Establishment and application of a screening anti-HIV-1 drug model targeted nuclear trafficking of virus RNA / 药学学报
Acta Pharmaceutica Sinica
; (12): 257-262, 2010.
Article
in Zh
| WPRIM
| ID: wpr-250633
Responsible library:
WPRO
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.
Full text:
1
Index:
WPRIM
Main subject:
Pharmacology
/
Virus Replication
/
Codon
/
RNA, Viral
/
Transfection
/
Cell Nucleus
/
HIV-1
/
Receptors, Cytoplasmic and Nuclear
/
Genes, Reporter
/
Anti-HIV Agents
Type of study:
Diagnostic_studies
/
Prognostic_studies
/
Screening_studies
Limits:
Humans
Language:
Zh
Journal:
Acta Pharmaceutica Sinica
Year:
2010
Type:
Article