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

YAO Aihong; CHANG Yujie; JIANG Cheng; SUN Haiying

doi:10.11665/j.issn.1000-5048.20160101

Journal of China Pharmaceutical University > 2016 > 47(1): 1-8. > DOI: 10.11665/j.issn.1000-5048.20160101

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

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

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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.
- Polo-like kinase 1,
- Polo-box domain,
- inhibitors,
- antitumor,
- progress

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