Cannabinoid 1 (CB₁ ) receptor arrestin subtype-selectivity and phosphorylation dependence.

ABSTRACT:

Background and purpose

Arrestin or G protein bias may be desirable for novel cannabinoid therapeutics. Arrestin-2 and arrestin-3 translocation to CB₁ receptor have been suggested to mediate different functions that may be exploited with biased ligands. Here, the requirement of a recently described phosphorylation motif 'pxxp' (where 'p' denotes phosphorylatable serine or threonine and 'x' denotes any other amino acid) within the CB₁ receptor C-terminus for interaction with different arrestin subtypes was examined.

Experimental approach

Site-directed mutagenesis was conducted to generate nine different phosphorylation-impaired CB₁ receptor C-terminal mutants. Bioluminescence resonance energy transfer (BRET) was employed to measure arrestin-2/3

SUBMITTER: Manning JJ 

PROVIDER: S-EPMC10100024 | biostudies-literature | 2023 Feb

REPOSITORIES: biostudies-literature