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首页> 外文期刊>Current opinion in pharmacology >Targeting the cell division cycle in cancer: CDK and cell cycle checkpoint kinase inhibitors.
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Targeting the cell division cycle in cancer: CDK and cell cycle checkpoint kinase inhibitors.

机译:针对癌症中的细胞分裂周期:CDK和细胞周期检查点激酶抑制剂。

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摘要

The cyclin-dependent kinase (CDK) family of serine/threonine kinases regulate progression through each stage of the cell division cycle and as such are major targets for deregulation in cancer. This has led to the development of several small-molecule inhibitors of CDKs as potential therapeutic agents for the treatment of this disease. Progression through the cell cycle is also monitored at several positions known as cell cycle checkpoints, two of which occur during G1 and G2 in response to DNA damage. These are often defective in cancer, leading to the suggestion that inhibition of one or both of the cell cycle checkpoint kinases CHK1 and CHK2 may drive a cancer cell that already has defects in its cell cycle checkpoints towards death.
机译:丝氨酸/苏氨酸激酶的细胞周期蛋白依赖性激酶(CDK)家族可调节细胞分裂周期各个阶段的进程,因此是癌症中放松调节作用的主要靶点。这导致了几种小分子CDK抑制剂的开发,作为CDKs潜在的治疗剂。还可以在几个称为细胞周期检查点的位置监视整个细胞周期的进程,其中两个响应于DNA损伤在G1和G2期间发生。这些通常在癌症中是有缺陷的,从而提示对细胞周期检查点激酶CHK1和CHK2中的一个或两个的抑制可能会导致已经在其细胞周期检查点中存在缺陷的癌细胞死亡。

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