期刊文献+

小分子极光激酶抑制剂的研究进展

Advances on small-miolecule aurora kinase inhibitors
原文传递
导出
摘要 极光激酶是丝氨酸/苏氨酸激酶家族的成员之一。在有丝分裂细胞周期中极光激酶负责纺锤体的组装、染色体与中心体的分离,以及细胞质的分离等多个过程。极光激酶的异常将导致细胞功能紊乱,研究表明极光激酶在多种肿瘤细胞中高表达并且参与肿瘤细胞的形成。近年已经陆续发现了多种类型的小分子极光激酶抑制剂,本文主要对小分子极光激酶抑制剂的研究进行综述。 Aurora kinase family is a member of the serine/threonine kinases.In the cell mitotic cycle,aurora kinases are responsible for spindle assembling,chromosome and centrosome separating,and cytoplasmic isolating and multiple process.The abnormalities of aurora kinase will lead to the centrosome abnormalities of cells cmitotic and abnormalities of cell cycle checkpoint and polyploid arising.Many studies have shown that aurora kinase is highly expressed in many tumor cells and is involved in tumor formation.In recent years,a variety of small molecule aurora kinase inhibitors have been discovered.In this paper,the research progress of various types of small molecule inhibitors of aurora kinase will be overviewed.
机构地区 辽宁大学药学院
出处 《中国药物化学杂志》 CAS CSCD 2016年第3期225-235,共11页 Chinese Journal of Medicinal Chemistry
基金 辽宁大学青年科研基金资助项目(LDQN201436) 辽宁省教育厅科学研究一般项目(L2015201)
关键词 极光激酶 有丝分裂 肿瘤 抑制剂 aurora kinase mitotic tumor inhibitor
  • 相关文献

参考文献38

  • 1KITZEN J,de JONGE M J A,VERWEIJ J.Aurora kinase inhibitors[J].Crit Rev Oncol Hemat,2010,73(2):99-110.
  • 2VADER G,LENS S M A.The aurora kinase family in cell division and cancer[J].BBA-Rev Cancer,2008,1786(1):60-72.
  • 3SHINDO M,NAKANO H,KUROYANAGI H,et al.cDNA cloning,expression,subcellular localization,and chromosomal assignment of mammalian aurora homologues,aurora-related kinase(ARK)1 and 2[J].Biochem Biophys Res Commun,1998,244(1):285-292.
  • 4GIET R,UZBEKOV R,CUBIZOLLES F,et al.The xenopus laevis aurora-related protein kinase pEg2 associates with and phosphorylates the kinesin-related protein XlEg5[J].J Biol Chem,1999,274(21):15005-15013.
  • 5CHI H.Sphingosine-1-phosphate and immune regulation:trafficking and beyond[J].Trends Pharmacol Sci,2011,32(1):16-24.
  • 6MURATA-HORI M TATSUKA M,WANG Y L.Probing the dynamics and functions of Aurora B kinase in living cells during mitosis and cytokinesis[J].Mol Biol Cell,2002 13(4):1099-1108.
  • 7BERNARD M,SANSEAU P,HENRY C,et al.Cloning of STK13 a third human protein kinase related to drosophi-1a aurora and budding yeast Ipl1 that maps on chromosome 19q13.3-ter[J].Genomics,1998,53(3):406-409.
  • 8LI X,SAKASHITA G,MATSUZAKI H et al.Direct association with inner centromere protein(INCENP)activates the novel chromosomal passenger protein,Aurora-C[J].J Biol Chem,2004,279(45):47201-47211.
  • 9MORIARTY K J,KOBLISH H K,GARRABRANT T,et al.The synthesis and SAR of 2-amino-pyrrolo[2,3-d]pyrimidines:a new class of Aurora-A kinase inhibitors[J].Bioorg Med Chem Lett,2006,16(22):5778-5783.
  • 10LAWRENCE H R,MARTIN M P,LUO Y,et al.Development of o-chlorophenyl substituted pyrimidines as exceptionally potent aurora kinase inhibitors[J].J Med Chem,2012 55(17):7392-7416.

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部