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Conformational Selection of Inhibitors and Substrates by Proteolytic Enzymes: Implications for Drug Design and Polypeptide Processing

Fairlie, David P; Tyndall, Joel; Reid, S; Wong, Allan; Abbenante, Giovanni; Scanlon, Martin; March, Darren; Bergman, Douglas; Chai, Christina; Burkett, Brenden


Inhibitors of proteolytic enzymes (proteases) are emerging as prospective treatments for diseases such as AIDS and vital infections, cancers, inflammatory disorders, and Alzheimer's disease. Generic approaches to the design of protease inhibitors are limited by the unpredictability of interactions between, and structural changes to, inhibitor and protease during binding. A computer analysis of superimposed crystal structures for 266 small molecule inhibitors bound to 48 proteases (16 aspattic,...[Show more]

CollectionsANU Research Publications
Date published: 2000
Type: Journal article
Source: Journal of Medicinal Chemistry
DOI: 10.1021/jm990315t


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