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Aurora激酶抑制药研究进展

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摘要 Aurora激酶是近年来发现的新型抗肿瘤靶点,它在肿瘤的发生发展中起到至关重要的作用。该文从Aurora激酶作为抗肿瘤靶点的意义,Aurora-A激酶特异性抑制药及临床应用,Aurora-B激酶特异性抑制药及临床应用,Pan-Aurora激酶特异性抑制药及临床应用等几个方面,对Aurora激酶抑制药的研究进展进行论述,期望能够对临床工作者有所帮助。
作者 姚汝铖 郑军
机构地区 三峡大学第一临床医学院普外科
出处 《医药导报》 CAS 北大核心 2013年第7期919-923,共5页 Herald of Medicine
基金 三峡大学研究生科研创新基金资助项目(2012CX059)
关键词 Aurora激酶抑制药 AURORA激酶 抗肿瘤靶点
分类号 R979.1 [医药卫生—药品]
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  • 1SABINO D, BROWN N H, BASTO R. Drosophila Ajuba is not an Aurora A activator but is required to maintain Aurora A at the centrosome [ J ]. J Cell Sci, 2011,124 ( Pt 7 ) : 1156-1166.
  • 2GAUTSCHI O, HEIGHWAY J, MACK P C. Aurora kinases as anticancer drug targets [ J ]. Clin Cancer Res, 2008, lg (6) :1639-1648.
  • 3SEN S,ZHOU H,WHITE R A. A putative serine/threonine kinase encoding gene BTAK on chromosome 20q13 is amplified and overexpressed in human breast cancer cell lines [ J ]. Oncogene, 1997,14 ( 18 ) : 2195-2200.
  • 4LIU Q, KANEKO S, YANG L, et" al. Aurora A abrogation of p53 DNA binding and transactivation activity by phosphorylation of serine 215 [ J ]. J Biol Chem, 2004,279 (50) :52175-52182.
  • 5TERAKAWA T, MIYAKE H, KUMANO M, et al. Growth in- hibition and enhanced chemosensitivity induced by down- regulation of Aurora A in human renal cell carcinoma Caki- 2 cells using short hairpin RNA[J]. Oncol Lett,2011,2 (4) :713-717.
  • 6KIM S J,JANG J E,CHEONG J W,et al. Aurora A kinase expression is increased in leukemia stem cells, and a selective Aurora A kinase inhibitor enhances Ara-C-induced apoptosis in acute myeloid leukemia stem cells [ J ]. Korean J Hematol,2012,47 (3) : 178-185.
  • 7WAN X B, LONG Z J, YAN M, et al. Inhibition of Aurora A suppresses epithelial-mesenchymal transition and invasion by downregulating MAPK in nasopharyngeal carcinoma cells [ J ]. Carcinogenesis, 2008,29 ( ! 0 ): 1930 - 1937.
  • 8SELLS T, ECSEDY J, STROUD S, et al. MLN8237 : an orally active small molecule inhibitor of Aurora A kinase in phaseI clinical trials [ C ]. AACR Ann Meeting, 2008, San Francisco, CA, USA, Abstract 237.
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医药导报
2013年 第7期

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