Work

Benzothiazinones: Prodrugs That Covalently Modify the Decaprenylphosphoryl-β- d -ribose 2′-epimerase DprE1 of Mycobacterium tuberculosis

Year: 2010

Type: article

Abstract: Benzothiazinones (BTZs) form a new class of potent antimycobacterial agents. Although the target of BTZs has been identified as decaprenylphosphoryl-β-D-ribose 2'-epimerase (DprE1), their detailed mechanism of action remains obscure. Here we demonstrate that BTZs are activated in the bacterium by reduction of an essential nitro group to a nitroso derivative, which then specifically reacts with a cysteine residue in the active site of DprE1.

Source: Journal of the American Chemical Society

DOI: 10.1021/ja106357w

Authors: Claudia Trefzer, Monica Rengifo-Gonzalez, Marlon J. Hinner, Patricia Schneider, Vadim Makarov, Stewart T. Cole, Kai Johnsson

Institutions: Russian Academy of Sciences, École Polytechnique Fédérale de Lausanne

Language: English

Topic: Tuberculosis Research and Epidemiology

Subfield: Infectious Diseases

Field: Medicine

Domain: Health Sciences

Open Access status: green

OpenAlex ID: W2004707638

FWCI: 7.509

Cites: 16

Cited by: 217

Related to: 9