Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis

  • J Med Chem. 2015 Mar 26;58(6):2834-44. doi: 10.1021/acs.jmedchem.5b00098.
Jason G Kettle  1 ,  Peter Ballard  1 ,  Catherine Bardelle  1 ,  Mark Cockerill  1 ,  Nicola Colclough  1 ,  Susan E Critchlow  1 ,  Judit Debreczeni  1 ,  Gary Fairley  1 ,  Shaun Fillery  1 ,  Mark A Graham  1 ,  Louise Goodwin  1 ,  Sylvie Guichard  1 ,  Kevin Hudson  1 ,  Richard A Ward  1 ,  David Whittaker  1
Affiliations
  • 1. Oncology iMed, AstraZeneca, Alderley Park, Macclesfield, SK10 4TG, United Kingdom.
PMID: 25738750 DOI: 10.1021/acs.jmedchem.5b00098
Abstract

Potent and selective inhibitors of DYRK1B kinase were developed to explore the hypothesis, based on siRNA studies, that DYRK1B may be a resistance mechanism in cells undergoing a stress response.

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