Reference : Thiazole- and selenazole-comprising high-affinity inhibitors possess bright microseco...
Scientific journals : Article
Physical, chemical, mathematical & earth Sciences : Chemistry
http://hdl.handle.net/10993/40429
Thiazole- and selenazole-comprising high-affinity inhibitors possess bright microsecond-scale photoluminescence in complex with protein kinase CK2.
English
Vahter, Jurgen [University of Tartu]
Viht, Kaido [University of Tartu]
Uri, Asko [University of Tartu]
Manoharan, Ganesh Babu mailto [University of Luxembourg > Faculty of Science, Technology and Communication (FSTC) > Life Science Research Unit]
Enkvist, Erki [University of Tartu]
2018
Bioorganic & medicinal chemistry
26
18
5062-5068
Yes
International
0968-0896
1464-3391
England
[en] A previously disclosed protein kinase (PK) CK2-selective inhibitor 4-(2-amino-1,3-thiazol-5-yl)benzoic acid (ATB) and its selenium-containing counterpart (ASB) revealed remarkable room temperature phosphorescence when bound to the ATP pocket of the protein kinase CK2. Conjugation of these fragments with a mimic of CK2 substrate peptide resulted in bisubstrate inhibitors with increased affinity towards the kinase. Attachment of the fluorescent acceptor dye 5-TAMRA to the conjugates led to significant enhancement of intensity of long-lifetime (microsecond-scale) photoluminescence of both sulfur- and selenium-containing compounds. The developed photoluminescent probes make possible selective determination of the concentration of CK2 in cell lysates and characterization of CK2 inhibitors by means of time-gated measurement of photoluminescence.
http://hdl.handle.net/10993/40429
Copyright (c) 2018 Elsevier Ltd. All rights reserved.

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