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

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(py...

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Autores principales: Fruit, Corinne, Couly, Florence, Bhansali, Rahul, Rammohan, Malini, Lindberg, Mattias F., Crispino, John D., Meijer, Laurent, Besson, Thierry
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Communication
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6958357/
https://www.ncbi.nlm.nih.gov/pubmed/31861110
http://dx.doi.org/10.3390/ph12040185
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author Fruit, Corinne
Couly, Florence
Bhansali, Rahul
Rammohan, Malini
Lindberg, Mattias F.
Crispino, John D.
Meijer, Laurent
Besson, Thierry
author_facet Fruit, Corinne
Couly, Florence
Bhansali, Rahul
Rammohan, Malini
Lindberg, Mattias F.
Crispino, John D.
Meijer, Laurent
Besson, Thierry
author_sort Fruit, Corinne
collection PubMed
description 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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spelling pubmed-69583572020-01-23 Biological Characterization of 8-Cyclopropyl-2-(pyridin-3-yl)thiazolo[5,4-f]quinazolin-9(8H)-one, a Promising Inhibitor of DYRK1A Fruit, Corinne Couly, Florence Bhansali, Rahul Rammohan, Malini Lindberg, Mattias F. Crispino, John D. Meijer, Laurent Besson, Thierry Pharmaceuticals (Basel) Communication 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). MDPI 2019-12-17 /pmc/articles/PMC6958357/ /pubmed/31861110 http://dx.doi.org/10.3390/ph12040185 Text en © 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Communication
Fruit, Corinne
Couly, Florence
Bhansali, Rahul
Rammohan, Malini
Lindberg, Mattias F.
Crispino, John D.
Meijer, Laurent
Besson, Thierry
Biological Characterization of 8-Cyclopropyl-2-(pyridin-3-yl)thiazolo[5,4-f]quinazolin-9(8H)-one, a Promising Inhibitor of DYRK1A
title Biological Characterization of 8-Cyclopropyl-2-(pyridin-3-yl)thiazolo[5,4-f]quinazolin-9(8H)-one, a Promising Inhibitor of DYRK1A
title_full Biological Characterization of 8-Cyclopropyl-2-(pyridin-3-yl)thiazolo[5,4-f]quinazolin-9(8H)-one, a Promising Inhibitor of DYRK1A
title_fullStr Biological Characterization of 8-Cyclopropyl-2-(pyridin-3-yl)thiazolo[5,4-f]quinazolin-9(8H)-one, a Promising Inhibitor of DYRK1A
title_full_unstemmed Biological Characterization of 8-Cyclopropyl-2-(pyridin-3-yl)thiazolo[5,4-f]quinazolin-9(8H)-one, a Promising Inhibitor of DYRK1A
title_short Biological Characterization of 8-Cyclopropyl-2-(pyridin-3-yl)thiazolo[5,4-f]quinazolin-9(8H)-one, a Promising Inhibitor of DYRK1A
title_sort biological characterization of 8-cyclopropyl-2-(pyridin-3-yl)thiazolo[5,4-f]quinazolin-9(8h)-one, a promising inhibitor of dyrk1a
topic Communication
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6958357/
https://www.ncbi.nlm.nih.gov/pubmed/31861110
http://dx.doi.org/10.3390/ph12040185
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