Utilizing comprehensive and mini-kinome panels to optimize the selectivity of quinoline inhibitors for cyclin G associated kinase (GAK)
Autor: | Daniel K. Treiber, Christopher R. M. Asquith, Caleb Hopkins, William J. Zuercher |
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Rok vydání: | 2018 |
Předmět: | |
DOI: | 10.1101/471615 |
Popis: | We demonstrate an innovative approach utilising both fit-for-purpose kinase mini-panels and kinome-wide panels to progress discovery programs in the optimization of inhibitor potency and selectivity. We present a focused case study on development of a selective inhibitor of cyclin G associated kinase (GAK) using the quin(az)oline inhibitor chemotype. These results exemplify a versatile, efficient approach to drive kinome selectivity during inhibitor development programs. |
Databáze: | OpenAIRE |
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