title: Responsive microsecond-lifetime photoluminescent probes for analysis of protein kinases and their inhibitors.
abstract: Responsive ARC-Lum probes were used for measurement of the concentration of active protein kinases (PKs) and determination of affinity of inhibitors of PKs. ARC-Lum probes incorporate thiophene or a selenophene heterocycle and a fluorophore conjugated to the lysine residue in the peptide fragment. In the complex with a PK, ARC-Lum probes emit long-lifetime (microsecond-scale) luminescence at the emission wavelengths of the fluorescent label if the complex is illuminated at the excitation wavelength of the thiophene- or selenophene-containing phosphorescence donors. Bisubstrate ARC-Lum probes bind with sub-nanomolar affinity with several PKs of the AGC group. This article is part of a Special Issue entitled: Inhibitors of Protein Kinases (2012).
authors.affiliation: Institute of Chemistry, University of Tartu, 14A Ravila St., 50411 Tartu, Estonia.
authors.forename: Marje
authors.initials: M
authors.lastname: Kasari
authors.forename: Kadri
authors.initials: K
authors.lastname: Ligi
authors.forename: J A Gareth
authors.initials: JA
authors.lastname: Williams
authors.forename: Angela
authors.initials: A
authors.lastname: Vaasa
authors.forename: Erki
authors.initials: E
authors.lastname: Enkvist
authors.forename: Kaido
authors.initials: K
authors.lastname: Viht
authors.forename: Lars-Olof
authors.initials: LO
authors.lastname: Pålsson
authors.forename: Asko
authors.initials: A
authors.lastname: Uri
mesh_terms: D000465:Algorithms; D016880:Anisotropy; D001665:Binding Sites; D001667:Binding, Competitive; D055162:Biocatalysis / Q000187:drug effects; D005456:Fluorescent Dyes / Q000737:chemistry / Q000378:metabolism*; D007700:Kinetics; D008239:Lysine / Q000737:chemistry / Q000378:metabolism*; D008956:Models, Chemical; D015394:Molecular Structure; D011485:Protein Binding; D011493:Protein Kinase C / Q000037:antagonists & inhibitors / Q000737:chemistry / Q000378:metabolism; D047428:Protein Kinase Inhibitors / Q000378:metabolism* / Q000494:pharmacology; D011494:Protein Kinases / Q000737:chemistry / Q000378:metabolism*; D013053:Spectrophotometry; D019311:Staurosporine / Q000378:metabolism / Q000494:pharmacology; D013876:Thiophenes / Q000737:chemistry / Q000378:metabolism; D013997:Time Factors
chemical_list: D005456:Fluorescent Dyes; D047428:Protein Kinase Inhibitors; D013876:Thiophenes; D011494:Protein Kinases; D011493:Protein Kinase C; D019311:Staurosporine; D008239:Lysine