Carbonic anhydrase inhibitors. Inhibition of the β-class enzyme from the yeast Saccharomyces cerevisiae with anions

被引：43

作者：

Isik, Semra ^{[1
]}

Kockar, Feray ^{[1
]}

Arslan, Oktay ^{[1
]}

Guler, Ozen Ozensoy ^{[1
]}

Innocenti, Alessio ^{[2
]}

Supuran, Claudiu T. ^{[2
]}

机构：

[1] Balikesir Univ, Dept Chem, Sci & Art Fac, Balikesir, Turkey

[2] Univ Florence, Lab Chim Bioinorgan, I-50019 Florence, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 24期

关键词：

Carbonic anhydrase; Yeast; Saccharomyces cerevisiae; Candida albicans; Nce103; gene; Inorganic anion; Sulfamide; Iodide;

D O I：

10.1016/j.bmcl.2008.10.100

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The protein encoded by the Nce103 gene of Saccharomyces cerevisiae, a beta-carbonic anhydrase (CA, EC 4.2.1.1) designated as scCA, has been cloned, purified, characterized kinetically, and investigated for its inhibition with a series simple, inorganic anions such as halogenides, pseudohalogenides, bicarbonate, carbonate, nitrate, nitrite, hydrogen sulfide, bisulfite, perchlorate, sulfate, and some of its isosteric species. The enzyme showed high CO2 hydrase activity, with a k(cat) of 9.4 x 10(5) s (1) and k(cat)/K-m of 9.8 x 10(7) M (1) s (1). scCA was weakly inhibited by metal poisons (cyanide, azide, cyanate, thiocyanate, K(I)s of 16.8-55.6 mM) and strongly inhibited by bromide, iodide, and sulfamide (K(I)s of 8.7-10.8 mu M). The other investigated anions showed inhibition constants in the low millimolar range. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：6327 / 6331

页数：5

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