GRKs as Key Modulators of Opioid Receptor Function

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

Abstract

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.

Citation

Lemel, L., Lane, J. R., & Canals, M. (2020). GRKs as Key Modulators of Opioid Receptor Function. Cells, 9(11), Article 2400. https://doi.org/10.3390/cells9112400

• 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
• DOI: https://doi.org/10.3390/cells9112400
• Keywords: General Medicine
• Public URL: https://nottingham-repository.worktribe.com/output/6738731
• Publisher URL: https://www.mdpi.com/2073-4409/9/11/2400/htm