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

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 insig...

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Bibliographic Details
Main Authors: 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
Format: Article
Language:English
Published: Nature Publishing Group 2020-06-01
Series:Nature Communications
Online Access:https://doi.org/10.1038/s41467-020-17027-5
Description
Summary: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.
ISSN:2041-1723