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- W2071217673 abstract "Selective protein kinase inhibitors have only been developed against a small number of kinase targets. Here we demonstrate that “high-throughput kinase profiling” is an efficient method for the discovery of lead compounds for established as well as unexplored kinase targets. We screened a library of 118 compounds constituting two distinct scaffolds (furan-thiazolidinediones and pyrimido-diazepines) against a panel of 353 kinases. A distinct kinase selectivity profile was observed for each scaffold. Selective inhibitors were identified with submicromolar cellular activity against PIM1, ERK5, ACK1, MPS1, PLK1-3, and Aurora A,B kinases. In addition, we identified potent inhibitors for so far unexplored kinases such as DRAK1, HIPK2, and DCAMKL1 that await further evaluation. This inhibitor-centric approach permits comprehensive assessment of a scaffold of interest and represents an efficient and general strategy for identifying new selective kinase inhibitors." @default.
- W2071217673 created "2016-06-24" @default.
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- W2071217673 date "2011-07-01" @default.
- W2071217673 modified "2023-09-25" @default.
- W2071217673 title "High-Throughput Kinase Profiling: A More Efficient Approach toward the Discovery of New Kinase Inhibitors" @default.
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- W2071217673 doi "https://doi.org/10.1016/j.chembiol.2011.05.010" @default.
- W2071217673 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3171802" @default.
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