Format

Send to:

Choose Destination
See comment in PubMed Commons below
Nat Chem Biol. 2009 Jun;5(6):394-6. doi: 10.1038/nchembio.162. Epub 2009 Apr 26.

A new screening assay for allosteric inhibitors of cSrc.

Author information

  • 1Chemical Genomics Centre of the Max Planck Society, Dortmund, Germany.

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.

PMID:
19396179
[PubMed - indexed for MEDLINE]
PubMed Commons home

PubMed Commons

0 comments
How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for Nature Publishing Group
    Loading ...
    Write to the Help Desk