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- W3037752835 abstract "Abstract Chemical tools to monitor drug-target engagement of endogenously expressed protein kinases are highly desirable for preclinical target validation in drug discovery. Here, we describe a chemical genetics strategy to selectively study target engagement of endogenous kinases. By substituting a serine residue into cysteine at the DFG-1 position in the ATP-binding pocket, we sensitize the non-receptor tyrosine kinase FES towards covalent labeling by a complementary fluorescent chemical probe. This mutation is introduced in the endogenous FES gene of HL-60 cells using CRISPR/Cas9 gene editing. Leveraging the temporal and acute control offered by our strategy, we show that FES activity is dispensable for differentiation of HL-60 cells towards macrophages. Instead, FES plays a key role in neutrophil phagocytosis via SYK kinase activation. This chemical genetics strategy holds promise as a target validation method for kinases." @default.
- W3037752835 created "2020-07-02" @default.
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- W3037752835 date "2020-06-25" @default.
- W3037752835 modified "2023-10-02" @default.
- W3037752835 title "Chemical genetics strategy to profile kinase target engagement reveals role of FES in neutrophil phagocytosis" @default.
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- W3037752835 doi "https://doi.org/10.1038/s41467-020-17027-5" @default.
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- W3037752835 hasPublicationYear "2020" @default.
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