A potent and highly selective sulfotransferase inhibitor

被引：37

作者：

Chapman, E

Ding, S

Schultz, PG

Wong, CH

机构：

[1] Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA

[2] Scripps Res Inst, Skaggs Inst Chem Biol, La Jolla, CA 92037 USA

[3] Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA

来源：

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY | 2002年 / 124卷 / 49期

关键词：

D O I：

10.1021/ja021086u

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

In the present work, we have used a newly developed, fluorescence-based assay to screen a library of >30000 compounds as potential β-arylsulfotransferase-IV inhibitors. A total of 11 inhibitors were discovered. Most of the compounds discovered showed low micromolar inhibition, but one of the compounds showed potent inhibition (Ki = 96 nM). The most potent of these inhibitors was tested against a variety of other purine binding enzymes and showed remarkable specificity. Copyright © 2002 American Chemical Society.

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页码：14524 / 14525

页数：2

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