Substances, either of biological or synthetic origin, that inhibit the action of proteases.
Protease Inhibitors & AIDS.JAMA 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.
a drug (e.g., saquinavir, ritonavir, indinavir)
which blocks the action of the HIV protease enzyme, thereby preventing
HIV replication. Unlike reverse transcriptase inhibitors, protease inhibitors
can inhibit HIV replication in cells that are already infected.
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