HIV-Protease Inhibitors

Abstract

Inhibitors of human immunodeficiency virus (HIV)–encoded protease, combined with nucleoside analogues with antiretroviral activity, cause profound and sustained suppression of viral replication, reduce morbidity, and prolong life in patients with HIV infection.¹³ Recent guidelines recommend that initial treatment of all HIV-infected patients include the administration of an HIV-protease inhibitor.⁴ The HIV-Encoded ProteaseThe HIV protease, encoded in the 5' end of the pol gene, is expressed as part of the gag–pol polyprotein (Figure 1A, Figure 1B, and Figure 1C). This gene encodes a 99-amino-acid protein. Homodimers of this protein have the aspartyl protease activity that is typical of retroviral proteases; monomers . . .