Rapid identification of potent nonpeptidic serine protease inhibitors

被引：21
|
作者：
Salisbury, Cleo M.
Ellman, Jonathan A. [1 ]
机构：
[1] Univ Calif Berkeley, Dept Chem, Ctr New Direct Organ Synth, Berkeley, CA 94720 USA
[2] Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA
[3] Scripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
来源：
CHEMBIOCHEM | 2006年 / 7卷 / 07期
关键词：
hydrolases; inhibitors; nonpeptidic; proteases;
D O I：
10.1002/cbic.200600081
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Substrate activity screening was used to rapidly identify a novel and potent (kinact/Ki = 59000 M-1 S-1) nonpeptidic chymotrypsin inhibitor with Mw < 500. The inhibitor is more potent than the best reported tetrapeptidyl phosphonate chymotrypsin inhibitor and demonstrated selectivity over a panel of other serine proteases, including the closely related enzyme cathepsin G. © 2006 Wiley-VCH Verlag GmbH & Co. KGaA.
引用
收藏
页码：1034 / 1037
页数：4
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