细胞周期蛋白依赖性激酶2（CDK2）化学抑制的结构基础
Structural basis for chemical inhibition of CDK2.
作者信息
Kim S H, Schulze-Gahmen U, Brandsen J, de Azevedo Júnior W F
机构信息
Department of Chemistry, Lawrence Berkeley National Laboratory, University of California 94720, USA.
出版信息
Prog Cell Cycle Res. 1996;2:137-45. doi: 10.1007/978-1-4615-5873-6_14.
The central role of cyclin-dependent kinases (CDKs) in cell cycle regulation makes them a promising target for discovering small inhibitory molecules that can modify the degree of cell proliferation. The three-dimensional structure of CDK2 provides a structural foundation for understanding the mechanisms of activation and inhibition of CDK2 and for the discovery of inhibitors. In this article five structures of human CDK2 are summarised: apoprotein, ATP complex, olomoucine complex, isopentenyladenine complex, and des-chloro-flavopiridol complex.
细胞周期蛋白依赖性激酶（CDK）在细胞周期调控中的核心作用使其成为发现能够改变细胞增殖程度的小分子抑制性分子的一个有前景的靶点。CDK2的三维结构为理解CDK2的激活和抑制机制以及发现抑制剂提供了结构基础。本文总结了人CDK2的五种结构：脱辅基蛋白、ATP复合物、olomoucine复合物、异戊烯基腺嘌呤复合物和去氯黄酮哌啶醇复合物。
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