Preparation of CDK/Cyclin Inhibitor Complexes for Structural Determination.
Preparation of CDK/Cyclin Inhibitor Complexes for Structural Determination.
复制标题
用于结构测定的 CDK/细胞周期蛋白抑制剂复合物的制备。
DOI：
10.1007/978-1-4939-2926-9_4
复制
发表时间：
2016
期刊：
影响因子：
--
通讯作者：
Kontopidis,George
中科院分区：
文献类型：
--
作者：
Grigoroudis,AsteriosI;Kontopidis,George
细胞周期蛋白依赖性蛋白激酶(CDKs)丰富的生化和结构知识使我们对其作用机制的分子决定因素有了全面而又不是详尽的了解。实现结构和功能的CDK模型以开发针对单个或多个CDK的新的抗癌策略仍然是一个关键的需求。迄今为止，已有250多个CDK的晶体结构可用，包括截断或完整的，修饰的或未修饰的，活性或非活性的形式，与周期蛋白和/或它们各自的假定的抑制剂共结晶，然而，据我们所知，到目前为止还没有可用的核磁共振解析结构。到目前为止，我们试图在概述已经阐明的CDK的结构、构筑和每种情况下的优选表达载体的基础上，为CDK/Inhibitors复合体的蛋白质生产到结晶提供有用的指导，以便产生各自的晶体。
The abundance of biochemical and structural knowledge on the Cyclin-Dependent Kinases (CDKs) has provided a comprehensive but not exhaustive insight into the molecular determinants that govern their function mechanisms. The implementation of structural and functional CDK models towards developing novel anticancer strategies that will specifically target individual or multiple CDKs remains a critical need.More than 250 CDKs crystal structures are available to-date, including truncated or whole, modified or not, active or inactive forms, co-crystallized with the cyclins and/or their respective putative inhibitors, though, to our knowledge, there is no NMR solved structure available to date. We hitherto attempt to provide a useful guide from protein production to crystallization for CDK/Inhibitors complexes based on an overview of the already elucidated CDK structures, constructs and the preferable expression vectors in each case, in order to yield the respective crystals.