PHOSPHONATE INHIBITORS OF GLYCERALDEHYDE-3-PHOSPHATE DEHYDROGENASE AND PHOSPHOGLYCERATE KINASE

被引：10

作者：

LI, YK ^{[1
]}

BYERS, LD ^{[1
]}

机构：

[1] TULANE UNIV,DEPT CHEM,NEW ORLEANS,LA 70118

来源：

BIOCHIMICA ET BIOPHYSICA ACTA | 1993年 / 1164卷 / 01期

关键词：

INHIBITION; PHOSPHONATE; GLYCERALDEHYDE-3-PHOSPHATE DEHYDROGENASE; PHOSPHOGLYCERATE KINASE;

D O I：

10.1016/0167-4838(93)90106-2

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：

Several bisphosphonates were examined as inhibitors of yeast GPD (glyceraldehyde-3-phosphate dehydrogenase, EC 1.2.1.12) and PGK (phosphoglycerate kinase, EC 2.7.2.3). The phosphonomethyl analog of 2-deoxy-1,3-bisphosphoglycerate (i.e., 2-oxo-1,5-bisphosphonopentane, 2-oxo-PC5P) is a good inhibitor of PGK (K(i) = 0.2 +/- 0.08 mM at pH 8.5, 27-degrees-C) and a poor inhibitor of GPD (K(i) = 20 +/- 1 mM, pH 8.5). The shorter, butane, analog (2-oxo-PC4P) binds more tightly to PGK (K(i) = 84 +/- 6 muM), and about equally well to GPD, as does 2-oxo-PC5P. The 2-oxo-bisphosphonates bind to PGK more tightly (by approx. 4 kJ/mol) than do the corresponding non-carbonyl analogues (1,4-bisphosphonobutane and 1,5-bisphosphonopentane).

引用

页码：17 / 21

页数：5

共 23 条

[1] COMMENTS TO THE AMINO-ACID-SEQUENCE OF YEAST GLYCERALDEHYDE-3-PHOSPHATE DEHYDROGENASE [J].