Research progress of PoIo-Iike kinase 1 inhibitors targeting PoIo-box domain
10.11665/j.issn.1000-5048.20160101
- VernacularTitle:作用于 Polo-box 结构域的 Polo 样激酶1抑制剂的研究进展
- Author:
Aihong YAO
;
Yujie CHANG
;
Cheng JIANG
;
Haiying SUN
- Publication Type:Journal Article
- Keywords:
Polo-like kinase 1;
Polo-box domain;
inhibitors;
antitumor;
progress
- From:
Journal of China Pharmaceutical University
2016;(1):1-8
- CountryChina
- Language:Chinese
-
Abstract:
The over-expression of Polo-like kinase 1(Plk1)is critical in the producing and progressing of multi-ple 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 substrates 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 also 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 intro-duced,the progress of small molecule and phosphoserine /phosphothreonine contained short peptide Plk1 inhibi-tors targeting PBD was summarized.Further development of this kind of inhibitors was also proposed.
