Carbonic anhydrase inhibitors: Inhibition of the cytosolic human isozyme VII with anions

被引：21
|
作者：
Vullo, Daniela
Ruusuvuori, Eva
Kaila, Kai
Scozzafava, Andrea
Supuran, Claudiu T.
机构：
[1] Univ Florence, Lab Chim Bioinorgan, I-50019 Florence, Italy
[2] Univ Helsinki, Dept Biol & Environm Sci, FIN-00014 Helsinki, Finland
[3] Univ Helsinki, Ctr Neurosci, FIN-00014 Helsinki, Finland
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 12期
关键词：
D O I：
10.1016/j.bmcl.2006.03.078
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
An inhibition study of the cytosolic carbonic anhydrase (CA, EC 4.2.1.1) isozyme VII (hCA VII) with anions has been conducted. Cyanate, cyanide, and hydrogensulfite were weak hCA VII inhibitors (K(I)s in the range of 7.3-15.2 mM). Cl- and HCO3- showed good inhibitory activity against hCA VII (K(I)s of 0.16-1.84 mM), suggesting that this enzyme is not involved in metabolons with anion exchangers or sodium bicarbonate cotransporters. The best inhibitors were sulfamate, sulfamide, phenylboronic, and phenylarsonic acid (K(I)s of 6.8-12.5 mu M). (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3139 / 3143
页数：5
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