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Powerful probes for glycosidases:: Novel, fluorescently tagged glycosidase inhibitors

被引：29
作者：
Hermetter, A
Scholze, H
Stütz, AE
Withers, SG
Wrodnigg, TM
机构：
[1] Graz Tech Univ, Inst Organ Chem, Glycogrp, A-8010 Graz, Austria
[2] Graz Tech Univ, Inst Biochem, A-8010 Graz, Austria
[3] Univ British Columbia, Dept Chem, Vancouver, BC V6T 1Z1, Canada
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 10期
基金：
奥地利科学基金会;
关键词：
D O I：
10.1016/S0960-894X(01)00209-8
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
1-Amino-1,2,5-trideoxy-2,5-imino-D-mannitol was fluorescently tagged by reaction with dansyl chloride at N-1 or by attachment of a dansyl amide bearing spacer to this centre. Compounds obtained are highly potent inhibitors of beta -glucosidase exhibiting K-i values in the single figure nanosmolar range. The 1-N-dansyl substituted inhibitor was successfully exploited for binding studies with beta -glucosidase from Agrobacterium sp. employing fluorescence spectrometric methods. (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：1339 / 1342
页数：4
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