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LY2183240 regioisomers act as competitive and selective inhibitors of class C β-lactamases

de Resende, Pedro Ernesto; Soares, Sarah; Zloh, Mire; Gibbons, Simon; Stapleton, Paul; (2023) LY2183240 regioisomers act as competitive and selective inhibitors of class C β-lactamases. International Journal of Antimicrobial Agents , 61 (5) , Article 106774. 10.1016/j.ijantimicag.2023.106774. Green open access

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Abstract

The regioisomers of the anandamide-acting drug LY2183240 exhibited specific potent and competitive inhibitory activities against class C β-lactamases. More explicitly, the 1,5- and 2,5-regioisomers inhibited AmpC from Enterobacter hormaechei (formerly Enterobacter cloacae) with Ki values of 1.8 µM and 2.45 µM, respectively. Structural molecular modelling studies revealed the interaction of the regioisomers with the relevant residues of the catalytic site of cephalosporinase from E. hormaechei P99, which included Tyr150, Lys315 and Thr316.

Type: Article
Title: LY2183240 regioisomers act as competitive and selective inhibitors of class C β-lactamases
Open access status: An open access version is available from UCL Discovery
DOI: 10.1016/j.ijantimicag.2023.106774
Publisher version: https://doi.org/10.1016/j.ijantimicag.2023.106774
Language: English
Additional information: This version is the author accepted manuscript. For information on re-use, please refer to the publisher’s terms and conditions.
Keywords: LY2183240, Tetrazole, β-lactamases, Competitive inhibitor, Antimicrobial resistance
UCL classification: UCL
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy
URI: https://discovery.ucl.ac.uk/id/eprint/10166696
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