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Targeting HIV-1 protease: A test of drug-design methodologies

Authors
Journal
Trends in Pharmacological Sciences
0165-6147
Publisher
Elsevier
Publication Date
Volume
16
Issue
2
Identifiers
DOI: 10.1016/s0165-6147(00)88980-4
Disciplines
  • Biology
  • Design
  • Pharmacology

Abstract

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.

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