Phenotypic screening of cannabinoid receptor 2 ligands shows different sensitivity to genotype

The Cannabinoid Receptor 2 (CB2R) is a G protein-coupled receptor (GPCR) investigated intensively as therapeutic target, however no drug has reached the market yet. We investigated personal differences in CB2R drug responses using a label-free whole-cell assay (xCELLigence) combined with cell lines (Lymphoblastoid Cell Lines) from individuals with varying CB2R genotypes. Responses to agonists, partial agonists and antagonists of various chemical classes were characterized. Endogenous cannabinoids such as 2-AG induced cellular effects vastly different from all synthetic cannabinoids, especially... Mehr ...

Verfasser: Hillger, Julia M
le Roy, Beau
Wang, Zi
Mulder-Krieger, Thea
Boomsma, Dorret I
Slagboom, P. Eline
Danen, Erik H J
IJzerman, Adriaan P
Heitman, Laura H
Dokumenttyp: Artikel
Erscheinungsdatum: 2017
Reihe/Periodikum: Hillger , J M , le Roy , B , Wang , Z , Mulder-Krieger , T , Boomsma , D I , Slagboom , P E , Danen , E H J , IJzerman , A P & Heitman , L H 2017 , ' Phenotypic screening of cannabinoid receptor 2 ligands shows different sensitivity to genotype ' , Biochemical Pharmacology , vol. 130 , pp. 60-70 . https://doi.org/10.1016/j.bcp.2017.01.014
Schlagwörter: Journal Article / /dk/atira/pure/keywords/cohort_studies/netherlands_twin_register_ntr_ / name=Netherlands Twin Register (NTR) / /dk/atira/pure/sustainabledevelopmentgoals/good_health_and_well_being / name=SDG 3 - Good Health and Well-being
Sprache: Englisch
Permalink: https://search.fid-benelux.de/Record/base-27623015
Datenquelle: BASE; Originalkatalog
Powered By: BASE
Link(s) : https://research.vu.nl/en/publications/eed7d277-4029-4d14-bb7e-0dfe79fcdf78

The Cannabinoid Receptor 2 (CB2R) is a G protein-coupled receptor (GPCR) investigated intensively as therapeutic target, however no drug has reached the market yet. We investigated personal differences in CB2R drug responses using a label-free whole-cell assay (xCELLigence) combined with cell lines (Lymphoblastoid Cell Lines) from individuals with varying CB2R genotypes. Responses to agonists, partial agonists and antagonists of various chemical classes were characterized. Endogenous cannabinoids such as 2-AG induced cellular effects vastly different from all synthetic cannabinoids, especially in their time-profile. Secondly, the Q63R polymorphism affected CB2R responses in general. Agonists and especially partial agonists showed higher efficacy in a Q63R minor homozygote versus other genotypes. Non-classical cannabinoid CP55940 showed the most pronounced personal effects with highly reduced potency and efficacy in this genotype. Contrarily, aminoalkylindole compounds showed less individual differences. In conclusion, a label-free whole-cell assay combined with personal cell lines is a promising vehicle to investigate personal differences in drug response originating from genetic variation in GPCRs. Such phenotypic screening allows early identification of compounds prone to personal differences ('precision medicine') or more suited as drugs for the general population.