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A Caged Ret Kinase ...
A Caged Ret Kinase Inhibitor and its Effect on Motoneuron Development in Zebrafish Embryos
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- Bliman, David (författare)
- Gothenburg University,Göteborgs universitet,Institutionen för kemi och molekylärbiologi,Department of Chemistry and Molecular Biology,University of Gothenburg
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- Nilsson, Jesper, 1984 (författare)
- Chalmers tekniska högskola,Chalmers University of Technology
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- Kettunen, Petronella (författare)
- Gothenburg University,Göteborgs universitet,Institutionen för neurovetenskap och fysiologi, sektionen för psykiatri och neurokemi,Institute of Neuroscience and Physiology, Department of Psychiatry and Neurochemistry,University of Gothenburg
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- Andreasson, Joakim, 1973 (författare)
- Chalmers tekniska högskola,Chalmers University of Technology
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- Grøtli, Morten, 1966 (författare)
- Gothenburg University,Göteborgs universitet,Institutionen för kemi och molekylärbiologi,Department of Chemistry and Molecular Biology,University of Gothenburg
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(creator_code:org_t)
- 2015-08-24
- 2015
- Engelska.
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Ingår i: Scientific Reports. - : Springer Science and Business Media LLC. - 2045-2322. ; 5
- Relaterad länk:
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https://gup.ub.gu.se... (primary) (free)
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https://www.nature.c...
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http://publications.... (primary) (free)
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https://gup.ub.gu.se...
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https://doi.org/10.1...
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https://research.cha...
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Abstract
Ämnesord
Stäng
- Proto-oncogene tyrosine-protein kinase receptor RET is implicated in the development and maintenance of neurons of the central and peripheral nervous systems. Attaching activity-compromising photocleavable groups (caging) to inhibitors could allow for external spatiotemporally controlled inhibition using light, potentially providing novel information on how these kinase receptors are involved in cellular processes. Here, caged RET inhibitors were obtained from 3-substituted pyrazolopyrimidine-based compounds by attaching photolabile groups to the exocyclic amino function. The most promising compound displayed excellent inhibitory effect in cell-free, as well as live-cell assays upon decaging. Furthermore, inhibition could be efficiently activated with light in vivo in zebrafish embryos and was shown to effect motoneuron development.
Ämnesord
- NATURVETENSKAP -- Biologi (hsv//swe)
- NATURAL SCIENCES -- Biological Sciences (hsv//eng)
- NATURVETENSKAP -- Kemi (hsv//swe)
- NATURAL SCIENCES -- Chemical Sciences (hsv//eng)
Publikations- och innehållstyp
- ref (ämneskategori)
- art (ämneskategori)
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