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

DOI: 10.1002/cmdc.202300228

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.

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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://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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