Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 64, Issue 13, Pages 8971-8991Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.1c00024
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The serine/threonine kinase DYRK1A is associated with cancer progression and severity of symptoms in Down's syndrome. A highly selective and well-tolerated DYRK1A inhibitor has been identified, showing in vivo activity in a tumor model, and providing a useful tool for further research on the effects of DYRK1A inhibition in disease models.
The serine/threonine kinase DYRK1A has been implicated in regulation of a variety of cellular processes associated with cancer progression, including cell cycle control, DNA damage repair, protection from apoptosis, cell differentiation, and metastasis. In addition, elevated-level DYRK1A activity has been associated with increased severity of symptoms in Down's syndrome. A selective inhibitor of DYRK1A could therefore be of therapeutic benefit. We have used fragment and structure-based discovery methods to identify a highly selective, well-tolerated, brain-penetrant DYRK1A inhibitor which showed in vivo activity in a tumor model. The inhibitor provides a useful tool compound for further exploration of the effect of DYRK1A inhibition in models of disease.
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