A Caged Ret Kinase Inhibitor and its Effect on Motoneuron Development in Zebrafish Embryos
Journal article, 2015

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.

Author

[Person 30630b9c-89a8-4ffd-99ae-c39cf1431cab not found]

University of Gothenburg

[Person e5b8fb97-a15f-4efd-9fad-7559d18e0ac6 not found]

Chalmers, Chemistry and Chemical Engineering, Chemistry and Biochemistry, Physical Chemistry

[Person 02184a58-e815-4e2e-907e-9a8c9aa9963e not found]

University of Gothenburg

[Person 16db8c28-4036-4e11-834f-44d71a16abe1 not found]

Chalmers, Chemistry and Chemical Engineering, Chemistry and Biochemistry, Physical Chemistry

[Person 1ce813ce-fd8b-4550-9456-285b715f3e5f not found]

University of Gothenburg

Scientific Reports

2045-2322 (ISSN)

Vol. 5 artikel nr 13109- 13109

Photonic switching of molecular properties using photochromes

Swedish Research Council (VR), 2011-01-01 -- 2016-12-31.

Photochromic Systems for Solid State Molecular Electronic Devices and Light-Activated Cancer Drugs (PHOTOCHROMES)

European Commission (EC), 2008-09-01 -- 2013-08-31.

Subject Categories

Biological Sciences

Chemical Sciences

DOI

10.1038/srep13109

PubMed

26300345

More information

Latest update

4/18/2018