Dynamics of agonist-evoked opioid receptor activation revealed by FRET- and BRET-based opioid receptor conformation sensors
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. Opioid...
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| Format: | Article |
| Language: | English |
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Nature Portfolio
2025-02-01
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| Series: | Communications Biology |
| Online Access: | https://doi.org/10.1038/s42003-025-07630-x |
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| author | Sina B. Kirchhofer Claudia Kurz Lorenz Geier Anna-Lena Krett Cornelius Krasel Moritz Bünemann |
| author_facet | Sina B. Kirchhofer Claudia Kurz Lorenz Geier Anna-Lena Krett Cornelius Krasel Moritz Bünemann |
| author_sort | Sina B. Kirchhofer |
| collection | DOAJ |
| description | 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. |
| format | Article |
| id | doaj-art-6474018540864ad6b8b8cf58d996d265 |
| institution | Kabale University |
| issn | 2399-3642 |
| language | English |
| publishDate | 2025-02-01 |
| publisher | Nature Portfolio |
| record_format | Article |
| series | Communications Biology |
| spelling | doaj-art-6474018540864ad6b8b8cf58d996d2652025-02-09T12:50:43ZengNature PortfolioCommunications Biology2399-36422025-02-018111110.1038/s42003-025-07630-xDynamics of agonist-evoked opioid receptor activation revealed by FRET- and BRET-based opioid receptor conformation sensorsSina B. Kirchhofer0Claudia Kurz1Lorenz Geier2Anna-Lena Krett3Cornelius Krasel4Moritz Bünemann5Department of Pharmacology and Clinical Pharmacy, University of MarburgDepartment of Pharmacology and Clinical Pharmacy, University of MarburgDepartment of Pharmacology and Clinical Pharmacy, University of MarburgDepartment of Pharmacology and Clinical Pharmacy, University of MarburgDepartment of Pharmacology and Clinical Pharmacy, University of MarburgDepartment of Pharmacology and Clinical Pharmacy, University of MarburgAbstract 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.https://doi.org/10.1038/s42003-025-07630-x |
| spellingShingle | Sina B. Kirchhofer Claudia Kurz Lorenz Geier Anna-Lena Krett Cornelius Krasel Moritz Bünemann Dynamics of agonist-evoked opioid receptor activation revealed by FRET- and BRET-based opioid receptor conformation sensors Communications Biology |
| title | Dynamics of agonist-evoked opioid receptor activation revealed by FRET- and BRET-based opioid receptor conformation sensors |
| title_full | Dynamics of agonist-evoked opioid receptor activation revealed by FRET- and BRET-based opioid receptor conformation sensors |
| title_fullStr | Dynamics of agonist-evoked opioid receptor activation revealed by FRET- and BRET-based opioid receptor conformation sensors |
| title_full_unstemmed | Dynamics of agonist-evoked opioid receptor activation revealed by FRET- and BRET-based opioid receptor conformation sensors |
| title_short | Dynamics of agonist-evoked opioid receptor activation revealed by FRET- and BRET-based opioid receptor conformation sensors |
| title_sort | dynamics of agonist evoked opioid receptor activation revealed by fret and bret based opioid receptor conformation sensors |
| url | https://doi.org/10.1038/s42003-025-07630-x |
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