Ontology highlight
ABSTRACT:
SUBMITTER: Yeliseev A
PROVIDER: S-EPMC7881127 | biostudies-literature | 2021 Feb
REPOSITORIES: biostudies-literature
Yeliseev Alexei A Iyer Malliga R MR Joseph Thomas T TT Coffey Nathan J NJ Cinar Resat R Zoubak Lioudmila L Kunos George G Gawrisch Klaus K
Scientific reports 20210212 1
Signaling through integral membrane G protein-coupled receptors (GPCRs) is influenced by lipid composition of cell membranes. By using novel high affinity ligands of human cannabinoid receptor CB<sub>2</sub>, we demonstrate that cholesterol increases basal activation levels of the receptor and alters the pharmacological categorization of these ligands. Our results revealed that (2-(6-chloro-2-((2,2,3,3-tetramethylcyclopropane-1-carbonyl)imino)benzo[d]thiazol-3(2H)-yl)ethyl acetate ligand (MRI-26 ...[more]