The evaluation of statins as potential inhibitors of the LEDGF/p75-HIV-1 integrase interaction
Date
2014
Authors
Harrison, A.T.
Kriel, F.H.
Papathanasopoulos, M.
Mosebi, S.
Abrahams, S.
Hewer, R.
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Journal article
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Chemical Biology and Drug Design, 2014; 85(3):290-295
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Abstract
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.
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Copyright 2014 John Wiley & Sons A/S