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The successful replication of many retroviruses requires an ordered pattern of viral gene expression. 1 Small organic molecules that target viral RNA sites and prevent the formation of key RNA-protein complexes are promising candidates for drug discovery. 2, 3 Regulatory proteins that act posttranscriptionally are particularly attractive since the RNA sequences they recognize are likely to also serve as coding sequences for other essential viral proteins. 4 The HIV-1 Rev-Response-Element (RRE) serves as the Rev-binding site responsible for the active export of unspliced HIV genomic RNA from the nucleus as well as part of the envelope-protein open reading frame. 5 Because of this dual function, the evolution of resistant variants may be prevented or impeded. Neomycin B and other aminoglycoside antibiotics have been shown to competitively block the binding of the Rev protein to its RNA recognition element …