Journal
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 53, Issue 12, Pages 3129-3133Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201310866
Keywords
F-19-NMR; antibiotic resistance; captopril; metallo--lactamases; NDM-1
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Funding
- Medical Research Council (MRC)/Canadian Grant [G1100135]
- Biotechnology and Biological Sciences Research Council (BBSRC)
- Cancer Research UK (CRUK)
- Dulverton Trust
- Rhodes Trust
- Medical Research Council [G1100135] Funding Source: researchfish
- MRC [G1100135] Funding Source: UKRI
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The New Delhi metallo--lactamase (NDM-1) is involved in the emerging antibiotic resistance problem. Development of metallo--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 (FNMR)-F-19 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.
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