DOI: 10.1101/471615Nov 17, 2018Paper

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

BioRxiv : the Preprint Server for Biology
Christopher R.M. AsquithWilliam J Zuercher

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 develop-ment 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.

Related Concepts

Case-Control Studies
Guanosine
Phosphotransferases
Inhibitors
GAK
C1orf56

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