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Chemical inhibitors of cyclin-dependent kinases.
Trends in Cell Biology ( IF 19.0 ) Pub Date : 1996-10-01 , DOI: 10.1016/0962-8924(96)10034-9
L Meijer 1
Affiliation  

Transient activation o f cyclin-dependent kinases (CDKs) is responsible for transition through the successive phases of the cell-division cycle. Major changes in the expression and regulation of CDKs have been described in human tumours. Enzymatic screening is starting to uncover chemical inhibitors o f CDKs that arrest the cell cycle at various steps. This review summarizes our knowledge of the first generation inhibitors, their molecular mechanisms of action and their effects on the cell cycle and apoptosis, and discusses their potential as synchronizing agents, as ligands for affinity chromatography and as therapeutic agents.

中文翻译:

细胞周期蛋白依赖性激酶的化学​​抑制剂。

细胞周期蛋白依赖性激酶(CDKs)的瞬时激活负责整个细胞分裂周期的连续阶段。在人类肿瘤中已经描述了CDKs表达和调控的主要变化。酶促筛选开始发现CDK的化学抑制剂,这些抑制剂在各个步骤都可阻止细胞周期。这篇综述总结了我们对第一代抑制剂的了解,它们的分子作用机理以及它们对细胞周期和细胞凋亡的影响,并讨论了它们作为同步剂,亲和色谱配体和治疗剂的潜力。
更新日期:2019-11-01
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