A search for pyrophosphate mimics for the development of substrates and inhibitors of glycosyltransferases

被引：109

作者：

Wang, R

Steensma, DH

Takaoka, Y

Yun, JW

Kajimoto, T

Wong, CH

机构：

[1] SCRIPPS RES INST, SKAGGS INST CHEM BIOL, LA JOLLA, CA 92037 USA

[2] RIKEN, INST PHYS & CHEM RES, FRONTIER RES PROGRAM GLYCOTECHNOL, WAKO, SAITAMA, JAPAN

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 1997年 / 5卷 / 04期

基金：

美国国家科学基金会;

关键词：

D O I：

10.1016/S0968-0896(97)00005-9

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The design and synthesis of several beta-1,4-galactosyltransferase inhibitors are reported. Mimics of the pyrophosphate-Mn2+ complex were the focus of the design. Malonic, tartaric, and monosaccharide moieties were used as replacements of the pyrophosphate moiety, and galactose or azasugars with potent galactosidase inhibitory activity were used as the 'donor' component. Compound 6, in which glucose was used as the pyrophosphate-Mn2+ complex mimic and galactose as the 'donor' component,showed the best inhibitory activity towards the transferase with a K-i of 119.6 mu M. (C) 1997 Elsevier Science Ltd.

引用

收藏

页码：661 / 672

页数：12

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