期刊
BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS
卷 1834, 期 7, 页码 1330-1335出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.bbapap.2013.02.039
关键词
Protein kinase; Luminescent probe; Bisubstrate inhibitor; Reporter displacement assay; Time-gated luminescence; Live cell imaging
资金
- Estonian Science Foundation [8230, 8419, 8055]
- Estonian Ministry of Education and Sciences [SF0180121s08]
- Royal Society
- EPSRC
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 PR, 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). (C) 2013 Elsevier B.V. All rights reserved.
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