Design and development of a photoswitchable DFG-out kinase inhibitor

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...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:Chemical communications (Cambridge, England) England), 2021, Vol.57 (78), p.143-146
Hauptverfasser: Xu, Yongjin, Gao, Chunxia, Håversen, Liliana, Lundbäck, Thomas, Andréasson, Joakim, Grøtli, Morten
Format: Artikel
Sprache:eng
Schlagworte:
binding
Chemical Sciences
Chemistry
Kemi
Kinases
p38 map kinase
ponatinib
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung: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.
ISSN:1359-7345
1364-548X
1364-548X
DOI:10.1039/d1cc04125h