极光激酶家族是一类结构与功能高度保守的丝氨酸/苏氨酸激酶,参与细胞有丝分裂中中心体成熟分离、纺锤体组装、染色体分离及胞质分裂等多个过程.极光激酶表达或功能异常都会导致遗传物质分配紊乱,继而影响基因组的稳定性.近年来,相关研究已证实极光激酶在多种肿瘤细胞中高表达并参与肿瘤的形成.目前已发现了一系列具有抑癌作用的小分子极光激酶抑制剂,有些已经进入临床试验阶段.本文主要对哺乳动物的3种极光激酶及其小分子抑制剂的研究进展进行综述.%Aurora kinases are a family of serine/threoning kinases whose structures and functions are highly conserved in different model organisms. They play significant roles in many events during cell mitosis, such as centrosome maturation and separation, spindle assembly and maintenance, chromosome segregation, cytokinesis. Overexpression of aurora kinases has been observed in some tumor cells and aberrations in aurora kinases have been proved to be strongly associated with tumorigenesis. Up to now, some small molecule aurora kinase inhibitors with anti-tumor activity have been developed. Some of those with promising pre-clinical results have reached clinical trial. This review describes the recent progress of aurora kinases and their small molecule inhibitors.
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