ArticleCommunications biology2025
Dynamics of agonist-evoked opioid receptor activation revealed by FRET- and BRET-based opioid receptor conformation sensors.
Article in Communications biology, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
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Who cites it
6 citing papers in PubMed.
- Uncoupling of the allosteric signalling network in the βNature communications · 2026Article
- Systematic Characterisation of GLP-1R in Human Enteric Nervous System: Implications for GLP-1 as a Key Regulator of Colonic Activity.Journal of neurochemistry · 2026Article
- A complex interplay of various intracellular motifs determines G protein binding and activation of muscarinic receptors.Scientific reports · 2026Article
- In vitro and in vivo pharmacological characterization of fentanyl analogs.Neuropharmacology · 2025Article
- Conformational Heterogeneity Underlying Divergent Signaling in Class A G Protein-Coupled Receptors.ACS pharmacology & translational science · 2025Review
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Authors and funding
6 authors.
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Abstract
The opioid receptor family, particularly the µ opioid receptor, are the main drug targets in the management of severe pain. However, their pain-relieving effects are often accompanied by severe adverse effects, underlining the necessity for extensive research on this receptor family. Opioids, the agonists targeting these receptors, differ in their chemical structure and also in their mode of action in different aspects of signaling. Here we introduce novel tools that facilitate the analysis of this receptor family, by the development of FRET- and BRET-based receptor conformation sensors. With these sensors we were able to characterize especially the µ opioid receptor in more detail and reveal a strongly agonist-dependent activation kinetics for this receptor. Moreover, our sensors offer an assay independent from other signaling pathways, thereby minimizing the potential for interfering influences or biases within the system.
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