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作用于Polo-box结构域的Polo样激酶1抑制剂的研究进展

姚爱红, 常玉杰, 江程, 孙海鹰

姚爱红, 常玉杰, 江程, 孙海鹰. 作用于Polo-box结构域的Polo样激酶1抑制剂的研究进展[J]. 中国药科大学学报, 2016, 47(1): 1-8. DOI: 10.11665/j.issn.1000-5048.20160101
引用本文: 姚爱红, 常玉杰, 江程, 孙海鹰. 作用于Polo-box结构域的Polo样激酶1抑制剂的研究进展[J]. 中国药科大学学报, 2016, 47(1): 1-8. DOI: 10.11665/j.issn.1000-5048.20160101
shu
YAO Aihong, CHANG Yujie, JIANG Cheng, SUN Haiying. Research progress of Polo-like kinase 1 inhibitors targeting Polo-box domain[J]. Journal of China Pharmaceutical University, 2016, 47(1): 1-8. DOI: 10.11665/j.issn.1000-5048.20160101
Citation: YAO Aihong, CHANG Yujie, JIANG Cheng, SUN Haiying. Research progress of Polo-like kinase 1 inhibitors targeting Polo-box domain[J]. Journal of China Pharmaceutical University, 2016, 47(1): 1-8. DOI: 10.11665/j.issn.1000-5048.20160101
shu

作用于Polo-box结构域的Polo样激酶1抑制剂的研究进展

  • 中国药科大学药学院，江苏省药物分子设计与成药性优化重点实验室

基金项目: 国家自然科学基金资助项目(No.81573278)；江苏省高校“青蓝工程”资助项目；江苏省特聘教授资助项目

Research progress of Polo-like kinase 1 inhibitors targeting Polo-box domain

摘要

    摘要
  • 摘要: Polo样激酶1(Plk1)的过度表达在多种肿瘤的发生及发展过程中起着关键作用，目前已有多个不同结构的作用于ATP结合口袋和底物结合位点的小分子Plk1抑制剂进入临床研究。Polo-box结构域(PBD)是Plks特有的结构域，对Plk1在细胞中的定位及其与底物的结合有重要作用，被认为是另一个靶向型Plk1抑制剂研究的潜在靶点。本文介绍了Plk1的PBD功能，从小分子化合物和含有磷酸化的丝氨酸/苏氨酸短肽及其衍生物两个方面综述了作用于PBD的Plk1抑制剂的最新研究进展，并对这类抑制剂的研究前景进行了展望。
    Abstract: The over-expression of Polo-like kinase 1(Plk1)is critical in the production and progression of multiple human tumors and is recognized as an effective target for the development of novel anti-cancer drugs. Currently a variety of small molecules targeting ATP or substrate binding sites have entered different stages of clinical trials. Polo-box domain(PBD)is a unique domain of Plks which plays an important role in the sub-cellular location of Plks and in the recognition of their substrates, therefore it has become an attractive target for the development of novel target-directed Plk1 inhibitors. In this paper, PBD function of Plk1 was introduced, the progress of small molecule and phosphoserine/phosphothreonine contained short peptide Plk1 inhibitors targeting PBD is summarized. Further development of this kind of inhibitors is also proposed.
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  • 刊出日期:  2016-02-24

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