极光激酶
激酶
生物
极光抑制剂
Polo样激酶
极光激酶B
丝氨酸苏氨酸激酶
癌症研究
细胞周期
白血病
极光A激酶
细胞周期蛋白依赖激酶
有丝分裂
磷酸化
细胞周期检查点
髓系白血病
细胞周期蛋白依赖激酶1
细胞生长
细胞周期蛋白依赖激酶2
细胞生物学
癌症
蛋白激酶A
遗传学
细胞
主轴装置
细胞分裂
作者
Benjamin Goldenson,John D. Crispino
出处
期刊:Oncogene
[Springer Nature]
日期:2015-01-29
卷期号:34 (5): 537-545
被引量:202
摘要
The Aurora kinases, which include Aurora A (AURKA), Aurora B (AURKB) and Aurora C (AURKC), are serine/threonine kinases required for the control of mitosis (AURKA and AURKB) and meiosis (AURKC). Since their discovery nearly 20 years ago, Aurora kinases have been studied extensively in cell and cancer biology. Several early studies found that Aurora kinases are amplified and overexpressed at the transcript and protein level in various malignancies, including several types of leukemia. These discoveries and others provided a rationale for the development of small-molecule inhibitors of Aurora kinases as leukemia therapies. The first generation of Aurora kinase inhibitors did not fare well in clinical trials, owing to poor efficacy and high toxicity. However, the creation of second-generation, highly selective Aurora kinase inhibitors has increased the enthusiasm for targeting these proteins in leukemia. This review will describe the functions of each Aurora kinase, summarize their involvement in leukemia and discuss inhibitor development and efficacy in leukemia clinical trials.
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