Inhibitors of HIV proteinase

This article briefly describes the identification of HIV proteinase as a potential target for antiviral chemotherapy, and discusses some of the strategies which have been used to discover inhibitors of this essential viral enzyme. Preclinical efficacy data are presented for selected inhibitors, and the ability of such compounds to generate a virus with reduced sensitivity is compared to that of reverse transcriptase inhibitors. The possibility of clinically useful synergistic interactions between inhibitors of HIV proteinase and other antiviral agents is also considered.