HIV
protease is an aspartyl
enzyme essential to the replicative life cycle of HIV. The three-dimensional molecular structure of the HIV
protease has been fully determined. Pharmaceutical developers are therefore able to rationally design compounds to inhibit it and thus interfere with replication of the
virus. In the US, five peptide-based
protease inhibitors (saquinavir, Roche; A-80987, ABT-538, Abbott Laboratories; L735,524, Merck; KNI-272,
NCI) are in
clinical development. All compounds inhibit
HIV-1 in vitro in nanomolar concentrations. In Europe, two peptide-based compounds (ABT-987, Abbott Laboratories; AG-1343, Agouron Pharmaceuticals, Inc.) are currently in development. See also
In Vitro.