Aurora激酶及其抑制剂的研究进展

Progress of Aurora Kinase and Its Inhibitors

目的从结构出发介绍Aurora激酶及其抑制剂的研究进展。方法总结Aurora激酶抑制剂骨架特征和结合模式,以及进入临床的Aurora激酶抑制剂的研究进展。结果和结论 Aurora激酶家族是肿瘤治疗的一个新兴靶标。腺嘌呤骨架可能是设计高活性Aurora激酶抑制剂的重要母核。

OBJECTIVE To introduce the research progress of Aurora kinase and its inhibitors based on their structures. METHODS To summarize the chemical scaffold, the common binding modes, and the clinical progress of Aurora kinase inhibitors. RESULTS CONCLUSION The Aurora kinase had emerged as an attractive target for cancer therapies. The adenosine mimic scaffolds could be used for further study to design addtional potential inhibitors of Aurora with high inhibitory activity.