Abstract 1643 Structure-Activity Relationship Assessment of Novel HIV-1 Protease Autoprocessing Inhibitors

The HIV-1 protease (PR) is initially produced as part of the Gag-Pol polyprotein precursor, which co-packages with Gag into immature viral particles. Shortly after these particles are released from infected CD4+ cells, the Gag-Pol precursor undergoes autoprocessing. During this process, the embedded precursor PR cleaves at its own N- and C- termini, releasing mature PRs that subsequently cleaves additional sites within Gag and Gag-Pol. Nearly complete cleavage of Gag and Gag-Pol, facilitated by the mature PR, is required to produce fully infectious viral particles.