GRKs as Key Modulators of Opioid Receptor Function
Understanding the link between agonist-induced phosphorylation of the mu-opioid receptor (MOR) and the associated physiological effects is critical for the development of novel analgesic drugs and is particularly important for understanding the mechanisms responsible for opioid-induced tolerance and...
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| Format: | Article |
| Language: | English |
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MDPI AG
2020-11-01
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| Series: | Cells |
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| Online Access: | https://www.mdpi.com/2073-4409/9/11/2400 |
| _version_ | 1797549048949899264 |
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| author | Laura Lemel J Robert Lane Meritxell Canals |
| author_facet | Laura Lemel J Robert Lane Meritxell Canals |
| author_sort | Laura Lemel |
| collection | DOAJ |
| description | Understanding the link between agonist-induced phosphorylation of the mu-opioid receptor (MOR) and the associated physiological effects is critical for the development of novel analgesic drugs and is particularly important for understanding the mechanisms responsible for opioid-induced tolerance and addiction. The family of G protein receptor kinases (GRKs) play a pivotal role in such processes, mediating phosphorylation of residues at the C-tail of opioid receptors. Numerous strategies, such as phosphosite specific antibodies and mass spectrometry have allowed the detection of phosphorylated residues and the use of mutant knock-in mice have shed light on the role of GRK regulation in opioid receptor physiology. Here we review our current understanding on the role of GRKs in the actions of opioid receptors, with a particular focus on the MOR, the target of most commonly used opioid analgesics such as morphine or fentanyl. |
| first_indexed | 2024-03-10T15:09:09Z |
| format | Article |
| id | doaj.art-824c4c2f05f54840bce7eaf516bf6374 |
| institution | Directory Open Access Journal |
| issn | 2073-4409 |
| language | English |
| last_indexed | 2024-03-10T15:09:09Z |
| publishDate | 2020-11-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Cells |
| spelling | doaj.art-824c4c2f05f54840bce7eaf516bf63742023-11-20T19:32:14ZengMDPI AGCells2073-44092020-11-01911240010.3390/cells9112400GRKs as Key Modulators of Opioid Receptor FunctionLaura Lemel0J Robert Lane1Meritxell Canals2Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, Queen’s Medical Centre, University of Nottingham, Nottingham NG7 2UH, UKDivision of Physiology, Pharmacology and Neuroscience, School of Life Sciences, Queen’s Medical Centre, University of Nottingham, Nottingham NG7 2UH, UKDivision of Physiology, Pharmacology and Neuroscience, School of Life Sciences, Queen’s Medical Centre, University of Nottingham, Nottingham NG7 2UH, UKUnderstanding the link between agonist-induced phosphorylation of the mu-opioid receptor (MOR) and the associated physiological effects is critical for the development of novel analgesic drugs and is particularly important for understanding the mechanisms responsible for opioid-induced tolerance and addiction. The family of G protein receptor kinases (GRKs) play a pivotal role in such processes, mediating phosphorylation of residues at the C-tail of opioid receptors. Numerous strategies, such as phosphosite specific antibodies and mass spectrometry have allowed the detection of phosphorylated residues and the use of mutant knock-in mice have shed light on the role of GRK regulation in opioid receptor physiology. Here we review our current understanding on the role of GRKs in the actions of opioid receptors, with a particular focus on the MOR, the target of most commonly used opioid analgesics such as morphine or fentanyl.https://www.mdpi.com/2073-4409/9/11/2400opioidGPCRGRKkinases |
| spellingShingle | Laura Lemel J Robert Lane Meritxell Canals GRKs as Key Modulators of Opioid Receptor Function Cells opioid GPCR GRK kinases |
| title | GRKs as Key Modulators of Opioid Receptor Function |
| title_full | GRKs as Key Modulators of Opioid Receptor Function |
| title_fullStr | GRKs as Key Modulators of Opioid Receptor Function |
| title_full_unstemmed | GRKs as Key Modulators of Opioid Receptor Function |
| title_short | GRKs as Key Modulators of Opioid Receptor Function |
| title_sort | grks as key modulators of opioid receptor function |
| topic | opioid GPCR GRK kinases |
| url | https://www.mdpi.com/2073-4409/9/11/2400 |
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