High-Throughput Screening for Inhibitors of Sialyl- and Fucosyltransferases

被引：50

作者：

Rillahan, Cory D. ^{[1
]}

Brown, Steven J. ^{[1
]}

Rosen, Hugh ^{[1
]}

Paulson, James C. ^{[1
]}

机构：

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

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2011年 / 50卷 / 52期

关键词：

carbohydrates; fucose; glycoproteins; glycosyltransferases; sialic acids; GDP-L-FUCOSE; ASSAY;

D O I：

10.1002/anie.201105065

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Sweet screens: A high-throughput screening platform for identification of inhibitors of sialyl- and fucosyltransferases based on fluorescence polarization (FP) has been developed. An analogue of the natural donor substrate carrying a fluorescent label (green star) is transferred to a glycoprotein acceptor, which results in robust FP (see picture). The screening of 16 000 compounds against different glycosyltransferases has identified various interesting inhibitors. Copyright © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

引用

页码：12534 / 12537

页数：4

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