Development of a membrane-based Gi-CASE biosensor assay for profiling compounds at cannabinoid receptors.

ABSTRACT: Introduction: The cannabinoid receptor (CBR) subtypes 1 (CB₁R) and 2 (CB₂R) are key components of the endocannabinoid system (ECS), playing a central role in the control of peripheral pain, inflammation and the immune response, with further roles in the endocrine regulation of food intake and energy balance. So far, few medicines targeting these receptors have reached the clinic, suggesting that a better understanding of the receptor signalling properties of existing tool compounds and clinical candidates may open the door to the development of more effective and safer treatments. Both CB₁R and CB₂R are Gα_i protein-coupled receptors but detecting Gα_i protein signalling activity reliably and reproducibly is challenging

SUBMITTER: Scott-Dennis M 

PROVIDER: S-EPMC10450933 | biostudies-literature | 2023

REPOSITORIES: biostudies-literature