Structural analysis of HIV integrase multimerization and development of inhibitors of integrase interactions with cellular cofactos

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In the present study period, we analyzed the dynamics of IN multimerization and attemoted to elucidate the mechanism of the inhibition of the multimerization by drugs using a newly generated quantitative bimolecular fluorescence complementation (BiFC) assay system. We found that such drugs cause over-multimerization of IN subunits and that EC50 of IN multimerization of the drugs was quite similar to that of their anti-HIV-1 EC50. Continuation of the drug discovery efforts on agents with such unique activity should not only shed lights to the understanding of IN's multimerization mechanism and but also help develop novel HIV treatment strategies for combating multi-drug resistant HIV-1.