The life cycle of the Mu-Opioid Receptor

Cuitavi, Javier; Hip�lito, Luc�a; Canals, Meritxell

Abstract

Opioid receptors are undisputed targets for the treatment of pain. Unfortunately, targeting these receptors therapeutically poses significant challenges including addiction, dependence, tolerance and the appearance of side-effects such as respiratory depression and constipation. Moreover, misuse of prescription and illicit narcotics has resulted in the current opioid crisis. The mu-opioid receptor is the cellular mediator of the effects of most commonly used opioids and is a prototypical G protein-coupled receptor (GPCR) where new pharmacological, signalling and cell biology concepts have been coined. This review summarises our knowledge of the life cycle of this therapeutic target including its biogenesis, trafficking to and from the plasma membrane, and how the regulation of these processes impacts its function and is related to pathophysiological conditions.

• Journal Article Type: Article
• Acceptance Date: Oct 1, 2020
• Online Publication Date: Oct 27, 2020
• Publication Date: Apr 1, 2021
• Deposit Date: Oct 12, 2020
• Publicly Available Date: Oct 28, 2021
• Journal: Trends in Biochemical Sciences
• Print ISSN: 0968-0004
• Electronic ISSN: 0167-7640
• Publisher: Elsevier
• Peer Reviewed: Peer Reviewed
• Volume: 46
• Issue: 4
• Pages: 315-328
• DOI: https://doi.org/10.1016/j.tibs.2020.10.002
• Keywords: G protein-coupled receptor; OPRM1; mu-opioid signalling; pain; reward; addiction
• Public URL: https://nottingham-repository.worktribe.com/output/4958683
• Publisher URL: https://www.sciencedirect.com/science/article/abs/pii/S0968000420302504