Effects of tyrphostins, protein kinase inhibitors, on human immunodeficiency virus type 1 integrase. The state of the art may have changed since the publication date. Effects of tyrphostins, protein kinase inhibitors, on human immunodeficiency virus type 1 integrase.
Integration is catalyzed by the viral integrase protein.
We have extended these findings by examining the effects of tryphostins, tyrosine kinase inhibitors. Both steps of the integration reaction, 3'-processing and strand transfer, were inhibited by tyrphostins at micromolar concentrations. The DNA binding activity of integrase was inhibited at higher concentrations of tryphostins. Binding of tyrphostins at or near the integrase catalytic site was also suggested by experiments showing a global inhibition of the choice of attacking nucleophile in the 3'-processing reaction. I, even at 100 microM, suggesting selectivity for integrase inhibition.