title: Targeting the HIV-protease in AIDS therapy: a current clinical perspective.
abstract: 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.
authors.affiliation: Department of Protein Science, Pharmacia and Upjohn, Kalamazoo, MI 49001, USA.
authors.forename: A G
authors.initials: AG
authors.lastname: Tomasselli
authors.forename: R L
authors.initials: RL
authors.lastname: Heinrikson
mesh_terms: D000163:Acquired Immunodeficiency Syndrome / Q000188:drug therapy* / Q000821:virology; D019380:Anti-HIV Agents / Q000009:adverse effects / Q000627:therapeutic use*; D001665:Binding Sites; D002219:Carbamates; D002986:Clinical Trials as Topic; D017076:Computer-Aided Design; D018360:Crystallography, X-Ray; D015195:Drug Design; D004352:Drug Resistance, Microbial / Q000235:genetics; D004359:Drug Therapy, Combination; D005663:Furans; D016333:HIV Protease / Q000737:chemistry / Q000235:genetics*; D017320:HIV Protease Inhibitors / Q000009:adverse effects / Q000627:therapeutic use*; D015497:HIV-1 / Q000201:enzymology* / Q000235:genetics; D006801:Humans; D019469:Indinavir / Q000627:therapeutic use; D019888:Nelfinavir / Q000737:chemistry / Q000627:therapeutic use; D009842:Oligopeptides / Q000627:therapeutic use; D011725:Pyridines / Q000737:chemistry / Q000627:therapeutic use; D011753:Pyrones / Q000737:chemistry / Q000627:therapeutic use; D016032:Randomized Controlled Trials as Topic; D019438:Ritonavir / Q000627:therapeutic use; D019258:Saquinavir / Q000627:therapeutic use; D013449:Sulfonamides / Q000737:chemistry / Q000627:therapeutic use
chemical_list: D019380:Anti-HIV Agents; D002219:Carbamates; D005663:Furans; D017320:HIV Protease Inhibitors; D009842:Oligopeptides; D011725:Pyridines; D011753:Pyrones; D013449:Sulfonamides; C065978:U 75875; C095108:amprenavir; D019469:Indinavir; D016333:HIV Protease; D019888:Nelfinavir; D019258:Saquinavir; D019438:Ritonavir; C107201:tipranavir