碳酸酐酶抑制剂。用阴离子抑制来自酿酒酵母的β类酶。
Carbonic anhydrase inhibitors. Inhibition of the beta-class enzyme from the yeast Saccharomyces cerevisiae with anions.
作者信息
Isik Semra, Kockar Feray, Arslan Oktay, Guler Ozen Ozensoy, Innocenti Alessio, Supuran Claudiu T
机构信息
Department of Chemistry, Science and Art Faculty, Balikesir University, Balikesir, Turkey.
出版信息
Bioorg Med Chem Lett. 2008 Dec 15;18(24):6327-31. doi: 10.1016/j.bmcl.2008.10.100. Epub 2008 Oct 25.
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 CO(2) hydrase activity, with a k(cat) of 9.4x10(5) s(-1) and k(cat)/K(m) of 9.8x10(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 microM). The other investigated anions showed inhibition constants in the low millimolar range.
酿酒酵母Nce103基因编码的蛋白质，一种被命名为scCA的β-碳酸酐酶（CA，EC 4.2.1.1），已被克隆、纯化、进行动力学表征，并研究了其被一系列简单无机阴离子（如卤化物、拟卤化物、碳酸氢盐、碳酸盐、硝酸盐、亚硝酸盐、硫化氢、亚硫酸氢盐、高氯酸盐、硫酸盐及其一些等排体）抑制的情况。该酶表现出高二氧化碳水合酶活性，催化常数k(cat)为9.4×10⁵ s⁻¹，催化效率k(cat)/K(m)为9.8×10⁷ M⁻¹ s⁻¹。scCA被金属毒物（氰化物、叠氮化物、氰酸盐、硫氰酸盐，抑制常数K(I)为16.8 - 55.6 mM）弱抑制，被溴化物、碘化物和磺胺（抑制常数K(I)为8.7 - 10.8 μM）强抑制。其他研究的阴离子显示出在低毫摩尔范围内的抑制常数。
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