Aurora Kinase Inhibitors: Current Status and Outlook.
Aurora Kinase Inhibitors: Current Status and Outlook.
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DOI：
10.3389/fonc.2015.00278
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发表时间：
2015
影响因子：
4.7
通讯作者：
Linardopoulos S
中科院分区：
文献类型：
--
作者：
Bavetsias V;Linardopoulos S
Aurora激酶家族包括对有丝分裂重要的细胞周期调节的丝氨酸/苏氨酸激酶。它们的活性和蛋白质表达受细胞周期调节，在有丝分裂期间达到峰值以协调重要的有丝分裂过程，包括中心体成熟、染色体排列、染色体分离和胞质分裂。在人类中，Aurora激酶家族由三个成员组成：Aurora-A、Aurora-B和Aurora-C，它们各自共享保守的C末端催化结构域，但在亚细胞定位、底物特异性和有丝分裂期间的功能方面不同。此外，已发现Aurora-A和Aurora-B在多种人类肿瘤中过表达。这些观察结果导致了学术和制药组织之间的许多项目，以发现小分子极光激酶抑制剂作为抗癌药物。本文将总结目前已知的极光激酶抑制剂在临床上，并讨论了当前和未来的发展方向。
The Aurora kinase family comprises of cell cycle-regulated serine/threonine kinases important for mitosis. Their activity and protein expression are cell cycle regulated, peaking during mitosis to orchestrate important mitotic processes including centrosome maturation, chromosome alignment, chromosome segregation, and cytokinesis. In humans, the Aurora kinase family consists of three members; Aurora-A, Aurora-B, and Aurora-C, which each share a conserved C-terminal catalytic domain but differ in their sub-cellular localization, substrate specificity, and function during mitosis. In addition, Aurora-A and Aurora-B have been found to be overexpressed in a wide variety of human tumors. These observations led to a number of programs among academic and pharmaceutical organizations to discovering small molecule Aurora kinase inhibitors as anti-cancer drugs. This review will summarize the known Aurora kinase inhibitors currently in the clinic, and discuss the current and future directions.