[Establishment and application of a screening anti-HIV-1 drug model targeted nuclear trafficking of virus RNA].
Yao Xue Xue Bao
; 45(2): 257-62, 2010 Feb.
Article
em Zh
| MEDLINE
| ID: mdl-21351437
ABSTRACT
The HIV-1 Rev protein facilitates nuclear export of unspliced and singly spliced viral transcripts containing RRE RNA through the CRM1 export pathway. Inhibition of Rev-mediated RNA nuclear export can arrest HIV-1 transcriptional process, which clearly, reveals a target for anti-HIV drug development. In this work, a cell-based assay has been established for screening anti-HIV compounds targeting the Rev-mediated RNA nuclear export. This assay utilized a codon-optimized green fluorescent protein (GFP) as reporter gene, which expression is in a Rev-dependent manner. Any compound that inhibits the Rev-mediated RNA nuclear export is identified by reducing emission of GFP. The Z' score of this model is 0.8220. Three thousands compounds were screened and the positive rate was 9.3% with a cutoff at 50% inhibition. IMB7C7, one of the positive compounds, efficiently inhibits viral production from HIV-1 infected cells.
Buscar no Google
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Núcleo Celular
/
HIV-1
/
Fármacos Anti-HIV
/
Transporte Ativo do Núcleo Celular
/
Produtos do Gene rev do Vírus da Imunodeficiência Humana
Tipo de estudo:
Diagnostic_studies
/
Prognostic_studies
/
Screening_studies
Limite:
Humans
Idioma:
Zh
Ano de publicação:
2010
Tipo de documento:
Article