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Wiley, Angewandte Chemie, 12(126), p. 3193-3197, 2014

DOI: 10.1002/ange.201310866

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Monitoring conformational changes in the NDM-1 metallo-β-lactamase by <sup>19</sup>F NMR spectroscopy

Journal article published in 2014 by Anna M. Rydzik, Jürgen Brem ORCID, Sander S. Van Berkel, Inga Pfeffer, Anne Makena, Timothy D. W. Claridge, Christopher J. Schofield
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Abstract

The New Delhi metallo-β-lactamase (NDM-1) is involved in the emerging antibiotic resistance problem. Development of metallo-β-lactamases (MBLs) inhibitors has proven challenging, due to their conformational flexibility. Here we report site-selective labeling of NDM-1 with 1,1,1-trifluoro-3-bromo acetone (BFA), and its use to study binding events and conformational changes upon ligand-metal binding using (19) F NMR spectroscopy. The results demonstrate different modes of binding of known NDM-1 inhibitors, including L- and D-captopril by monitoring the changing chemical environment of the active-site loop of NDM-1. The method described will be applicable to other MBLs and more generally to monitoring ligand-induced conformational changes.