Mechanism of opioid receptor ubiquitination and its effect on receptor function
10.3867/j.issn.1000-3002.2015.02.019
- VernacularTitle:阿片受体泛素化机制及其对受体功能的影响
- Author:
Jiebing JLANG
;
Peilan ZHOU
;
Zhibing ZHENG
;
Ruibin SU
- Publication Type:Journal Article
- Keywords:
ubiquitination;
opioid receptor;
G protein-coupled receptors;
lysosome
- From:
Chinese Journal of Pharmacology and Toxicology
2015;(2):302-309
- CountryChina
- Language:Chinese
-
Abstract:
Opioid receptors, as an important member of G protein coupled receptors (GPCR), are the binding targets of endogenous opioid peptides and exogenous opiates. The activation of opioid receptors influences the nervous system, immune physiology and endocrine system. However, prolonged activation of opioid receptors is likely to produce opioid tolerance, leading to opioid addiction. Receptor endocytosis and sorting into the recycling pathway contribute to recovery of cellular opioid responsiveness. Recent studies have revealed that GPCR can be modulated by ubiquitination which plays a unique roles in governing GPCR trafficking. Moreover, ubiquitination of the opioid receptors (μ, κand δ) is increased after stimulation of most opioid agonists. Mutation of the ubiquitin sites affects the internalization and degradation of opioid receptors, which contributes to changes in signal pathways and regulation of opioid receptors. ln this paper, ubiquitination of opioid receptors and the fundamental role of ubiquitination in trafficking of opioid receptors are reviewed.
