Nature Communications (Jun 2020)

Chemical genetics strategy to profile kinase target engagement reveals role of FES in neutrophil phagocytosis

  • Tom van der Wel,
  • Riet Hilhorst,
  • Hans den Dulk,
  • Tim van den Hooven,
  • Nienke M. Prins,
  • Joost A. P. M. Wijnakker,
  • Bogdan I. Florea,
  • Eelke B. Lenselink,
  • Gerard J. P. van Westen,
  • Rob Ruijtenbeek,
  • Herman S. Overkleeft,
  • Allard Kaptein,
  • Tjeerd Barf,
  • Mario van der Stelt

DOI
https://doi.org/10.1038/s41467-020-17027-5
Journal volume & issue
Vol. 11, no. 1
pp. 1 – 20

Abstract

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Chemical tools to monitor drug-target engagement of endogenous enzymes are essential for preclinical target validation. Here, the authors present a chemical genetics strategy to study target engagement of endogenous kinases, achieving specific labeling and inactivation of FES kinase to provide insights into FES’ role in neutrophil phagocytosis.