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A protein structure-guided covalent scaffold selectively targets the B1 and B2 subclass metallo-β-lactamases

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Abstract

We report the discovery of ebselen-based dual covalent inhibitors of metallo-β-lactamases. Fluorescence and MALDI-TOF analysis suggested that the scaffold could bind to NDM-1 by forming a S–Se bond with Cys221 and an amide bond with Lys224 of NDM-1, thereby exhibiting selective inhibition and labeling against B1 and B2 subclass enzymes in vitro and in vivo.

Graphical abstract: A protein structure-guided covalent scaffold selectively targets the B1 and B2 subclass metallo-β-lactamases

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Publication details

The article was received on 07 Feb 2018, accepted on 16 Apr 2018 and first published on 16 Apr 2018


Article type: Communication
DOI: 10.1039/C8CC01067F
Citation: Chem. Commun., 2018, Advance Article
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    A protein structure-guided covalent scaffold selectively targets the B1 and B2 subclass metallo-β-lactamases

    C. Chen, Y. Xiang, K. Yang, Y. Zhang, W. Wang, J. Su, Y. Ge and Y. Liu, Chem. Commun., 2018, Advance Article , DOI: 10.1039/C8CC01067F

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