Optimization of the Heterologous Expression of the Cannabinoid Type-1 (CB₁) Receptor.

ABSTRACT: The G protein-coupled type 1 cannabinoid receptor (CB₁R) mediates virtually all classic cannabinoid effects, and both its agonists and antagonists hold major therapeutic potential. Heterologous expression of receptors is vital for pharmacological research, however, overexpression of these proteins may fundamentally alter their localization pattern, change the signalling partner preference and may also spark artificial clustering. Additionally, recombinant CB₁Rs are prone to intense proteasomal degradation, which may necessitate substantial modifications, such as N-terminal truncation or signal sequence insertion, for acceptable cell surface expression. We report here that tuning down the expression intensity of the full-length CB₁R reduces proteasomal degra

SUBMITTER: Horvath VB 

PROVIDER: S-EPMC8564136 | biostudies-literature | 2021

REPOSITORIES: biostudies-literature