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PLoS One. 2014 Jun 10;9(6):e98800. doi: 10.1371/journal.pone.0098800. eCollection 2014.

A comparison of protein kinases inhibitor screening methods using both enzymatic activity and binding affinity determination.

Author information

1
Novo Nordisk Foundation Center for Protein Research, Faculty of Health Sciences, University of Copenhagen, Copenhagen, Denmark.
2
Structural Genomics Consortium, Nuffield Department of Clinical Medicine, University of Oxford, Oxford, United Kingdom.
3
Novo Nordisk Foundation Center for Protein Research, Faculty of Health Sciences, University of Copenhagen, Copenhagen, Denmark; Costerton Biofilm Center, Institute for International Health, Immunology and Microbiology, Faculty of Health Sciences, University of Copenhagen, Copenhagen, Denmark.

Abstract

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.

PMID:
24915177
PMCID:
PMC4051630
DOI:
10.1371/journal.pone.0098800
[Indexed for MEDLINE]
Free PMC Article

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