Biological Characterization of 8-Cyclopropyl-2-(pyridin-3-yl)thiazolo[5,4- f]quinazolin-9(8 H)-one, a Promising Inhibitor of DYRK1A

8-环丙基-2-(吡啶-3-基)噻唑并[5,4- f]喹唑啉-9(8 H)-酮(一种有前途的 DYRK1A 抑制剂)的生物学特性

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作者:Corinne Fruit, Florence Couly, Rahul Bhansali, Malini Rammohan, Mattias F Lindberg, John D Crispino, Laurent Meijer, Thierry Besson

Abstract

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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