Article
Chemical genetics strategy to profile kinase target engagement reveals role of FES in neutrophil phagocytosis.
Nature communications - 25 Jun 2020
van der Wel Tom, Hilhorst Riet, den Dulk Hans, van den Hooven Tim, Prins Nienke M, Wijnakker Joost A P M, Florea Bogdan I, Lenselink Eelke B, van Westen Gerard J P, Ruijtenbeek Rob, Overkleeft Herman S, Kaptein Allard, Barf Tjeerd, van der Stelt Mario
Abstract excerpt
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...
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