摘要: |
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。 |
关键词: Aurora激酶 抑制剂 结合模式 抗肿瘤 |
DOI: |
分类号:R284.1;R917.101 |
基金项目: |
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Progress of Aurora Kinase and Its Inhibitors |
ZHU Haijing1, JIAO Yu2
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1.The Second Artillery General Hospital of Chinese People’s Liberation Army, Beijing 100088, China;2.Division of Organic Chemistry, China Pharmaceutical University, Nanjing 211198, China
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Abstract: |
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. |
Key words: Aurora kinase inhibitor binding mode anti-tumor |