Article
Identification of a DYRK1A Inhibitor that Induces Degradation of the Target Kinase using Co-chaperone CDC37 fused with Luciferase nanoKAZ.
Scientific reports - 3 Aug 2015
Sonamoto Rie, Kii Isao, Koike Yuka, Sumida Yuto, Kato-Sumida Tomoe, Okuno Yukiko, Hosoya Takamitsu, Hagiwara Masatoshi
Abstract excerpt
The protein kinase family includes attractive targets for drug development. Methods for screening of kinase inhibitors remain largely limited to in vitro catalytic assays. It has been shown that ATP-competitive inhibitors antagonize interaction between the target kinase and kinase-specific co-chaperone CDC37 in living cells. Here we show a cell-based method to screen kinase inhibitors using fusion protein of...
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