Aurora-B激酶及其抑制剂研究进展
The research progress of Aurora-B kinase and its inhibitors
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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, 当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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