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All-photonic kinase...
All-photonic kinase inhibitors: light-controlled release-and-report inhibition
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- Fleming, Cassandra, 1987 (författare)
- Göteborgs universitet,University of Gothenburg
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- Benitez-Martin, Carlos, 1994 (författare)
- Chalmers tekniska högskola,Chalmers University of Technology
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- Bernson, Elin (författare)
- Göteborgs universitet,University of Gothenburg
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- Xu, Yongjin (författare)
- Göteborgs universitet,University of Gothenburg
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- Kristenson, Linnea (författare)
- Göteborgs universitet,University of Gothenburg
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- Inghardt, Tord (författare)
- AstraZeneca AB
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- Lundback, Thomas (författare)
- AstraZeneca AB
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- Thoren, Fredrik B. (författare)
- Göteborgs universitet,University of Gothenburg
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- Grötli, Morten, 1966 (författare)
- Göteborgs universitet,University of Gothenburg
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- Andreasson, Joakim, 1973 (författare)
- Chalmers tekniska högskola,Chalmers University of Technology
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(creator_code:org_t)
- 2024
- 2024
- Engelska.
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Ingår i: Chemical Science. - 2041-6539 .- 2041-6520. ; 15:18, s. 6897-6905
- Relaterad länk:
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https://research.cha... (primary) (free)
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https://research.cha...
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https://doi.org/10.1...
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Abstract
Ämnesord
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- Light-responsive molecular tools targeting kinases affords one the opportunity to study the underlying cellular function of selected kinases. In efforts to externally control lymphocyte-specific protein tyrosine kinase (LCK) activity, the development of release-and-report LCK inhibitors is described, in which (i) the release of the active kinase inhibitor can be controlled externally with light; and (ii) fluorescence is employed to report both the release and binding of the active kinase inhibitor. This introduces an unprecedented all-photonic method for users to both control and monitor real-time inhibitory activity. A functional cellular assay demonstrated light-mediated LCK inhibition in natural killer cells. The use of coumarin-derived caging groups resulted in rapid cellular uptake and non-specific intracellular localisation, while a BODIPY-derived caging group predominately localised in the cellular membrane. This concept of release-and-report inhibitors has the potential to be extended to other biorelevant targets where both spatiotemporal control in a cellular setting and a reporting mechanism would be beneficial.
Ämnesord
- NATURVETENSKAP -- Biologi -- Biokemi och molekylärbiologi (hsv//swe)
- NATURAL SCIENCES -- Biological Sciences -- Biochemistry and Molecular Biology (hsv//eng)
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Fleming, Cassand ...
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Benitez-Martin, ...
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Bernson, Elin
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Xu, Yongjin
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Kristenson, Linn ...
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Inghardt, Tord
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Lundback, Thomas
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Thoren, Fredrik ...
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Grötli, Morten, ...
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Andreasson, Joak ...
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