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Scientific article
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English

Kinase-templated abiotic reaction

Published inChemical science, vol. 8, no. 7, p. 5119-5125
Publication date2017
Abstract

Protein kinases are quintessential regulators of cellular function. Numerous pathologies are intimately linked to the dysregulated activity of a particular protein kinase. Herein we report a technology based on a proximity-induced chemical transformation that enables the detection and imaging of specific kinases. Using two probes that target the nucleotide-binding site and substrate binding site of a target kinase respectively, the reagents appended on the probes are brought within reactive distance thereby enabling the chemical transformation. The reaction used for sensing is a ruthenium-photocatalyzed reduction of a pyridinium immolative linker, which uncages a fluorophore (rhodamine). We demonstrate that this technology can be used to discriminate between closely related kinases with a high signal to noise ratio. We further demonstrate that the technology operates within the complexity of a cellular context with a good correlation between the level of kinase activity and fluorescence output.

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Citation (ISO format)
SAARBACH, Jacques et al. Kinase-templated abiotic reaction. In: Chemical science, 2017, vol. 8, n° 7, p. 5119–5125. doi: 10.1039/C7SC01416C
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ISSN of the journal2041-6520
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Creation06/30/2017 6:52:00 PM
First validation06/30/2017 6:52:00 PM
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