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A Caged Ret Kinase Inhibitor and its Effect on Motoneuron Development in Zebrafish Embryos

David Bliman ; Jesper Nilsson (Institutionen för kemi och kemiteknik, Fysikalisk kemi) ; Petronella Kettunen ; Joakim Andréasson (Institutionen för kemi och kemiteknik, Fysikalisk kemi) ; Morten Grøtli
Scientific Reports (2045-2322). Vol. 5 (2015), p. artikel nr 13109.
[Artikel, refereegranskad vetenskaplig]

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.



Denna post skapades 2015-08-26. Senast ändrad 2016-10-24.
CPL Pubid: 221282

 

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Institutioner (Chalmers)

Institutionen för kemi och molekylärbiologi (GU)
Institutionen för kemi och kemiteknik, Fysikalisk kemi
Institutionen för neurovetenskap och fysiologi, sektionen för psykiatri och neurokemi (GU)

Ämnesområden

Kemi
Biologiska vetenskaper

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