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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

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

Tsuji Kohei K Hymel David D Burke Terrence R TR

Analytical methods : advancing methods and applications 20200903 36

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<sub>50</sub>) 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. ...[more]

PMID: 32970049

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