A high throughput luminescent assay for glycogen synthase kinase-3β inhibitors

被引：108

作者：

Baki, Andrea ^{[1
]}

Bielik, Attila ^{[1
]}

Molnar, Laszlo ^{[1
]}

Szendrei, Gyorgyi ^{[1
]}

Keseru, Gyorgy M. ^{[1
]}

机构：

[1] Gedeon Richter Chem Works Ltd, Chem & Biotechnol R&D, Budapest, Hungary

来源：

ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES | 2007年 / 5卷 / 01期

关键词：

D O I：

10.1089/adt.2006.029

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

A high throughput luminescent assay based on the Kinase-Glo (TM) system (Promega, Madison, WI) has been developed for screening against glycogen synthase kinase-3 beta (GSK-3 beta). Careful optimization of assay parameters allowed us to develop a robust, reproducible, and sensitive assay. Its usefulness has been demonstrated in a high throughput screening run when screening 55,000 compounds. This campaign yielded five chemical classes of hits, including several highly potent GSK-3 beta inhibitors.

引用

页码：75 / 83

页数：9

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