NDLI: A FRET-based microplate assay for human protein kinase CK2, a target in neoplastic disease

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Proceedings of the 17th annual conference of the Groupement des Pharmacochimistes de l’Arc Atlantique (GP2A) and the 22nd “Journées Franco-Belges de Pharmacochimie”

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A FRET-based microplate assay for human protein kinase CK2, a target in neoplastic disease

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A FRET-based microplate assay for human protein kinase CK2, a target in neoplastic disease

Content Provider	Taylor & Francis Online
Author	Gratz, Andreas Götz, Claudia Jose, Joachim
Abstract	Besides cardiovascular diseases, cancer represents the major cause of death in developed countries. In many different human tumors, increased activity of serine/threonine protein kinase CK2 has been detected, and recent in vivo studies support a direct involvement of CK2 in tumor progression. Therefore, potent compounds to decrease CK2 activity to a non-pathogenic level would be a promising effort toward an antineoplastic therapy. In this study, an alternative to the established radiometric phosphorylation assay for quantification of CK2 activity was developed. For this purpose, the substrate peptide RRRDDDSDDD was coupled at the C-terminus to the fluorophore EDANS (5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid) and at the N-terminus to the quencher DABCYL (4-(4-dimethylaminophenylazo)benzoic acid). This resulted in quenched fluorescence of EDANS due to a FRET-based effect. After proteolytic cleavage of the peptide by elastase, the quenching effect was reduced and, as a consequence, fluorescence was increased. Because elastase is supposed to cleave at the S/D site of the peptide, phosphorylation of serine by CK2 hampered substrate binding of elastase and blocked the increase in fluorescence by proteolytic cleavage. This means that the new assay to quantify human CK2 activity is based on the differential accessibility of the proteolytic cleavage site, which is dependent on kinase phosphorylation. It could be used to measure inhibition of the human target in neoplastic diseases by the compounds TBB (4,5,6,7-tetrabromobenzotriazole) and Emodin.
Starting Page	234
Ending Page	239
Page Count	6
File Format	PDF HTM / HTML
ISSN	14756366 14756374
DOI	10.3109/14756360903170038
Journal	Journal of Enzyme Inhibition and Medicinal Chemistry
Volume Number	25
Issue Number	2
Language	English
Publisher	Taylor & Francis
Publisher Date	2010-03-11
Access Restriction	Open
Subject Keyword	Protein kinase Phosphorylation assay CK2 Casein kinase 2 FRET peptide Cancer Porcine pancreatic elastase Protease cleavage
Content Type	Text
Resource Type	Article
Subject	Drug Discovery Medicine Pharmacology

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