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

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 (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.

SUBMITTER: Tsuji K 

PROVIDER: S-EPMC7523589 | biostudies-literature | 2020 Sep

REPOSITORIES: biostudies-literature