"Photo-Adrenalines": Photoswitchable β 2 -Adrenergic Receptor Agonists as Molecular Probes for the Study of Spatiotemporal Adrenergic Signaling

β -adrenergic receptor (β -AR) agonists are used for the treatment of asthma and chronic obstructive pulmonary disease, but also play a role in other complex disorders including cancer, diabetes and heart diseases. As the cellular and molecular mechanisms in various cells and tissues of the β -AR re...

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Veröffentlicht in:Chemistry : a European journal 2024-01, p.e202303506
Hauptverfasser: Sink, Alexandra, Gerwe, Hubert, Hübner, Harald, Boivin-Jahns, Valerie, Fender, Julia, Lorenz, Kristina, Gmeiner, Peter, Decker, Michael
Format: Artikel
Sprache:eng
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Zusammenfassung:β -adrenergic receptor (β -AR) agonists are used for the treatment of asthma and chronic obstructive pulmonary disease, but also play a role in other complex disorders including cancer, diabetes and heart diseases. As the cellular and molecular mechanisms in various cells and tissues of the β -AR remain vastly elusive, we developed tools for this investigation with high temporal and spatial resolution. Several photoswitchable β -AR agonists with nanomolar activity were synthesized. The most potent agonist for β -AR with reasonable switching is a one-digit nanomolar active, trans-on arylazopyrazole-based adrenaline derivative and comprises valuable photopharmacological properties for further biological studies with high structural accordance to the native ligand adrenaline.
ISSN:0947-6539
1521-3765
DOI:10.1002/chem.202303506