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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