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一种用于糖原合酶激酶-3β抑制剂的高通量发光测定法。

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

作者信息

Baki Andrea, Bielik Attila, Molnár László, Szendrei Györgyi, Keserü György M

机构信息

Chemical and Biotechnological R&D, Gedeon Richter Ltd., Budapest, Hungary.

出版信息

Assay Drug Dev Technol. 2007 Feb;5(1):75-83. doi: 10.1089/adt.2006.029.

DOI:10.1089/adt.2006.029
PMID:17355201
Abstract

A high throughput luminescent assay based on the Kinase-Glo() system (Promega, Madison, WI) has been developed for screening against glycogen synthase kinase-3beta (GSK-3beta). 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-3beta inhibitors.

摘要

已开发出一种基于Kinase-Glo()系统（普洛麦格公司，威斯康星州麦迪逊市）的高通量发光检测法，用于筛选糖原合酶激酶-3β（GSK-3β）。通过仔细优化检测参数，我们开发出了一种稳健、可重复且灵敏的检测方法。在对55000种化合物进行高通量筛选时，该方法的实用性得到了证明。此次筛选产生了五类活性化合物，包括几种高效的GSK-3β抑制剂。

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