Nonpeptidic, noncovalent inhibitors of the cysteine protease cathepsin S.

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 Chem

authors

Thurmond RL,Beavers MP,Cai H,Meduna SP,Gustin DJ,Sun S,Almond HJ,Karlsson L,Edwards JP

doi

10.1021/jm0496133

keywords:

subject

Has Abstract

pub_date

2004-09-23 00:00:00

pages

4799-801

issue

20

eissn

0022-2623

issn

1520-4804

journal_volume

47

pub_type

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