Journal
PHARMACEUTICALS
Volume 12, Issue 4, Pages -Publisher
MDPI
DOI: 10.3390/ph12040185
Keywords
thiazolo[5; 4-f]quinazolin-9(8H)-one; CMGC kinases; DYRK family kinases; SH-SY5Y-Tau-4R cells; pre-B cells; quiescence
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Funding
- MESR (French Ministere de l'Enseignement Superieur AMP
- de la Recherche)
- LABEX SynOrg [ANR-11-LABX-0029]
- Fonds Unique Interministeriel (FUI) TRIAD project
- Conseil Regional de Bretagne
- Fondation Jerome Lejeune
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Dual-specificity tyrosine phosphorylation-regulated kinases (DYRKs) hyperactivity has been linked to the development of a number of human malignancies. DYRK1A is the most studied family member, and the discovery of novel specific inhibitors is attracting considerable interest. The 8-cyclopropyl-2(pyridin-3-yl)thiazolo[5,4-f]quinazolin-9(8H)-one (also called FC162) was found to be a promising inhibitor of DYRK1A and was characterized in biological experiments, by western transfer and flow cytometry on SH-SY5Y and pre-B cells. Here, the results obtained with FC162 are compared to well-characterized known DYRK1A inhibitors (e.g., Leucettine L41 and EHT1610).
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