Nonpeptidic, Noncovalent Inhibitors of the Cysteine Protease Cathepsin S
Journal of Medicinal Chemistry2004Vol. 47(20), pp. 4799–4801
Citations Over TimeTop 24% of 2004 papers
Robin L. Thurmond, Mary Pat Beavers, Hui Cai, Steven P. Meduna, Darin J. Gustin, Siquan Sun, Harold J. Almond, Lars Karlsson, James P. Edwards
Abstract
The first nonpeptidic, noncovalent inhibitors of the cysteine protease cathepsin S (CatS) are described. Electronic database searching using the program DOCK generated a screening set of potential CatS inhibitors from which two lead structures were identified as promising starting points for a drug discovery effort. Lead optimization afforded potent (IC(50) < 50 nM) and selective inhibitors of CatS demonstrating cellular activity and reversibility of enzyme inhibition.
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