AuroraB激酶及其抑制剂研究进展.pdfVIP

药学学报 Acta Pharmaceutica Sinica 20 13, 48 (4): 457 465 ·457 · Aurora-B 激酶及其抑制剂研究进展 2, 3 2, 3 1, 2* 2, 3 2, 3 董丹丹 , 肖燕燕 , 刘 伟 , 周红刚 , 杨 诚 (1. 天津科技大学理学院, 天津 300457; 2. 天津市国际生物医 联合研究院高通量 物筛选中心, 天津 300457; 3. 南开大学药学院, 天津 300071) 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, 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。 关键词: Aurora-B; 细胞有丝分裂; 激酶抑制剂; 抗肿瘤药物 中图分类号: R9 16 文献标识码: A 文章编号: 0513-4870 (20 13) 04-0457-09 The research progress of Aurora-B kinase and its inhibitors DONG Dan-dan2, 3, XIAO Yan-yan2, 3, LIU Wei1, 2*, ZHOU Hong-gang2, 3, YANG Cheng2, 3 (1. College of Sciences, Tianjin University of Science and Technology, Tianjin 30045 7, China; 2. High Throughput Molecular Drug Discovery Center, Tianj in International Joint A cademy of Biotechnology and Medicine, Tianj in 30045 7, China; 3. College of Pharmacy, Nankai University, Tianjin 300071, China ) Abstract : Aurora-B as an important kinase to adj ust 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 Auror