A new genre of fluorescence recovery assay to evaluate polo-like kinase 1 ATP-competitive inhibitors. Issue 36 (3rd September 2020)

• Record Type: Journal Article
• Authors: Tsuji, Kohei; Hymel, David; Burke, Terrence R.
• Is Part Of: Analytical methods. Volume 12:Issue 36(2020)
• Page Start: 4418
• Page End: 4421
• Publication Date: 2020-09-03
• Subjects: Chemistry, Analytic -- Periodicals; Analytical biochemistry -- Periodicals; Chemical laboratories -- Standards -- Periodicals; 543.1905
• DOI: 10.1039/d0ay01223h
• Languages: English
• ISSNs: 1759-9660

Abstract

Abstract : Using a probe consisting of a fluorescein-labeled variant of the potent polo-like kinase 1 (Plk1) inhibitor BI2536, we determined the IC50 of ATP-competitive Type 1 inhibitors of Plk1 by means of a fluorescence recovery assay. 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.