High-throughput screen with the <scp>l,d</scp>-transpeptidase Ldt<sub>Mt2</sub> of <i>Mycobacterium tuberculosis</i> reveals novel classes of covalently reacting inhibitors
Mariska de Munnik, Pauline A. Lang, Francisco De Dios Anton, Mónica Cacho, Robert H. Bates, Jürgen Brem, Beatriz Rodríguez-Miquel, Christopher J. Schofield
Abstract
10 000 electrophilic compounds were screened for inhibition of the essential l,d -transpeptidase (Ldt Mt2 ) of Mycobacterium tuberculosis . Potent covalently reacting inhibitors were identified and characterised by protein X-ray and MS studies.
Topics & Concepts
Mycobacterium tuberculosisCovalent bondChemistryElectrophileTuberculosisBiochemistryStereochemistryMicrobiologyBiologyOrganic chemistryMedicineCatalysisPathologyPeptidase Inhibition and AnalysisBiochemical and Molecular ResearchTuberculosis Research and Epidemiology