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Bioorg Med Chem. 2010 Mar 1;18(5):1789-97. doi: 10.1016/j.bmc.2010.01.056. Epub 2010 Jan 28.

Colony stimulating factor-1 receptor as a target for small molecule inhibitors.

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School of Biomedical Sciences, University of Newcastle, Callaghan, NSW 2308, Australia.


Imatinib, dasatinib, sunitinib, CEP-701, and PKC-412, ATP-competitive small molecule inhibitors of type III receptor tyrosine kinases c-KIT and/or FLT3, were evaluated for binding to the closely related receptor, FMS, by docking into models of inactive and active conformations of the FMS kinase domain. To confirm the docking predictions, the drugs were tested for their activity and selectivity in inhibiting cell proliferation and FMS phosphorylation upon stimulation by the FMS ligand, CSF-1. All five drugs inhibited FMS activity. Imatinib, dasatinib and CEP-701 represent three different types of interactions determining drug potency and selectivity.

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