Establishment and application of a high-throughput screening assay for premature activation of HIV-1 precursors / 药学学报
Acta Pharmaceutica Sinica
; (12): 247-252, 2010.
Article
em Zh
| WPRIM
| ID: wpr-250635
Biblioteca responsável:
WPRO
ABSTRACT
Strict regulation of HIV-1 PR function is critical for efficient production of mature viral particles. During viral protein expression and viral assembly, HIV-1 PR located within Gag-Pol precursor must be inactive to prevent premature cytoplasmic processing of the viral Gag and Gag-Pol precursors. Premature activation of HIV-1 precursors leads to major defects in viral assembly and production of viral particles. A cell-level premature activation of HIV-1 precursors assay using bioluminescence resonance energy transfer (BRET) was established. Three thousand compounds were screened to evaluate this assay. The results showed that the assay is sensitive, specific and stable (Z' factor is 0.905).
Texto completo:
1
Índice:
WPRIM
Assunto principal:
Farmacologia
/
Fisiologia
/
Plasmídeos
/
Precursores de Proteínas
/
Piridazinas
/
Vírion
/
Transfecção
/
Protease de HIV
/
Proteínas de Fusão gag-pol
/
HIV-1
Tipo de estudo:
Diagnostic_studies
/
Screening_studies
Limite:
Humans
Idioma:
Zh
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2010
Tipo de documento:
Article