Publication Abstract from PubMed
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.
A new screening assay for allosteric inhibitors of cSrc.,Simard JR, Kluter S, Grutter C, Getlik M, Rabiller M, Rode HB, Rauh D Nat Chem Biol. 2009 Jun;5(6):394-6. Epub 2009 Apr 26. PMID:19396179[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
