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Keywords:

  • AlphaScreen;
  • HIV-1 integrase;
  • LEDGF/p75;
  • lovastatin;
  • statins

Lovastatin was identified through virtual screening as a potential inhibitor of the LEDGF/p75–HIV-1 integrase interaction. In an AlphaScreen assay, lovastatin inhibited the purified recombinant protein–protein interaction (IC50 = 1.97 ± 0.45 μm) more effectively than seven other tested statins. None of the eight statins, however, yielded antiviral activity in vitro, while only pravastatin lactone yielded detectable inhibition of HIV-1 integrase strand transfer activity (31.65% at 100 μm). A correlation between lipophilicity and increased cellular toxicity of the statins was observed.