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

TY - JOUR

T1 - A comparison of protein kinases inhibitor screening methods using both enzymatic activity and binding affinity determination

AU - Rudolf, Amalie Frederikke

AU - Skovgaard, Tine

AU - Knapp, Stefan

AU - Jensen, Lars Juhl

AU - Berthelsen, Jens

PY - 2014/6/10

Y1 - 2014/6/10

N2 - 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.

AB - 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.

U2 - 10.1371/journal.pone.0098800

DO - 10.1371/journal.pone.0098800

M3 - Journal article

C2 - 24915177

SN - 1932-6203

VL - 9

SP - 1

EP - 5

JO - PLoS Computational Biology

JF - PLoS Computational Biology

IS - 6

M1 - e98800

ER -