Highly potent bisphosphonate ligands for phosphoglycerate kinase

…, AJ Ivory, MP Williamson, GM Blackburn

Index: Jakeman, David L.; Ivory, Andrew J.; Williamson, Michael P.; Blackburn, G. Michael Journal of Medicinal Chemistry, 1998 , vol. 41, # 23 p. 4439 - 4452

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Citation Number: 62

Abstract

We have synthesized a series of novel analogs of 1, 3-bisphospho-d-glyceric acid, 1, 3-BPG, 3 and evaluated their binding to phosphoglycerate kinase, PGK (EC 2.7. 2.3). Nonscissile methanephosphonic acids replace the two phosphate monoesters of 1, 3-BPG and lead to several stable, tight-binding mimics of this intermediate species in glycolysis. Multiple fluorine substitution for hydrogen in the α-methylene groups of the phosphonic acid 1, 3- ...