Journal of Enzyme Inhibition and Medicinal Chemistry

Alarmingly growing bacterial resistance to antibiotics might become one of the most worrying threats to Public Health worldwide. In this context, WHO has published a list of resistant bacteria for which new antibiotics are urgently needed. Main priority concerns Gram-negative opportunistic pathogens responsible of severe nosocomial infections, which are resistant to the invaluable β-lactam antibiotics carbapenems and 3rd generation cephalosporins through the production of β-lactamases (BLs). These carbapenem-hydrolyzing BLs can be separated in two large families according to their catalytic mechanism. They are either serine-hydrolases (SBLs, e.g. KPC-type, OXA-48) or metallo-hydrolases (MBLs, e.g. VIM-, NDM-, IMP- types). Several inhibitors of SBLs only (e.g. avibactam) were recently marketed in association with β-lactam antibiotics, but resistances to these combinations have already been reported. In the case of MBLs, no inhibitor has received FDA approval yet, and only a few compounds are in preclinical or clinical stages (e.g. taniborbactam). Therefore, efforts are still needed to expand the therapeutic arsenal to preserve the precious carbapenems and last-generation cephalosporins.

In contrast, BLs might be exploited in the design of prodrugs or diagnostic tools, thanks to their substrate selectivity and the absence of β-lactam-hydrolysing activity in eukaryotic cells. In this strategy, β-lactam-based molecules undergo fragmentation upon BL cleavage to release either an antibacterial species or a reporter molecule in the bacteria.

The goal of this Article Collection is to provide an overview of the latest advances in BL inhibition and in the exploitation of BLs in targeted antibacterial therapy and diagnostic.

Reviews and original articles from experts in the fields of medicinal chemistry, biochemistry, microbiology, structural biology, biotechnology, and pharmaceutics are welcome.

Subtopics include, but are not limited to: inhibitors of either serine- (SBL) or metallo-b-lactamases (MBL), or both (mixed inhibitors); b-Lactamase-activated antibacterial drugs (prodrug) and b-lactamase-activated probes (diagnostic).

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All manuscripts submitted to this Article Collection will undergo desk assessment and peer-review as part of our standard editorial process. Guest Advisors will not be involved in peer-reviewing manuscripts unless they are an existing member of the Editorial Board.

Please review the journal scope and author submission instructions prior to submitting a manuscript.

The deadline for submitting manuscripts is 30 June 2024.

Please be sure to select the Article Collection ‘β-Lactamases in Antibacterial Therapy and Diagnostics’ from the drop-down menu in the submission system.

Please contact Sam Zhang at [email protected] with any queries regarding this Article Collection.