High-Throughput Screening for Inhibitors of Sialyl- and Fucosyltransferases

被引：50
|
作者：
Rillahan, Cory D. [1 ]
Brown, Steven J. [1 ]
Register, Amy C. [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
收藏
页码：12534 / 12537
页数：4
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