u-75875 and Acquired-Immunodeficiency-Syndrome

This review deals with clinical applications of compounds that inhibit the action of the protease encoded within the genome of human immunodeficiency virus (HIV). The HIV-protease is essential for viral maturation and represents an important therapeutic target in the fight against AIDS. Following a brief overview of the enzyme structure and function, the article focuses on a number of peptide and non-peptide based HIV-protease inhibitors that are in current clinical use. These drugs are discussed both with respect to their efficacy in treatment of AIDS, and to problems related to insurgence of viral resistance and side effects seen to date in patient populations.

Topics: Acquired Immunodeficiency Syndrome; Anti-HIV Agents; Binding Sites; Carbamates; Clinical Trials as Topic; Computer-Aided Design; Crystallography, X-Ray; Drug Design; Drug Resistance, Microbial; Drug Therapy, Combination; Furans; HIV Protease; HIV Protease Inhibitors; HIV-1; Humans; Indinavir; Nelfinavir; Oligopeptides; Pyridines; Pyrones; Randomized Controlled Trials as Topic; Ritonavir; Saquinavir; Sulfonamides

Topics: Acquired Immunodeficiency Syndrome; Amino Acid Sequence; Aspartic Acid Endopeptidases; HIV Protease; HIV Protease Inhibitors; HIV-1; Humans; Molecular Sequence Data; Molecular Structure; Mutagenesis, Site-Directed; Substrate Specificity; Virus Replication