Preferential Gs protein coupling of the galanin Gal₁ receptor in the µ-opioid-Gal₁ receptor heterotetramer.

ABSTRACT: Recent studies have proposed that heteromers of µ-opioid receptors (MORs) and galanin Gal₁ receptors (Gal₁Rs) localized in the mesencephalon mediate the dopaminergic effects of opioids. The present study reports converging evidence, using a peptide-interfering approach combined with biophysical and biochemical techniques, including total internal reflection fluorescence microscopy, for a predominant homodimeric structure of MOR and Gal₁R when expressed individually, and for their preference to form functional heterotetramers when co-expressed. Results show that a heteromerization-dependent change in the Gal₁R homodimeric interface leads to a switch in G-protein coupling from inhibitory Gi to stimulatory Gs proteins. The MOR-Gal₁R heter

SUBMITTER: De Oliveira PA 

PROVIDER: S-EPMC9462584 | biostudies-literature | 2022 Aug

REPOSITORIES: biostudies-literature