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Overview
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Background
Amprenavir (agenerase), an N,N-disubstituted hydroxyethylamino sulfonamide, is a novel inhibitor of human immunodeficiency virus type 1 (HIV-1) protease that potently inhibits the activity of HIV-1 protease with a value of 50% inhibition concentration IC50 of 0.6 nM and also weakly inhibits HIV-2 protease with IC50 value of 19 nM. Amprenavir binds to the catalytic aspartate residues of the HIV-1 protease and hence inhibits the processing of the gag and gag-pol polyprotein precursors, which cleave to yield structural proteins and replication enzymes of HIV, resulting in immature and noninfectious viral particles. Amprenavir has been effectively used for the treatment of HIV disease in patients with primary HIV infection.
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Overview