| 氮唑类抗真菌药物靶酶CYP51的研究进展 |
| 投稿时间：2015-12-21 修订日期：2016-01-26 点此下载全文 |
| 引用本文：李冉,张大志.氮唑类抗真菌药物靶酶CYP51的研究进展[J].药学实践杂志,2016,34(2):106~109 |
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| 中文摘要:氮唑类药物是临床上应用最广、种类最多的广谱高效抗真菌药物,其作用靶点为真菌甾醇合成过程中的一个关键酶——羊毛甾醇14α-去甲基化酶(CYP51)。CYP51由CYP 51基因(同名ERG 11)表达。一方面,真菌CYP51是跨膜蛋白,难以纯化获得其准确的结构信息,成为药物研发的瓶颈之一;另一方面,CYP51变异是公认的真菌耐药的主要原因之一,研究其结构变化对于抗真菌耐药具有重要意义。因此,笔者对近年来CYP51的研究进展进行综述。 |
| 中文关键词:CYP51靶酶 三维结构 动力学 突变 耐药 |
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| Development in research of CYP51 as the target of triazoles |
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| Abstract:Triazoles are the most widely used antifungal drugs in clinic with broad spectrum and high efficacy, which targets sterol 14α-demethylase(CYP51), an enzyme expressed by the gene EGR 11, which is a key enzyme in the fungi ergosterol biosynthesis. On the one hand, the CYP51 belongs to a transmembrane protein. It is difficult to get the exact functional structure conformation which becomes a big challenge for the development of new drugs. On the other hand, it becomes consensus that EGR11 exon mutation cause CYP51 structural change is one of the major reasons for antifungal drugs resistance. Therefore, study of the structural changes toward the antifungal drug resistance is quite important. The review authors have summarized the research progress on CYP51 over the recent years. |
| keywords:target CYP51 gene sequence three-dimensional structure kinetics variation and resistance |
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