甾醇14a-去甲基化酶(CYP51)的研究进展

Advances in Sterol 14a-Demethylase (CYP51)

摘要:

甾醇14a-去甲基化酶(CYP51)是分布最广的细胞色素P450家族成员, 是生物甾醇合成过程中的关键酶。故CYP51不仅是细胞色素P450蛋白结构、功能、结构与功能关系等研究的模板, 而且是重要的降胆固醇药物、抗真菌药物和除草剂作用靶标, 具有重要的经济价值。以下就CYP51家族的序列特征、功能(生理功能和生化特征)、结构、结构与功能的关系、CYP51活性的抑制等方面的研究进展进行了综述。并对CYP51抑制剂的研究局限方面进行了讨论, 探讨了CYP51抑制剂设计开发的相关问题。

Abstract:

Sterol 14a-demethylase (CYP51), the most widely distributed member of the P450 superfamily, is the key enzyme in sterol biosynthesis pathway. CYP51 is not only an important model for fundamental P450 structure/function studies, but also an important target protein of cholesterol-lowering agents, antifungal drugs and herbicides. This article reviewed the research advances in CYP51 at various aspects, including sequence characteristics, physiological roles, catalytic properties in vitro, protein structure, structure-function relationships and inhibition of CYP51. The problems remained in current research and designations of CYP51 inhibitors are also discussed.