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Using Light to Regulate the Activity of RET Kinase: Design, synthesis and evaluation of photoswitchable DFG-out RET kinase inhibitors


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Title: Using Light to Regulate the Activity of RET Kinase: Design, synthesis and evaluation of photoswitchable DFG-out RET kinase inhibitors
Authors: Xu, Yongjin
E-mail: yongjin.xu@chem.gu.se
xyjxiangke@hotmail.com
Issue Date: 26-Aug-2021
University: University of Gothenburg. Faculty of Science
Institution: Department of Chemistry and Molecular Biology ; Institutionen för kemi och molekylärbiologi
Parts of work: Xu, Y., Gao, C., Andréasson, J., Grøtli, M. (2018). Synthesis and Photophysical Characterization of Azoheteroarenes, Org. Lett. 20(16), 4875-4879.
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Xu, Y., Gao, C., Håversen, L., Lundbäck, T., Andréasson, J., Grøtli, M. (2021). Design and Development of a Photoswitchable DFG-Out Kinase Inhibitor. Manuscript.

Xu, Y., Gao, C., Andreasson, M., Håversen, L., Carrasco, M., Fleming, C., Lundbäck, T., Andréasson, J., Grøtli, M. (2021). Design and Development of Photoswitchable DFG-Out RET Kinase Inhibitor with Quinoline and 7-azaindole Based Azoheteroarenes. Manuscript.
Date of Defence: 2021-09-17
Disputation: fredagen den 17 september 2021 kl. 09.00 via ZOOM i sal Arvid Carlsson, Medicinaregatan 3
Degree: Doctor of Philosophy
Publication type: Doctoral thesis
Keywords: RET kinase
kinase inhibitor
DFG-out
photoparmacology
azoheteroarene
Buchwald-Hartwig coupling
quinoline
7-azaindole
Abstract: Protein kinases are essential for signal transduction and regulate most cellular processes, such as metabolism, membrane transport, motility, and cell cycle. Although they play a critical role in cells and have a strong association with diseases, details of their physiologic and pathologic mechanisms remain at least partially unclear, especially the spatiotemporal dynamics of the signalling. Reversible photo-regulation of kinase inhibitors could be an approach to gain spatiotemporal control, the... more
ISBN: 978-91-8009-444-3
978-91-8009-445-0
URI: http://hdl.handle.net/2077/68712
Appears in Collections:Doctoral Theses from University of Gothenburg / Doktorsavhandlingar från Göteborgs universitet
Doctoral Theses / Doktorsavhandlingar Institutionen för kemi och molekylärbiologi

 

 

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