Monitoring conformational changes in the NDM-1 metallo-ß-lactamase by 19Fâ
NMR spectroscopy.
Angew Chem Int Ed Engl
; 53(12): 3129-33, 2014 Mar 17.
Article
em En
| MEDLINE
| ID: mdl-24615874
ABSTRACT
The New Delhi metallo-ß-lactamase (NDM-1) is involved in the emerging antibiotic resistance problem. Development of metallo-ß-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) Fâ
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.
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Beta-Lactamases
/
Espectroscopia de Ressonância Magnética
Idioma:
En
Ano de publicação:
2014
Tipo de documento:
Article