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.
See: A new genre of fluorescence recovery assay to evaluate polo-like kinase 1 ATP-competitive inhibitors by Kohei Tsuji, David Hymel and Terrence R. Burke, Jr. in Analytical Methods, 2020, 12, 4418 -4421.
This article can be accessed directly from the Royal Society of Chemistry at https://pubs.rsc.org/en/content/articlelanding/2020/AY/D0AY01223H#!divAb...
Analytical Methods, 2020, 12, 4418 -4421.