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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amino Acid Sequence
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Anti-HIV Agents / pharmacology*
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Ciprofloxacin / analogs & derivatives
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Ciprofloxacin / pharmacology*
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DNA, Viral / drug effects
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DNA, Viral / genetics
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Gene Products, tat / antagonists & inhibitors*
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Gene Products, tat / metabolism*
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HIV Long Terminal Repeat / drug effects*
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HIV Long Terminal Repeat / genetics
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HIV-1 / drug effects
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HIV-1 / metabolism*
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Isoquinolines
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Molecular Sequence Data
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Mutation / genetics
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Plasmids / genetics
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Pyrroles
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Quinolones / pharmacology*
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RNA, Viral / drug effects
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RNA, Viral / genetics
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tat Gene Products, Human Immunodeficiency Virus
Substances
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Anti-HIV Agents
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DNA, Viral
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Gene Products, tat
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Isoquinolines
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Pyrroles
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Quinolones
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RNA, Viral
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WM5 compound
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tat Gene Products, Human Immunodeficiency Virus
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Ciprofloxacin