Abstract
β-Lactamases threaten the clinical use of carbapenems, which are considered antibiotics of last resort. The classical mechanism of serine carbapenemase catalysis proceeds through hydrolysis of an acyl-enzyme intermediate. We show that class D β-lactamases also degrade clinically used 1β-methyl-substituted carbapenems through the unprecedented formation of a carbapenem-derived β-lactone. β-Lactone formation results from nucleophilic attack of the carbapenem hydroxyethyl side chain on the ester carbonyl of the acyl-enzyme intermediate. The carbapenem-derived lactone products inhibit both serine β-lactamases (particularly class D) and metallo-β-lactamases. These results define a new mechanism for the class D carbapenemases, in which a hydrolytic water molecule is not required.
Original language | English |
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Pages (from-to) | 1282-1285 |
Number of pages | 4 |
Journal | Angewandte Chemie - International Edition |
Volume | 57 |
Issue number | 5 |
Early online date | 5 Jan 2018 |
DOIs | |
Publication status | Published - Jan 2018 |
Keywords
- antibiotics
- carbapenems
- hydrolases
- lactones
- β-lactamases