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

  1. Author:
    Tsuji, Kohei
    Hymel, David
    Burke,Terrence
  2. Author Address

    Chemical Biology Laboratory, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Frederick, Maryland, 21702 USA. burkete@mail.nih.gov.,
    1. Year: 2020
    2. Date: Sep 28
    3. Epub Date: 2020 09 03
  1. Journal: Analytical methods : advancing methods and applications
    1. 12
    2. 36
    3. Pages: 4418-4421
  2. Type of Article: Article
  3. ISSN: 1759-9660
  1. 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.

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External Sources

  1. DOI: 10.1039/d0ay01223h
  2. PMID: 32970049
  3. WOS: 000572249700012

Library Notes

  1. Fiscal Year: FY2020-2021
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