DprE1 Is a Vulnerable Tuberculosis Drug Target Due to Its Cell Wall Localization.
ACS Chem Biol
; 10(7): 1631-6, 2015 Jul 17.
Article
em En
| MEDLINE
| ID: mdl-25906160
ABSTRACT
The flavo-enzyme DprE1 catalyzes a key epimerization step in the decaprenyl-phosphoryl d-arabinose (DPA) pathway, which is essential for mycobacterial cell wall biogenesis and targeted by several new tuberculosis drug candidates. Here, using differential radiolabeling with DPA precursors and high-resolution fluorescence microscopy, we disclose the unexpected extracytoplasmic localization of DprE1 and periplasmic synthesis of DPA. Collectively, this explains the vulnerability of DprE1 and the remarkable potency of the best inhibitors.
Texto completo:
1
Bases de dados:
MEDLINE
Assunto principal:
Proteínas de Bactérias
/
Tuberculose
/
Parede Celular
/
Oxirredutases do Álcool
/
Mycobacterium tuberculosis
/
Antituberculosos
Limite:
Humans
Idioma:
En
Revista:
ACS Chem Biol
Ano de publicação:
2015
Tipo de documento:
Article
País de afiliação:
Eslováquia