Biased Coupling to β-Arrestin of Two Common Variants of the CB₂ Cannabinoid Receptor.

ABSTRACT: β-arrestins are partners of the G protein-coupled receptors (GPCRs), regulating their intracellular trafficking and signaling. Development of biased GPCR agonists, selectively targeting either G protein or β-arrestin pathways, are in the focus of interest due to their therapeutic potential in different pathological conditions. The CB₂ cannabinoid receptor (CB₂R) is a GPCR involved in various functions in the periphery and the central nervous system. Two common occurring variants of CB₂R, harboring Q63R or L133I missense mutations, have been implicated in the development of a diverse set of disorders. To evaluate the effect of these mutations, we characterized the binding profile of these mutant CB₂ receptors to G proteins and β-arrestin2. Althoug

SUBMITTER: Turu G 

PROVIDER: S-EPMC8415483 | biostudies-literature | 2021

REPOSITORIES: biostudies-literature