A Comparison of Protein Kinases Inhibitor Screening Methods Using Both Enzymatic Activity and Binding Affinity Determination

Binding assays are increasingly used as a screening method for protein kinase inhibitors; however, as yet only a weak correlation with enzymatic activity-based assays has been demonstrated. We show that the correlation between the two types of assays can be improved using more precise screening cond...

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Autores principales: Rudolf, Amalie Frederikke, Skovgaard, Tine, Knapp, Stefan, Jensen, Lars Juhl, Berthelsen, Jens
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Public Library of Science 2014
Materias:
Research Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4051630/
https://www.ncbi.nlm.nih.gov/pubmed/24915177
http://dx.doi.org/10.1371/journal.pone.0098800
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author Rudolf, Amalie Frederikke
Skovgaard, Tine
Knapp, Stefan
Jensen, Lars Juhl
Berthelsen, Jens
author_facet Rudolf, Amalie Frederikke
Skovgaard, Tine
Knapp, Stefan
Jensen, Lars Juhl
Berthelsen, Jens
author_sort Rudolf, Amalie Frederikke
collection PubMed
description Binding assays are increasingly used as a screening method for protein kinase inhibitors; however, as yet only a weak correlation with enzymatic activity-based assays has been demonstrated. We show that the correlation between the two types of assays can be improved using more precise screening conditions. Furthermore a marked improvement in the correlation was found by using kinase constructs containing the catalytic domain in presence of additional domains or subunits.
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spelling pubmed-40516302014-06-18 A Comparison of Protein Kinases Inhibitor Screening Methods Using Both Enzymatic Activity and Binding Affinity Determination Rudolf, Amalie Frederikke Skovgaard, Tine Knapp, Stefan Jensen, Lars Juhl Berthelsen, Jens PLoS One Research Article Binding assays are increasingly used as a screening method for protein kinase inhibitors; however, as yet only a weak correlation with enzymatic activity-based assays has been demonstrated. We show that the correlation between the two types of assays can be improved using more precise screening conditions. Furthermore a marked improvement in the correlation was found by using kinase constructs containing the catalytic domain in presence of additional domains or subunits. Public Library of Science 2014-06-10 /pmc/articles/PMC4051630/ /pubmed/24915177 http://dx.doi.org/10.1371/journal.pone.0098800 Text en © 2014 Rudolf et al http://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are properly credited.
spellingShingle Research Article
Rudolf, Amalie Frederikke
Skovgaard, Tine
Knapp, Stefan
Jensen, Lars Juhl
Berthelsen, Jens
A Comparison of Protein Kinases Inhibitor Screening Methods Using Both Enzymatic Activity and Binding Affinity Determination
title A Comparison of Protein Kinases Inhibitor Screening Methods Using Both Enzymatic Activity and Binding Affinity Determination
title_full A Comparison of Protein Kinases Inhibitor Screening Methods Using Both Enzymatic Activity and Binding Affinity Determination
title_fullStr A Comparison of Protein Kinases Inhibitor Screening Methods Using Both Enzymatic Activity and Binding Affinity Determination
title_full_unstemmed A Comparison of Protein Kinases Inhibitor Screening Methods Using Both Enzymatic Activity and Binding Affinity Determination
title_short A Comparison of Protein Kinases Inhibitor Screening Methods Using Both Enzymatic Activity and Binding Affinity Determination
title_sort comparison of protein kinases inhibitor screening methods using both enzymatic activity and binding affinity determination
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4051630/
https://www.ncbi.nlm.nih.gov/pubmed/24915177
http://dx.doi.org/10.1371/journal.pone.0098800
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