PROTEASE INHIBITORS

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.
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