董丹丹, 肖燕燕, 刘 伟, 周红刚, 杨 诚. Aurora-B激酶及其抑制剂研究进展J. 药学学报, 2013,48(4): 457-465.
引用本文: 董丹丹, 肖燕燕, 刘 伟, 周红刚, 杨 诚. Aurora-B激酶及其抑制剂研究进展J. 药学学报, 2013,48(4): 457-465.
DONG Dan-dan, XIAO Yan-yan, LIU Wei, ZHOU Hong-gang, YANG Cheng. The research progress of Aurora-B kinase and its inhibitorsJ. 药学学报, 2013,48(4): 457-465.
Citation: DONG Dan-dan, XIAO Yan-yan, LIU Wei, ZHOU Hong-gang, YANG Cheng. The research progress of Aurora-B kinase and its inhibitorsJ. 药学学报, 2013,48(4): 457-465.

Aurora-B激酶及其抑制剂研究进展

The research progress of Aurora-B kinase and its inhibitors

  • 摘要:

    Aurora-B是调节细胞有丝分裂正常进行的重要激酶, 是癌症治疗的重要靶点。Aurora-B在肿瘤中广泛存在过量表达, Aurora-B被抑制时, 肿瘤细胞变得更敏感。鉴于Aurora-B在细胞有丝分裂过程中的关键作用, 针对该激酶开发抑制剂显得越来越重要。现有一些Aurora-B激酶抑制剂已进入临床, 并表现出良好的抗肿瘤活性。本文就Aurora-B激酶的生物学功能、作为抗肿瘤靶标的优势及其抑制剂的临床前及临床研究进行综述。

     

    Abstract:

    Aurora-B as an important kinase to adjust the cell normal mitosis is a potent target for cancer treatment.  Aurora-B is overexpressed in a broad range of tumor and tumor cells are more sensitive while Aurora-B is inhibited.  Due to the key role of the Aurora-B in cell mitosis, the development of its inhibitors is becoming more and more important.  Several small molecules inhibit with a similar efficacy both Aurora-A and Aurora-B, however, in most cases the effects resemble Aurora-B disruption by genetic methods, indicating that Aurora-B represents an effective therapeutic target.  There were several Aurora-B kinase inhibitors which had entered the clinics and displayed good antitumor activity.  In this review, we will outline the functions of Aurora kinase B in normal cell division and in malignancy.  We will focus on recent preclinical and clinical studies that have explored the mechanism of action and clinical effect of Aurora-B inhibitors in cancer treatment.

     

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