HIV-Protease Inhibitors

• Published in: The New England journal of medicine Vol. 338; no. 18; pp. 1281 - 1293
• Main Author: Flexner, Charles
• Format: Journal Article
• Language: English
• Published: Boston, MA Massachusetts Medical Society 30.04.1998
• Subjects: Anti-HIV Agents - therapeutic use; Biological and medical sciences; Drug Interactions; Drug Resistance; Drug therapy; Drug Therapy, Combination; Enzymes; HIV; HIV Infections - drug therapy; HIV Protease - chemistry; HIV Protease Inhibitors - adverse effects; HIV Protease Inhibitors - chemistry; HIV Protease Inhibitors - pharmacology; HIV Protease Inhibitors - therapeutic use; Human immunodeficiency virus; Human viral diseases; Humans; Infectious diseases; Medical sciences; Molecular Structure; Protease inhibitors; Proteins; Treatment Failure; Viral diseases; Viral diseases of the lymphoid tissue and the blood. Aids; Human; Immunopathology; Evaluation; Protein inhibitor; Enzyme; Retroviridae; AIDS; Review; Immune deficiency; Lentivirus; Infection; Virus; Peptidases; Chemotherapy; Perspective; Viral disease; Hydrolases; Human immunodeficiency virus; Effectiveness factor; Pharmacokinetics; Physicochemical properties
• ISSN: 0028-4793; 1533-4406
• DOI: 10.1056/NEJM199804303381808

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. 1 – 3 Recent guidelines recommend that initial treatment of all HIV-infected patients include the administration of an HIV-protease inhibitor. 4 The HIV-Encoded Protease The 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 . . .