ABSTRACT
The human immunodeficiency virus (HIV) is one of only a few retroviruses known to infect humans. It is known from drug design studies with HIV reverse transcriptase and protease that the virus is able to escape from the pressures of inhibitors by mutation of the drug targets. The requirement of the conversion of viral RNA to double-stranded DNA is a feature unique to retroviruses. Although details of the timing of reverse transcription, nuclear localization, and integration are not yet clear, it is generally recognized that the movement of double-stranded viral DNA across the nuclear membrane is followed by insertion, or integration, of the viral genome into a host-cell chromosome. It has been demonstrated that the chemical steps that comprise DNA integration are carried out by the viral protein, integrase. In 1993, the effects of selected topoisomerase II inhibitors, antimalarial agents, DNA binders, naphthoquinones, and various other agents on integrase activity in vitro were investigated.
