Effect of detergent on "promiscuous" inhibitors

被引：197

作者：

Ryan, AJ ^{[1
]}

Gray, NM ^{[1
]}

Lowe, PN ^{[1
]}

Chung, CW ^{[1
]}

机构：

[1] GlaxoSmithKline, Computat & Struct Sci, Stevenage SG1 2NY, Herts, England

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 46卷 / 16期

关键词：

D O I：

10.1021/jm0340896

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The term "promiscuous" inhibitors has been coined for compounds whose inhibition mechanism involves the interaction of aggregates of many compound molecules with the target protein, rather than the binding of individual molecules. This paper demonstrates that promiscuous inhibitors can be differentiated from classical 1:1 inhibitors by the judicious use of detergents, making it possible to configure assays that significantly reduce this undesirable mechanism of inhibition without compromising assay performance.

引用

页码：3448 / 3451

页数：4

共 9 条

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