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

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.

SUBMITTER: Rudolf AF

PROVIDER: S-EPMC4051630 | biostudies-literature | 2014

REPOSITORIES: biostudies-literature

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

Rudolf Amalie Frederikke AF Skovgaard Tine T Knapp Stefan S Jensen Lars Juhl LJ Berthelsen Jens J

PloS one 20140610 6

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. ...[more]

PMID: 24915177

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