| 隋旭 韩斌 杨梦莉 陈香岭 俞建昆 牛华.WEE1 激酶及其抑制剂在抗肿瘤治疗中的应用进展[J].,2016,16(13):2589-2592 |
| WEE1 激酶及其抑制剂在抗肿瘤治疗中的应用进展 |
| Progress in WEE1 Kinase and Its Inhibitor for Anticancer Therapy |
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| DOI： |
| 中文关键词: WEE1 激酶 有丝分裂 检查点 癌症治疗 |
| 英文关键词: WEE1 kinase Mitotic Checkpoint Cancer therapy |
| 基金项目:国家自然科学基金项目（81260066）；高等学校博士点学科点专项科研基金（20111106120056） |
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| 中文摘要: |
| WEE1 激酶是一种细胞周期调节蛋白，能调控细胞周期蛋白依赖性激酶1（cyclin-dependent kinase 1，CDK1）的磷酸化状态，
从而调节CDK1 与细胞周期蛋白B（cyclinB）复合物的活性从而实现对细胞周期的调控，且对DNA 损伤检查点具有重要的调节
作用。WEE1 是G2/M期阻滞的关键基因，起着重要的监测作用，在一些癌症中过表达，抑制或下调WEE1 激酶均能引发有丝分裂
灾难，因此WEE1 激酶抑制剂可能在抗癌治疗中有关键作用。在癌症的治疗过程中，WEE1抑制剂与DNA 损伤剂、化学药物等联
合使用会得到比单独使用更为有效，且在p53 缺失的癌细胞中能发挥更好的效果。目前WEE1 已成为许多癌症治疗的关键靶点
之一，其抑制剂MK-1775 已处于临床研究阶段，且能增强一些DNA 损伤剂对p53 缺失的癌细胞的杀伤能力。本文就WEE1 激酶
及其抑制剂在抗癌治疗中的应用作一综述。 |
| 英文摘要: |
| WEE1 kinase is a kind of cell cycle regulatory proteins. It can control the phosphorylation status of CDK1 so as to
regulate the activity of CDK1 and Cyclin B complex to realize the regulation of cell cycle. WEE1 kinase plays an important role for DNA
damage checkpoint. WEE1 kinase is important to the G2 /Mphase and is overexpression in some cancer. Inhibition or downregulation of
WEE1 kinase could trigger the mitotic catastrophe". Therefore, WEE1 kinase inhibitors may have a key role in anticancer therapy. In the
process of the treatment of cancer, the combination of WEE1 inhibitors with DNA damage agents can be more effective than those of
monotherapy, and in the loss of p53 cancer cells can play a better effect. At present, it has become one of the key targets for many cancer
therapy, its inhibitor MK-1775 has been in clinical research stage, and it can enhance the killing ability of some DNA damaging agents
against the loss of p53 cancer cells. This paper reviewed progress in WEE1 kinase and its inhibitor for anticancer therapy. |
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