Small-molecule inhibitors of the c-Fes protein-tyrosine kinase.

Journal article

The c-Fes protein-tyrosine kinase modulates cellular signaling pathways governing differentiation, the innate immune response, and vasculogenesis. Here, we report the identification of types I and II kinase inhibitors with potent activity against c-Fes both in vitro and in cell-based assays. One of the most potent inhibitors is the previously described anaplastic lymphoma kinase inhibitor TAE684. The crystal structure of TAE684 in complex with the c-Fes SH2-kinase domain showed excellent shap...

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Authors: Hellwig, S; Miduturu, C; Kanda, S; Zhang, J; Filippakopoulos, P

• Publication status: Published
• Journal: Chemistry and biology
• Volume: 19
• Issue: 4
• Pages: 529-540
• Publication date: 2012-04-01
• DOI: 10.1016/j.chembiol.2012.01.020
• EISSN: 1879-1301
• ISSN: 1074-5521
• Language: English
• Keywords: Binding Sites; COS Cells; Animals; Cell Differentiation; src Homology Domains; Cell Line; Protein-Tyrosine Kinases; Cercopithecus aethiops; Proto-Oncogene Proteins c-fes; Mice; Microtubules; Pyrimidines; Computer Simulation; Phosphorylation; Crystallography, X-Ray; Signal Transduction; Small Molecule Libraries