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Inhibition of glutathione S-transferase in rat hepatocytes by a glycine-tetrazole modified S-alkyl-GSH analogue

被引：22
作者：
Burg, D
Hameetman, L
Filippov, DV
van der Marel, GA
Mulder, GJ
机构：
[1] Leiden Univ, Leiden Amsterdam Ctr Drug Res, Div Toxicol, NL-2300 RA Leiden, Netherlands
[2] Leiden Univ, Leiden Inst Chem, Div Bioorgan Synth, NL-2300 RA Leiden, Netherlands
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 12期
关键词：
D O I：
10.1016/S0960-894X(02)00247-0
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Glutathione (GSH) conjugates inhibit enzymes that are involved in drug metabolism and drug resistance, but their cellular uptake is very low. To improve membrane-permeability, we synthesized a novel GSH-conjugate analogue with a tetrazole carboxylate isostere at the glycine position. Introduction of the tetrazole decreases inhibitory potency towards CDNB conjugation by glutathione S-transferase. However, the tetrazole derivative inhibited 2-bromoisovalerylurea conjugation in rat liver cytosol, as well as in hepatocytes. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：1579 / 1582
页数：4
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