Design and development of a photoswitchable DFG-out kinase inhibitor

We report the synthesis and characterisation of a photoswitchable DFG-out kinase inhibitor. Photocontrol of the target kinase in both enzymatic and living cell assays is demonstrated. A photoswitchable DFG-out kinase inhibitor has been developed. The activity of the inhibitor can efficiently be regu...

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Published inChemical communications (Cambridge, England) Vol. 57; no. 78; pp. 143 - 146
Main Authors Xu, Yongjin, Gao, Chunxia, Håversen, Liliana, Lundbäck, Thomas, Andréasson, Joakim, Grøtli, Morten
Format Journal Article
LanguageEnglish
Published CAMBRIDGE Royal Soc Chemistry 2021
Royal Society of Chemistry
Subjects
binding
Chemical Sciences
Chemistry
Chemistry, Multidisciplinary
Kemi
Kinases
p38 map kinase
Physical Sciences
ponatinib
Science & Technology
BINDING
PONATINIB
P38 MAP KINASE
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Summary:We report the synthesis and characterisation of a photoswitchable DFG-out kinase inhibitor. Photocontrol of the target kinase in both enzymatic and living cell assays is demonstrated. A photoswitchable DFG-out kinase inhibitor has been developed. The activity of the inhibitor can efficiently be regulated by light in both enzymatic and living cell assays.
Bibliography:10.1039/d1cc04125h
Electronic supplementary information (ESI) available: Detailed synthetic procedure and characterization of compounds, NMR spectra, HRMS spectra, photophysical characterization, biological characterization and protocol for docking. See DOI
Swedish Research Council
ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:1359-7345
1364-548X
1364-548X
DOI:10.1039/d1cc04125h