2. Academic Validation
  3. Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis

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

Affiliation

  • 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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