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  • Title: Molecular basis of HIV-1 TAR RNA specific recognition by an acridine tat-antagonist.
    Author: Gelus N, Hamy F, Bailly C.
    Journal: Bioorg Med Chem; 1999 Jun; 7(6):1075-9. PubMed ID: 10428376.
    Abstract:
    We investigated the interaction of a highly potent acridine-based tat-antagonist with the TAR RNA of HIV-1. The wild type TAR RNA and three mutants with U-->C23, G x C-->C x G26-39 or G x C-->A x U26-39 substitutions were used as substrates to study the molecular basis of drug-TAR RNA complex formation. Melting temperature and RNase protection experiments reveal that the G x C26-39 pair is a critical element for specific major groove recognition of TAR at the pyrimidine bulge. The results provide a rational basis for future design of optimized tat/TAR inhibitors.
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