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See detailThiazole- and selenazole-comprising high-affinity inhibitors possess bright microsecond-scale photoluminescence in complex with protein kinase CK2.
Vahter, Jurgen; Viht, Kaido; Uri, Asko et al

in Bioorganic & medicinal chemistry (2018), 26(18), 5062-5068

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 ... [more ▼]

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. [less ▲]

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See detailBifunctional Ligands for Inhibition of Tight-Binding Protein–Protein Interactions
Ivan, Taavi; Enkvist, Erki; Viira, Birgit et al

in Bioconjugate Chemistry (2016), 27(8), 1900-1910

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See detailCombining chemical and genetic approaches for development of responsive FRET-based sensor systems for protein kinases
Manoharan, Ganesh Babu UL; Enkvist, Erki; Uri, Asko

in Biophysical Chemistry (2016), 211

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See detailFRET-based screening assay using small-molecule photoluminescent probes in lysate of cells overexpressing RFP-fused protein kinases
Manoharan, Ganesh Babu UL; Enkvist, Erki; Kasari, Marje et al

in Analytical Biochemistry (2015)

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See detailPIM kinase-responsive microsecond-lifetime photoluminescent probes based on selenium-containing heteroaromatic tricycle
Ekambaram, Ramesh; Manoharan, Ganesh Babu UL; Enkvist, Erki et al

in RSC Advances (2015)

Detailed reference viewed: 42 (1 UL)
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See detailBenzoselenadiazole-based responsive long-lifetime photoluminescent probes for protein kinases
Ekambaram, Ramesh; Enkvist, Erki; Manoharan, Ganesh Babu UL et al

in Chemical Communications (2014)

Detailed reference viewed: 37 (0 UL)