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蛋白激酶及其治疗应用。

Protein kinases and their therapeutic exploitation.

作者信息

Johnson L

机构信息

Laboratory of Molecular Biophysics, University of Oxford, UK.

出版信息

Biochem Soc Trans. 2007 Feb;35(Pt 1):7-11. doi: 10.1042/BST0350007.

Abstract

This review focuses on the recognition properties of protein kinases at the molecular level. Phosphorylation of the substrate protein by a protein kinase can result in enzyme activation or inhibition, conformational changes that change recognition properties, or the creation of a surface with distinct binding properties. Protein kinases have become important targets for the development of inhibitors with potential therapeutic application. Various examples are considered in this review, and I discuss our own work on glycogen phosphorylase and phosphorylase kinase, and the structures of proteins involved with the cell cycle, including cyclins and cyclin-dependent kinases.

摘要

本综述聚焦于蛋白激酶在分子水平上的识别特性。蛋白激酶对底物蛋白的磷酸化作用可导致酶的激活或抑制、改变识别特性的构象变化,或形成具有独特结合特性的表面。蛋白激酶已成为开发具有潜在治疗应用的抑制剂的重要靶点。本综述考虑了各种实例,并讨论了我们自己关于糖原磷酸化酶和磷酸化酶激酶的研究工作,以及与细胞周期相关的蛋白质结构,包括细胞周期蛋白和细胞周期蛋白依赖性激酶。

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