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ORBilu is a project developed by
   Thiazole- and selenazole-comprising high-affinity inhibitors possess bright microsecond-scale photoluminescence in complex with protein kinase CK2.; ; 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 ▲] Detailed reference viewed: 326 (2 UL)Bifunctional Ligands for Inhibition of Tight-Binding Protein–Protein Interactions; ; et al in Bioconjugate Chemistry (2016), 27(8), 1900-1910 Detailed reference viewed: 165 (1 UL)Combining chemical and genetic approaches for development of responsive FRET-based sensor systems for protein kinasesManoharan, Ganesh Babu  ; ; in Biophysical Chemistry (2016), 211 Detailed reference viewed: 198 (3 UL)FRET-based screening assay using small-molecule photoluminescent probes in lysate of cells overexpressing RFP-fused protein kinasesManoharan, Ganesh Babu ; ; et alin Analytical Biochemistry (2015) Detailed reference viewed: 179 (3 UL)PIM kinase-responsive microsecond-lifetime photoluminescent probes based on selenium-containing heteroaromatic tricycle; Manoharan, Ganesh Babu ; et alin RSC Advances (2015) Detailed reference viewed: 151 (1 UL)Benzoselenadiazole-based responsive long-lifetime photoluminescent probes for protein kinases; ; Manoharan, Ganesh Babu et alin Chemical Communications (2014) Detailed reference viewed: 174 (0 UL) |
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