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

Title: Colony stimulating factor-1 receptor as a target for small molecule inhibitors
Creator: Mashkani, Baratali; Griffith, Renate; Ashman, Leonie K.
Relation: Bioorganic & Medicinal Chemistry Vol. 18, Issue 5, p. 1789-1797
Publisher Link: http://dx.doi.org/10.1016/j.bmc.2010.01.056
Publisher: Elsevier
Resource Type: journal article
Date: 2010
Description: 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.
Subject: binding mode; kinase inhibition; flexible docking; kinase domain conformation; drug design
Identifier: http://hdl.handle.net/1959.13/928644
Identifier: uon:10405
Identifier: ISSN:0968-0896
Language: eng
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