Small-molecule inactivation of HIV-1 NCp7 by repetitive intracellular acyl transfer.
Nat Chem Biol
; 6(12): 887-9, 2010 Dec.
Article
en En
| MEDLINE
| ID: mdl-20953192
ABSTRACT
The zinc fingers of the HIV-1 nucleocapsid protein, NCp7, are prime targets for antiretroviral therapeutics. Here we show that S-acyl-2-mercaptobenzamide thioester (SAMT) chemotypes inhibit HIV by modifying the NCp7 region of Gag in infected cells, thereby blocking Gag processing and reducing infectivity. The thiol produced by SAMT reaction with NCp7 is acetylated by cellular enzymes to regenerate active SAMTs via a recycling mechanism unique among small-molecule inhibitors of HIV.
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Benzamidas
/
Fármacos Anti-VIH
/
Productos del Gen gag del Virus de la Inmunodeficiencia Humana
Idioma:
En
Revista:
Nat Chem Biol
Asunto de la revista:
BIOLOGIA
/
QUIMICA
Año:
2010
Tipo del documento:
Article
País de afiliación:
Estados Unidos