Rudolph Johannes
Department of Biochemistry, Duke University Medical Center, Durham, North Carolina 27710, USA.
Biochemistry. 2007 Mar 27;46(12):3595-604. doi: 10.1021/bi700026j. Epub 2007 Mar 1.
Cdc25 phosphatases, as activators of the Cdk/cyclins, play critical roles in the regulation of the eukaryotic cell cycle. Because of their overexpression and correlation with poor prognosis in many diverse cancers, Cdc25 phosphatases are attractive targets for anticancer drug development. Over the past few years, much knowledge of the basic enzymology of the Cdc25 phosphatases that may aid in the development of specific inhibitors has been gained. We review herein the structure, specificity, and mechanism of the Cdc25 phosphatases with a special focus on the activity of Cdc25 phosphatases with native protein substrates.
细胞周期蛋白磷酸酶25(Cdc25磷酸酶)作为细胞周期蛋白依赖性激酶(Cdk)/细胞周期蛋白的激活剂,在真核细胞周期调控中发挥着关键作用。由于其在多种癌症中过表达且与不良预后相关,Cdc25磷酸酶成为抗癌药物开发的有吸引力的靶点。在过去几年中,我们已经获得了许多关于Cdc25磷酸酶基本酶学的知识,这些知识可能有助于开发特异性抑制剂。我们在此综述Cdc25磷酸酶的结构、特异性和作用机制,特别关注Cdc25磷酸酶对天然蛋白质底物的活性。