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
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.
引用
收藏
页码:2573 / 2578
页数:6
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