Skip to main content

Research Repository

Advanced Search

GRK mediates ?-opioid receptor plasma membrane reorganization

Gondin, Arisbel B.; Halls, Michelle L.; Canals, Meritxell; Briddon, Stephen J.


Arisbel B. Gondin

Michelle L. Halls


Differential regulation of the ?-opioid receptor (MOP) has been linked to the development of opioid tolerance and dependence which both limit the clinical use of opioid analgesics. At a cellular level, MOP regulation occurs via receptor phosphorylation, desensitization, plasma membrane redistribution, and internalization. Here, we used fluorescence correlation spectroscopy (FCS) and fluorescence recovery after photobleaching (FRAP) to detect and quantify ligand-dependent changes in the plasma membrane organization of MOP expressed in human embryonic kidney (HEK293) cells. The low internalizing agonist morphine and the antagonist naloxone did not alter constitutive MOP plasma membrane organization. In contrast, the internalizing agonist DAMGO changed MOP plasma membrane organization in a pertussis toxin-insensitive manner and by two mechanisms. Firstly, it slowed MOP diffusion in a manner that was independent of internalization but dependent on GRK2/3. Secondly, DAMGO reduced the surface receptor number and the proportion of mobile receptors, and increased receptor clustering in a manner that was dependent on clathrin-mediated endocytosis. Overall, these results suggest the existence of distinct sequential MOP reorganization events at the plasma membrane and provide insights into the specific protein interactions that control MOP plasma membrane organization.


Gondin, A. B., Halls, M. L., Canals, M., & Briddon, S. J. (2019). GRK mediates ?-opioid receptor plasma membrane reorganization. Frontiers in Molecular Neuroscience, 12,

Journal Article Type Article
Acceptance Date Apr 8, 2019
Online Publication Date May 1, 2019
Publication Date May 1, 2019
Deposit Date Apr 30, 2019
Publicly Available Date May 1, 2019
Journal Frontiers in Molecular Neuroscience
Electronic ISSN 1662-5099
Publisher Frontiers Media
Peer Reviewed Peer Reviewed
Volume 12
Keywords Molecular Biology; Cellular and Molecular Neuroscience
Public URL
Publisher URL


You might also like

Downloadable Citations