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 (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.

中文翻译：

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一种新类型的荧光恢复试验，用于评估 polo 样激酶 1 ATP 竞争性抑制剂。

使用由强效 polo 样激酶 1 (Plk1) 抑制剂 BI2536 [FITC-PEG-Lys(BI2536) 4 ]的荧光素标记变体组成的探针，我们能够确定ATP 的半数最大抑制浓度 (IC ₅₀ ) -通过荧光恢复测定的 Plk1 竞争性 1 型抑制剂。这种方法代表了传统激酶检测的一种经济高效且简单的替代方法，用于初步筛选潜在的 Plk1 抑制剂。