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Antimicrob Agents Chemother. 2004 May;48(5):1895-9.

Inhibition of human immunodeficiency virus type 1 tat-trans-activation-responsive region interaction by an antiviral quinolone derivative.

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  • 1Department of Pharmaceutical Sciences, University of Padua, 35131 Padua, Italy.

Abstract

WM5, a 6-aminoquinolone derivative, binds with high affinity to the bulge of the trans-activation-responsive region (TAR), whereas it displays low binding affinity for the loop and stem regions of TAR and for random RNA and DNA sequences. Furthermore, WM5 disrupts the natural protein-nucleic acid complex with a 50% inhibitory concentration in the low micromolar range in both in vitro and in vivo assays.

PMID:
15105155
[PubMed - indexed for MEDLINE]
PMCID:
PMC400552
Free PMC Article
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