Ontology highlight
ABSTRACT:
SUBMITTER: Richter A
PROVIDER: S-EPMC6128881 | biostudies-literature | 2018 Sep
REPOSITORIES: biostudies-literature
Richter Adrian A Rudolph Ines I Möllmann Ute U Voigt Kerstin K Chung Chun-Wa CW Singh Onkar M P OMP Rees Michael M Mendoza-Losana Alfonso A Bates Robert R Ballell Lluís L Batt Sarah S Veerapen Natacha N Fütterer Klaus K Besra Gurdyal G Imming Peter P Argyrou Argyrides A
Scientific reports 20180907 1
Nitro-substituted 1,3-benzothiazinones (nitro-BTZs) are mechanism-based covalent inhibitors of Mycobacterium tuberculosis decaprenylphosphoryl-β-D-ribose-2'-oxidase (DprE1) with strong antimycobacterial properties. We prepared a number of oxidized and reduced forms of nitro-BTZs to probe the mechanism of inactivation of the enzyme and to identify opportunities for further chemistry. The kinetics of inactivation of DprE1 was examined using an enzymatic assay that monitored reaction progress up to ...[more]