Publication date :

2018

Journal title :

Drug Resistance Updates

ISSN :

1368-7646

Publisher :

Churchill Livingstone

Volume :

Pages :

13-29

Peer reviewed :

Peer reviewed

Available on ORBi :

since 13 November 2020

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47 (1 by ULiège)

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1 (1 by ULiège)

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Scopus citations^®

165

Scopus citations^®
without self-citations

151

OpenCitations

137

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