SYNTHESIS OF PHOSPHONATE ANALOGS OF 1,3-BISPHOSPHOGLYCERIC ACID AND THEIR BINDING TO YEAST PHOSPHOGLYCERATE KINASE

被引：45
作者：
BLACKBURN, GM
JAKEMAN, DL
IVORY, AJ
WILLIAMSON, MP
机构：
[1] Krebs Institute, Department of Chemistry, University of Sheffield, Sheffield
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 21期
关键词：
D O I：
10.1016/S0960-894X(01)80286-9
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Phosphonate analogues of 1,3-bisphosphoglyceric acid, several incorporating non-scissile alpha-difluoro phosphonates, have been synthesised and their binding to phosphoglycerate kinase measured by NMR analysis. The tetrafluoroamide analogue (4) of 1,3-P(2)GA shows the strongest binding, with a dissociation constant of 2 mu M.
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页码：2573 / 2578
页数：6
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