GRKs as Key Modulators of Opioid Receptor Function.
GPCR
GRK
kinases
opioid
Journal
Cells
ISSN: 2073-4409
Titre abrégé: Cells
Pays: Switzerland
ID NLM: 101600052
Informations de publication
Date de publication:
02 11 2020
02 11 2020
Historique:
received:
07
10
2020
revised:
21
10
2020
accepted:
28
10
2020
entrez:
5
11
2020
pubmed:
6
11
2020
medline:
16
6
2021
Statut:
epublish
Résumé
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.
Identifiants
pubmed: 33147802
pii: cells9112400
doi: 10.3390/cells9112400
pmc: PMC7692057
pii:
doi:
Substances chimiques
Mutant Proteins
0
Receptors, Opioid, mu
0
G-Protein-Coupled Receptor Kinases
EC 2.7.11.16
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Review
Langues
eng
Sous-ensembles de citation
IM
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