A new screening assay for allosteric inhibitors of cSrc.

ID: ALA1212717

Journal: Nat Chem Biol

Title: A new screening assay for allosteric inhibitors of cSrc.

Authors: Simard JR, Klüter S, Grütter C, Getlik M, Rabiller M, Rode HB, Rauh D.

Abstract: Targeting kinases outside the highly conserved ATP pocket is thought to be a promising strategy for overcoming bottlenecks in kinase inhibitor research, such as limited selectivity and drug resistance. Here we report the development and application of a direct binding assay to detect small molecules that stabilize the inactive conformation of the tyrosine kinase cSrc. Protein X-ray crystallography validated the assay results and confirmed an exclusively allosteric binding mode.

CiteXplore: 19396179

DOI: 10.1038/nchembio.162

Patent ID: ┄