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- Title
Photoactivatable Small‐Molecule Inhibitors for Light‐Controlled TAM Kinase Activity.
- Authors
Le Bescont, Julie; Mouawad, Liliane; Boddaert, Thomas; Bombard, Sophie; Piguel, Sandrine
- Abstract
The TAM kinase family arises as a promising therapeutic target for cancer therapy, as well as auto‐immune and viral diseases. In this study, we report the first photoactivatable caged inhibitors of Tyro3 and Mer. This strategy enables spatial and temporal control of the biological activity of the inhibitor upon irradiation with UV light. We describe the design, synthesis, photocleavage properties, and inhibitory activities of four Tyro3 and Mer photoactivatable small molecules. The proof of concept on the TAM kinase family was achieved in vitro, since irradiation by UV light restored the full inhibitory activity of two prodrugs.
- Subjects
SMALL molecules; VIRUS diseases; PROTEIN kinases; PROOF of concept; CANCER treatment
- Publication
ChemPhotoChem, 2021, Vol 5, Issue 11, p989
- ISSN
2367-0932
- Publication type
Article
- DOI
10.1002/cptc.202100131