The urgent need for metallo-β-lactamase inhibitors: an unattended global threat

MF Mojica, MA Rossi, AJ Vila… - The Lancet Infectious …, 2022 - thelancet.com
… The β-lactamase genes (bla genes) encoding subclass B1 metallo-β-lactamases are
largely plasmid-borne and are of greater clinical relevance compared with metallo-β-lactamase

Metallo-β-lactamase-mediated antimicrobial resistance and progress in inhibitor discovery

Y Yang, YH Yan, CJ Schofield, A McNally, Z Zong… - Trends in …, 2023 - cell.com
… Here we review the classification, structures, substrate profiles, and inhibition mechanisms
of MBLs, highlighting current clinical problems due to MBL-mediated resistance and progress …

Inhibiting the metallo-β-lactamases: Challenges and strategies to overcome bacterial β-lactam resistance

MA Jeffs, CT Lohans - Future Medicinal Chemistry, 2022 - Taylor & Francis
… Delhi metallo-β-lactamase-1 (NDM-1), imipenemase-1 (IMP-1) and Verona integron-encoded
metallo-β-lactamase-2 … Cephalosporins inhibit human metallo β-lactamase fold DNA repair …

Metallo-β-lactamases in the age of multidrug resistance: from structure and mechanism to evolution, dissemination, and inhibitor design

G Bahr, LJ Gonzalez, AJ Vila - Chemical reviews, 2021 - ACS Publications
… Because the first solved structure of this superfamily was BcII, the metallo-β-lactamase from
B. cereus by Carfi, Dideberg, and co-workers, (217) it is known as the MBL fold. The large …

Metallo-β-lactamase inhibitors inspired on snapshots from the catalytic mechanism

AR Palacios, MA Rossi, GS Mahler, AJ Vila - Biomolecules, 2020 - mdpi.com
… -lactam antibiotics, and no clinically useful inhibitors against them have yet been approved.
mechanism with similar reaction species. Here, we describe a number of MBL inhibitors that …

Recent advances in β-lactamase inhibitor chemotypes and inhibition modes

R Li, X Chen, C Zhou, QQ Dai, L Yang - European journal of medicinal …, 2022 - Elsevier
… -spectrum MBLs and SBLs inhibitors to combat rapidly growing β… inhibitor chemotypes and
their inhibition mechanisms. The common pharmacophore features of MBL and SBL inhibitors

Metallo-β-lactamases: structure, function, epidemiology, treatment options, and the development pipeline

SE Boyd, DM Livermore, DC Hooper… - Antimicrobial agents …, 2020 - Am Soc Microbiol
Metallo-β-lactamase (MBL) enzymes are a particular concern and are increasingly …
Nonboronate inhibitors face toxicity issues, particularly if they interact with other metalloenzymes or …

Biochemical exploration of β-lactamase inhibitors

V Arer, D Kar - Frontiers in Genetics, 2023 - frontiersin.org
… the metallo-β-lactamase, while the rest are serine β-lactamases. The clinical use of β-lactamase
inhibitors began … researchers address root issues and develop more effective inhibitors. …

Imitation of β-lactam binding enables broad-spectrum metallo-β-lactamase inhibitors

J Brem, T Panduwawala, JU Hansen, J Hewitt… - Nature Chemistry, 2022 - nature.com
… In the meantime, to ensure continued support, we are displaying the site without styles and
… MBL inhibition is challenging because of the structural diversity in MBL active sites (Fig. 1b) …

Designing inhibitors of β-lactamase enzymes to overcome carbapenem resistance in Gram-negative bacteria

DT Davies, M Everett - Accounts of Chemical Research, 2021 - ACS Publications
… encountered and solved a range of issues. For example, in the MBL inhibitor series we were
able to … campaign resulting in the discovery of the metallo-β-lactamase inhibitor ANT2681. …