Ontology highlight
ABSTRACT:
SUBMITTER: van der Wel T
PROVIDER: S-EPMC7316778 | biostudies-literature | 2020 Jun
REPOSITORIES: biostudies-literature
Nature communications 20200625 1
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 mu ...[more]