Boss David S, Beijnen Jos H, Schellens Jan H M
The Netherlands Cancer Institute, Plesmanlaan 121, 1066 CX Amsterdam, The Netherlands.
Oncologist. 2009 Aug;14(8):780-93. doi: 10.1634/theoncologist.2009-0019. Epub 2009 Aug 14.
The aurora kinase family of serine/threonine kinases comprises three members, designated auroras A, B, and C. Auroras A and B are essential components of the mitotic pathway, ensuring proper chromosome assembly, formation of the mitotic spindle, and cytokinesis. The role of aurora C is less clear. Overexpression of aurora A and B has been observed in several tumor types, and has been linked with a poor prognosis of cancer patients. Several small molecules targeting aurora kinases A and B or both have been evaluated preclinically and in early phase I trials. In this review we aim to summarize the most recent advances in the development of aurora kinase inhibitors, with a focus on the clinical data.
丝氨酸/苏氨酸激酶的极光激酶家族由三个成员组成,分别命名为极光激酶A、B和C。极光激酶A和B是有丝分裂途径的重要组成部分,确保染色体正确组装、有丝分裂纺锤体形成和胞质分裂。极光激酶C的作用尚不清楚。在几种肿瘤类型中均观察到极光激酶A和B的过表达,且这与癌症患者的不良预后相关。几种靶向极光激酶A和B或两者的小分子已在临床前和I期早期试验中进行了评估。在本综述中,我们旨在总结极光激酶抑制剂开发的最新进展,重点关注临床数据。