Abstract
In order to evaluate the isoform selectivity of novel inhibitors within the c-Jun N-terminal kinase (JNK) family, a fluorescence polarization-based competition binding assay, previously developed for JNK3, was extended to the other isoforms JNK1 and JNK2. The assay is based on the displacement of a versatile fluorescent pyridinylimidazole-based probe and was validated by testing the precursor of the probe as well as standard JNK inhibitors.
Keywords:
Binding assay; Fluorescence polarization; JNK1; JNK2; c-Jun N-terminal kinases.
Copyright © 2017 Elsevier Inc. All rights reserved.
MeSH terms
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Binding, Competitive
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Fluorescence Polarization*
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Fluorescent Dyes / metabolism*
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Humans
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Mitogen-Activated Protein Kinase 10 / antagonists & inhibitors
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Mitogen-Activated Protein Kinase 10 / metabolism*
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Mitogen-Activated Protein Kinase 8 / antagonists & inhibitors
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Mitogen-Activated Protein Kinase 8 / metabolism*
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Mitogen-Activated Protein Kinase 9 / antagonists & inhibitors
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Mitogen-Activated Protein Kinase 9 / metabolism*
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Protein Binding
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Protein Kinase Inhibitors / metabolism*
Substances
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Fluorescent Dyes
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Protein Kinase Inhibitors
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Mitogen-Activated Protein Kinase 10
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Mitogen-Activated Protein Kinase 9
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Mitogen-Activated Protein Kinase 8