title: Targeting HIV-1 protease: a test of drug-design methodologies.
abstract: The proteinase of the human immunodeficiency virus (HIV-1 protease) is an obvious example of a receptor for which drug design methodologies have been successfully applied. In this article, Michael West and David Fairlie outline the specific progress made to date towards the rational design of protease inhibitors as anti-HIV drugs, and compare their pharmacological profiles. The rationale employed in designing protease inhibitors illustrates evolving trends in drug design, problems in comparing assay data, and obstacles to developing enzyme inhibitors into drugs.
authors.affiliation: Centre for Drug Design and Development, University of Queensland, Brisbane, Australia.
authors.forename: M L
authors.initials: ML
authors.lastname: West
authors.forename: D P
authors.initials: DP
authors.lastname: Fairlie
mesh_terms: D000595:Amino Acid Sequence; D015195:Drug Design; D015658:HIV Infections / Q000188:drug therapy*; D017320:HIV Protease Inhibitors / Q000494:pharmacology* / Q000627:therapeutic use; D015497:HIV-1; D006801:Humans; D008969:Molecular Sequence Data
chemical_list: D017320:HIV Protease Inhibitors