A new genre of fluorescence recovery assay to evaluate polo-like kinase 1 ATP-competitive inhibitors

被引：3
|
作者：
Tsuji, Kohei [1 ,2 ]
Hymel, David [1 ]
Burke, Terrence R., Jr. [1 ]
机构：
[1] NIH, NCI, Chem Biol Lab, Ctr Canc Res, Frederick, MD 21702 USA
[2] Tokyo Med & Dent Univ TMDU, Dept Med Chem, Inst Biamatenals & Bioengn, Chiyoda Ku, 2-3-10 Kandasurugadai, Tokyo 1010062, Japan
来源：
ANALYTICAL METHODS | 2020年 / 12卷 / 36期
关键词：
BINDING ASSAY; BOX DOMAIN; POTENT; POLO-LIKE-KINASE-1; PLK1;
D O I：
10.1039/d0ay01223h
中图分类号：
O65 [分析化学];
学科分类号：
070302 ; 081704 ;
摘要：
Using a probe consisting of a fluorescein-labeled variant of the potent polo-like kinase 1 (Plk1) inhibitor BI2536 [FITC-PEG-Lys(BI2536) 4], we were able to determine halfmaximal inhibitory concentration (IC50) of ATP-competitive Type 1 inhibitors of Plk1 by means of a fluorescence recovery assay. This methodology represents a cost-effective and simple alternative to traditional kinase assays for initial screening of potential Plk1 inhibitors.
引用
收藏
页码：4418 / 4421
页数：4
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