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抗肿瘤新靶点——极光激酶及其小分子抑制剂研究进展 被引量：2

Novel anti-tumor targets: aurora kinases and their small molecule inhibitors
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摘要 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.
作者 陈聪琴 范艳华 吕文文 赵庆春
机构地区 沈阳军区总医院药剂科 沈阳药科大学药学院
出处 《国际药学研究杂志》 CAS CSCD 2013年第1期73-78,104,共7页 Journal of International Pharmaceutical Research
关键词 极光激酶 抗肿瘤药 有丝分裂 抑制剂 aurora kinases antineoplastic agents mitosis inhibitors
分类号 R96 [医药卫生—药理学]
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参考文献36

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共引文献8

同被引文献22

  • 1李强,吴燕华,闫晓梅,余龙,赵寿元.极光(aurora)激酶在细胞有丝分裂和肿瘤形成中的重要功能[J].生命科学,2005,17(5):424-432. 被引量：9
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国际药学研究杂志
2013年 第1期

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