Responsive microsecond-lifetime photoluminescent probes for analysis of protein kinases and their inhibitors.

Kasari, Marje; Ligi, Kadri; Gareth Williams, J.A.; Vaasa, Angela; Enkvist, Erki; Viht, Kaido; Pålsson, Lars-Olof; Uri, Asko

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).

Citation

Kasari, M., Ligi, K., Gareth Williams, J., Vaasa, A., Enkvist, E., Viht, K., …Uri, A. (2013). Responsive microsecond-lifetime photoluminescent probes for analysis of protein kinases and their inhibitors. BBA - Proteins and Proteomics, 1834(7), 1330-1335. https://doi.org/10.1016/j.bbapap.2013.02.039

• Journal Article Type: Article
• Acceptance Date: Feb 27, 2013
• Online Publication Date: Mar 14, 2013
• Publication Date: 2013-07
• Deposit Date: Nov 14, 2014
• Journal: BBA - Proteins and Proteomics
• Print ISSN: 1570-9639
• Publisher: Elsevier
• Peer Reviewed: Peer Reviewed
• Volume: 1834
• Issue: 7
• Pages: 1330-1335
• DOI: https://doi.org/10.1016/j.bbapap.2013.02.039