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

Anal Methods. 2020 Sep 28;12(36):4418-4421. doi: 10.1039/d0ay01223h. Epub 2020 Sep 3.

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.

Publication types

  • Research Support, N.I.H., Intramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine Triphosphate
  • Cell Cycle Proteins*
  • Fluorescence
  • Polo-Like Kinase 1
  • Protein Serine-Threonine Kinases*
  • Proto-Oncogene Proteins

Substances

  • Cell Cycle Proteins
  • Proto-Oncogene Proteins
  • Adenosine Triphosphate
  • Protein Serine-Threonine Kinases