Targeting the cell division cycle in cancer: CDK and cell cycle checkpoint kinase inhibitors
Targeting the cell division cycle in cancer: CDK and cell cycle checkpoint kinase inhibitors
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DOI：
10.1016/j.coph.2005.04.009
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发表时间：
2005-08-01
影响因子：
4
通讯作者：
Garrett, MD
中科院分区：
文献类型：
--
作者：
Collins, I;Garrett, MD
丝氨酸/苏氨酸激酶的细胞周期蛋白依赖性激酶（CDK）家族通过细胞分裂周期的每个阶段调节进展，因此是癌症中失调的主要靶标。这导致了几种CDK的小分子抑制剂作为治疗这种疾病的潜在治疗剂的发展。细胞周期的进程也在几个被称为细胞周期检查点的位置进行监测，其中两个检查点发生在G（1）和G（2）期间，以响应DNA损伤。这些在癌症中通常是有缺陷的，导致细胞周期检查点激酶CHK 1和CHK 2中的一种或两种的抑制可能会驱使已经在其细胞周期检查点中存在缺陷的癌细胞走向死亡。
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 G(1) and G(2) 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.