一种用于评估polo样激酶1 ATP竞争性抑制剂的新型荧光恢复测定法。
A new genre of fluorescence recovery assay to evaluate polo-like kinase 1 ATP-competitive inhibitors.
作者信息
Tsuji Kohei, Hymel David, Burke Terrence R
机构信息
Chemical Biology Laboratory, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Frederick, Maryland, 21702 USA.
出版信息
Anal Methods. 2020 Sep 28;12(36):4418-4421. doi: 10.1039/d0ay01223h. Epub 2020 Sep 3.
Abstract
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 half maximal inhibitory concentration (IC) 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.
摘要
我们使用一种由强力polo样激酶1（Plk1）抑制剂BI2536的荧光素标记变体[FITC-PEG-Lys(BI2536)4]组成的探针，通过荧光恢复测定法确定了Plk1的ATP竞争性1型抑制剂的半数最大抑制浓度（IC）。对于潜在Plk1抑制剂的初步筛选，该方法是一种经济高效且简单的传统激酶测定替代方法。
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