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GRKs as Key Modulators of Opioid Receptor Function

Lemel, Laura; Lane, J Robert; Canals, Meritxell

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Laura Lemel

Associate Professor


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.

Journal Article Type Review
Acceptance Date Oct 28, 2021
Online Publication Date Nov 2, 2020
Publication Date Nov 2, 2020
Deposit Date Nov 19, 2021
Publicly Available Date Nov 19, 2021
Journal Cells
Electronic ISSN 2073-4409
Publisher MDPI
Peer Reviewed Peer Reviewed
Volume 9
Issue 11
Article Number 2400
Keywords General Medicine
Public URL
Publisher URL


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