Aurora激酶抑制剂的研究进展  

Advances in studies on anticancer activity of Aurora inhibitors

作　　者：刘经国[1,2] 邓小莲[1] 刘金雷[1,2] 邹美香[2] 王玉成[3] 李祎亮[2,3] 

机构地区：[1]广西中医学院药学院,南宁530001 [2]天津药物研究院,天津市新药设计与发现重点实验室,天津300193 [3]中国医学科学院医药生物技术所,北京100050

出　　处：《中国抗生素杂志》2010年第9期641-646,共6页Chinese Journal of Antibiotics

摘　　要：在有丝分裂的过程中,Aurora激酶参与纺锤体形成,中心体成熟,染色体分化和胞质分裂。Aurora激酶的过度表达或分化易导致有丝分裂异常,与形成肿瘤的基因组不稳定性密切相关。以Aurora激酶为靶点设计、合成的药物已成为近年来肿瘤药物治疗的研究热点。本文综述了已经进入临床研究的Aurora小分子抑制剂在临床前、临床的研究进展。Aurora kinase are essential for spindle assembly, centrosome maturation, chromosomal segregation and cytokinesis during mitosis. Abnormalities in the mitotic process as a result of overexpression amplification of Aurora have been linked to genomic instability leading to tumorigenesis. The use of Aurora kinase small-molecule inhibitors as a potential molecular-targeted therapeutic intervention for cancer is being pursued by various researchers. In this paper, we review the Aurora kinase small-molecule inhibitors has entered the clinical in pre-clinical and clinical testing research advances.

关 键 词：AURORA激酶抑制剂 有丝分裂 抗肿瘤作用 

分 类 号：R931.71[医药卫生—生药学]