Design of a GAK/EGFR inhibitor set to interrogate the relationship of EGFR and GAK in chordoma

Asquith, C.; Naegeli, K.; East, M. P.; Laitinen, T.; Havener, T. M.; Wells, C. I.; Johnson, G. L.; Drewry, D. H.; Zuercher, W. J.; Morris, D. C.

doi:10.1101/475251

bioRxiv · 10.1101/475251

Design of a GAK/EGFR inhibitor set to interrogate the relationship of EGFR and GAK in chordoma

Asquith, C.·Naegeli, K.·East, M. P.·Laitinen, T.·Havener, T. M.·Wells, C. I.·Johnson, G. L.·Drewry, D. H.·Zuercher, W. J.·Morris, D. C.

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Abstract

We describe the design of a set of inhibitors to investigate the relationship between cyclin G associated kinase (GAK) and epidermal growth factor receptor (EGFR) in chordoma bone cancers. These compounds were characterized both in vitro and using in cell target engagement assays. The most potent chordoma inhibitors were further characterized in a kinome-wide screen demonstrating narrow spectrum profiles.

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Asquith, C., Naegeli, K., East, M. P., Laitinen, T., Havener, T. M., Wells, C. I., Johnson, G. L., Drewry, D. H., Zuercher, W. J., Morris, D. C.. 2018-11-20. Design of a GAK/EGFR inhibitor set to interrogate the relationship of EGFR and GAK in chordoma. https://doi.org/10.1101/475251

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