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

页码：1034 / 1037

页数：4

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