Utilizing comprehensive and mini-kinome panels to optimize the selectivity of quinoline inhibitors for cyclin G associated kinase (GAK)

Asquith, C.; Hopkins, C.; Treiber, D. K.; Zuercher, W.

doi:10.1101/471615

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bioRxiv · 10.1101/471615

Utilizing comprehensive and mini-kinome panels to optimize the selectivity of quinoline inhibitors for cyclin G associated kinase (GAK)

Asquith, C.·Hopkins, C.·Treiber, D. K.·Zuercher, W.

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Abstract

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.

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Asquith, C., Hopkins, C., Treiber, D. K., Zuercher, W.. 2018-11-17. Utilizing comprehensive and mini-kinome panels to optimize the selectivity of quinoline inhibitors for cyclin G associated kinase (GAK). https://doi.org/10.1101/471615

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