Journal
ACS CHEMICAL BIOLOGY
Volume 11, Issue 5, Pages 1296-1304Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acschembio.5b01018
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Funding
- University of Michigan College of Pharmacy
- Kathy Bruk Pearce Research Fund of the University of Michigan Comprehensive Cancer Center
- National Institutes of Health Chemistry Biology Interface Training Grant [GM008597]
- National Institutes of Health Cellular Biotechnology Training Grant [GM008353]
- U.S. DOE [DE-AC02-06CH11357]
- Michigan Economic Development Corporation
- Michigan Technology Tri-Corridor Grant [085P1000817]
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In the kinase field, there are many widely held tenets about conformation-selective inhibitors that have yet to be validated using controlled experiments. We have designed, synthesized, and characterized a series of kinase inhibitor analogues of dasatinib, an FDA-approved kinase inhibitor that binds the active conformation. This inhibitor series includes two Type II inhibitors that bind the DFG-out inactive conformation and two inhibitors that bind the alpha C-helix-out inactive conformation. Using this series of compounds, we analyze the impact that conformation-selective inhibitors have on target binding and kinome-wide selectivity.
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