Development of Photoswitchable Tethered Ligands that Target the μ-Opioid Receptor
Lahmy R, Hübner H, Lachmann D, Gmeiner P, König B (2023)
Publication Type: Journal article
Publication year: 2023
Journal
Book Volume: 18
Article Number: e202300228
Journal Issue: 23
Abstract
Converting known ligands into photoswitchable derivatives offers the opportunity to modulate compound structure with light and hence, biological activity. In doing so, these probes provide unique control when evaluating G-protein-coupled receptor (GPCR) mechanism and function. Further conversion of such compounds into covalent probes, known as photoswitchable tethered ligands (PTLs), offers additional advantages. These include localization of the PTLs to the receptor binding pocket. Covalent localization increases local ligand concentration, improves site selectivity and may improve the biological differences between the respective isomers. This work describes chemical, photophysical and biochemical characterizations of a variety of PTLs designed to target the μ-opioid receptor (μOR). These PTLs were modeled on fentanyl, with the lead disulfide-containing agonist found to covalently interact with a cysteine-enriched mutant of this medically-relevant receptor.
Authors with CRIS profile
Harald Hübner
Lehrstuhl für Pharmazeutische Chemie
Peter Gmeiner
Lehrstuhl für Pharmazeutische Chemie
Involved external institutions
Germany (DE)How to cite
APA:
Lahmy, R., Hübner, H., Lachmann, D., Gmeiner, P., & König, B. (2023). Development of Photoswitchable Tethered Ligands that Target the μ-Opioid Receptor. ChemMedChem, 18(23). https://dx.doi.org/10.1002/cmdc.202300228
MLA:
Lahmy, Ranit, et al. "Development of Photoswitchable Tethered Ligands that Target the μ-Opioid Receptor." ChemMedChem 18.23 (2023).
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