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化学进展 2007, Vol. 19 Issue (05): 762-768 前一篇   后一篇

• 综述与评论 •

环肽类组蛋白去乙酰化酶抑制剂*

李晓晖1**;李建勋1;李世荣1;修志龙1;西野宪和2

  

  1. 1.大连理工大学环境与生命学院 大连 116024;

    2.日本九州工业大学 大学院生命体工学研究科 北九州 808-0196

  • 收稿日期:2006-07-20 修回日期:2006-09-22 出版日期:2007-05-24 发布日期:2007-05-24
  • 通讯作者: 李晓晖
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Cyclic Peptide Histone Deacetylases Inhibitors

Li Xiaohui1**; Li Jianxun1; Li Shirong1;Xiu Zhilong1;Nishino Norikazu2   

  1. 1.School of Environmental and Biological Science and Technology , Dalian University of Technology ,Dalian 116024, China;

    2.Graduate School of Life Science and Systems Engineering, Kyushu Institute of Technology, Kyushu 808-0196,Japan

  • Received:2006-07-20 Revised:2006-09-22 Online:2007-05-24 Published:2007-05-24
组蛋白乙酰化转移酶(HAT)和组蛋白去乙酰化酶(HDAC)调节组蛋白乙酰化程度，HDAC在基因表达和染色体形成等方面起着重要的调节作用。HDAC抑制剂能够引起肿瘤细胞生长停滞、诱导肿瘤细胞分化和调亡。通过对各种HDAC抑制剂结构及作用机制的研究有助于该类药物在临床上的应用和拓宽癌症治疗的适用范围。本文概述了近年来天然及合成的环肽类组蛋白去乙酰化酶抑制剂的研究进展。
关键词： 组蛋白乙酰转移酶, 组蛋白去乙酰化酶, 组蛋白去乙酰化酶抑制剂, 环肽
Histones acetyltransferases (HAT) and histone deacetylases (HDACs) as the corresponding enzymes regulate the change of histones in two antagonist forms, acetylated or deacetylated. In recent years, inhibition of HDACs has emerged as a potential strategy in human cancer therapy, since these enzymes play a fundamental role in regulating gene expression and chromatin assembly. The histone deacetylases inhibitors (HDACIs) are potent inducers of growth arrest, differentiation and apoptosis of tumor cells, and have entered clinical trials for both solid and liquid tumors. However, the molecular basis for their anticancer selectivity remains largely unknown. An improved understanding of the structure and action mechanism of HDAC inhibitors will likely accelerate the clinical development and broaden the future scope and utility ofHDAC inhibitors will likely accelerate the clinical development and broaden the future scope and utility of HDAC inhibitors for cancer treatment. In this review, we summarize recent advances of the HDACs inhibitors of cyclic peptide in structure, mechanism of action, clinical development.
Key words: histone acetylases, histone deacetylases, histone deacetylases inhibitors, cyclic peptides

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环肽类组蛋白去乙酰化酶抑制剂*