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Targeting HIV-1 protease: a test of drug-design methodologies.

作者信息

West M L, Fairlie D P

机构信息

Centre for Drug Design and Development, University of Queensland, Brisbane, Australia.

出版信息

Trends Pharmacol Sci. 1995 Feb;16(2):67-75. doi: 10.1016/s0165-6147(00)88980-4.

DOI:10.1016/s0165-6147(00)88980-4
PMID:7762084
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.

摘要

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