1-CHLORO-2,4-DINITROBENZENE-MEDIATED IRREVERSIBLE INACTIVATION OF ACIDIC GLUTATHIONE S-TRANSFERASES - INACTIVATION MECHANISM - A SATURATION-TYPE OR SIMPLE 2ND-ORDER KINETIC PROCESS

被引:2
作者
ADAMS, PA [1 ]
SIKAKANA, CNT [1 ]
机构
[1] UNIV CAPE TOWN,SCH MED,DEPT MED BIOCHEM,CAPE TOWN 7925,SOUTH AFRICA
关键词
D O I
10.1016/0006-2952(92)90707-P
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
A critical analysis of the inactivation kinetics exhibited by the acidic human glutathione S-transferase (GST) enzymes is presented. Data on the 1-chloro-2,4-dinitrobenzene (CDNB)-facilitated inactivation of human placental GST-pi have been utilized in conjunction with published inactivation data from the literature to answer the following two questions: (a) do the inactivation kinetics deviate significantly from a simple pseudo first-order model? (b) What is the kinetic mechanism of irreversible electrophilic co-substrate-mediated inactivation of human acidic GSTs? Inactivation of human placental GST-pi in the presence of 7-aminocephalosporanic acid. a non-electrophilic non-substrate ligand, is characterized and shown to occur via a process analogous to the second mechanism proposed for CDNB inactivation of the enzyme, namely: pH- and [ligand]-independent solvational inactivation.
引用
收藏
页码:1757 / 1760
页数:4
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