"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 |
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Hauptverfasser: | , , , , , , , |
Format: | Artikel |
Sprache: | eng |
Online-Zugang: | Volltext |
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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. |
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ISSN: | 0947-6539 1521-3765 |
DOI: | 10.1002/chem.202303506 |