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SGC-CK2-1 Is an Efficient Inducer of Insulin Production and Secretion in Pancreatic β-Cells

The pyrazolopyrimidine based compound SGC-CK2-1 is a potent and highly specific CK2 inhibitor and a new tool to study the biological functions of protein kinase CK2 irrespective from off-target effects. We used this compound in comparison with the well-established CK2 inhibitor CX-4945 to analyze th...

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Detalles Bibliográficos
Autores principales: Pack, Mandy, Götz, Claudia, Wrublewsky, Selina, Montenarh, Mathias
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8778508/
https://www.ncbi.nlm.nih.gov/pubmed/35056914
http://dx.doi.org/10.3390/pharmaceutics14010019
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author Pack, Mandy
Götz, Claudia
Wrublewsky, Selina
Montenarh, Mathias
author_facet Pack, Mandy
Götz, Claudia
Wrublewsky, Selina
Montenarh, Mathias
author_sort Pack, Mandy
collection PubMed
description The pyrazolopyrimidine based compound SGC-CK2-1 is a potent and highly specific CK2 inhibitor and a new tool to study the biological functions of protein kinase CK2 irrespective from off-target effects. We used this compound in comparison with the well-established CK2 inhibitor CX-4945 to analyze the importance of CK2 for insulin production and secretion from pancreatic β-cells. Both inhibitors affected the proliferation and viability of MIN6 cells only marginally and downregulated the endogenous CK2 activity to a similar level. Furthermore, both inhibitors increased the message for insulin and boosted the secretion of insulin from storage vesicles. Thus, regarding the high specificity of SGC-CK2-1, we can clearly attribute the observed effects to biological functions of protein kinase CK2.
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spelling pubmed-87785082022-01-22 SGC-CK2-1 Is an Efficient Inducer of Insulin Production and Secretion in Pancreatic β-Cells Pack, Mandy Götz, Claudia Wrublewsky, Selina Montenarh, Mathias Pharmaceutics Article The pyrazolopyrimidine based compound SGC-CK2-1 is a potent and highly specific CK2 inhibitor and a new tool to study the biological functions of protein kinase CK2 irrespective from off-target effects. We used this compound in comparison with the well-established CK2 inhibitor CX-4945 to analyze the importance of CK2 for insulin production and secretion from pancreatic β-cells. Both inhibitors affected the proliferation and viability of MIN6 cells only marginally and downregulated the endogenous CK2 activity to a similar level. Furthermore, both inhibitors increased the message for insulin and boosted the secretion of insulin from storage vesicles. Thus, regarding the high specificity of SGC-CK2-1, we can clearly attribute the observed effects to biological functions of protein kinase CK2. MDPI 2021-12-22 /pmc/articles/PMC8778508/ /pubmed/35056914 http://dx.doi.org/10.3390/pharmaceutics14010019 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/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 (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Pack, Mandy
Götz, Claudia
Wrublewsky, Selina
Montenarh, Mathias
SGC-CK2-1 Is an Efficient Inducer of Insulin Production and Secretion in Pancreatic β-Cells
title SGC-CK2-1 Is an Efficient Inducer of Insulin Production and Secretion in Pancreatic β-Cells
title_full SGC-CK2-1 Is an Efficient Inducer of Insulin Production and Secretion in Pancreatic β-Cells
title_fullStr SGC-CK2-1 Is an Efficient Inducer of Insulin Production and Secretion in Pancreatic β-Cells
title_full_unstemmed SGC-CK2-1 Is an Efficient Inducer of Insulin Production and Secretion in Pancreatic β-Cells
title_short SGC-CK2-1 Is an Efficient Inducer of Insulin Production and Secretion in Pancreatic β-Cells
title_sort sgc-ck2-1 is an efficient inducer of insulin production and secretion in pancreatic β-cells
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8778508/
https://www.ncbi.nlm.nih.gov/pubmed/35056914
http://dx.doi.org/10.3390/pharmaceutics14010019
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