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Metallo-β-lactamase inhibitors by bioisosteric replacement: preparation, activity and binding
(Journal article; Tidsskriftartikkel; Peer reviewed, 2017-04-14)
Bacterial resistance is compromising the use of β-lactam antibiotics including carbapenems. The
main resistance mechanism against β-lactams is hydrolysis of the β-lactam ring mediated by
serine- or metallo-β-lactamases (MBLs). Although several inhibitors of MBLs have been
reported, none has been developed into a clinically useful inhibitor. Mercaptocarboxylic acids
are among the most prominent ...
Structural studies of triazole inhibitors with promising inhibitor effects against antibiotic resistance metallo-β-lactamases
(Journal article; Tidsskriftartikkel; Peer reviewed, 2020-06-18)
Metallo-β-lactamases (MBLs) are an emerging cause of bacterial antibiotic resistance by hydrolysing all classes of β-lactams except monobactams, and the MBLs are not inhibited by clinically available serine-β-lactamase inhibitors. Two of the most commonly encountered MBLs in clinical isolates worldwide – the New Delhi metallo-β-lactamase (NDM-1) and the Verona integron-encoded metallo-β-lactamase ...
Structural insights into TMB-1 and the role of residues 119 and 228 in substrate and inhibitor binding
(Journal article; Tidsskriftartikkel; Peer reviewed, 2017-05-30)
Metallo-β-lactamases (MBLs) threaten the effectiveness of β-lactam antibiotics, including carbapenems, and are a concern for global public health. β-Lactam/β-lactamase inhibitor combinations active against class A and class D carbapenemases are used, but no clinically useful MBL inhibitor is currently available. Tripoli metallo-β-lactamase-1 (TMB-1) and TMB-2 are members of MBL subclass B1a, where ...