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.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Thurmond RL,Beavers MP,Cai H,Meduna SP,Gustin DJ,Sun S,Almond HJ,Karlsson L,Edwards JPdoi
10.1021/jm0496133keywords:
subject
Has Abstractpub_date
2004-09-23 00:00:00pages
4799-801issue
20eissn
0022-2623issn
1520-4804journal_volume
47pub_type
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journal_title:Journal of medicinal chemistry
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更新日期:2006-12-28 00:00:00
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