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Kinase-templated abiotic reaction

Georgeon, S.
Hantschel, O.
Published in Chemical science. 2017, vol. 8, no. 7, p. 5119-5125
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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Research group Groupe Winssinger
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SAARBACH, Jacques et al. Kinase-templated abiotic reaction. In: Chemical science, 2017, vol. 8, n° 7, p. 5119-5125. doi: 10.1039/C7SC01416C https://archive-ouverte.unige.ch/unige:95272

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Deposited on : 2017-07-04

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