Ontology highlight
ABSTRACT:
SUBMITTER: Fay JF
PROVIDER: S-EPMC3460482 | biostudies-literature | 2012 Sep
REPOSITORIES: biostudies-literature
Fay Jonathan F JF Farrens David L DL
The Journal of biological chemistry 20120730 40
Allosteric ligands that modulate how G protein-coupled receptors respond to traditional orthosteric drugs are an exciting and rapidly expanding field of pharmacology. An allosteric ligand for the cannabinoid receptor CB1, Org 27569, exhibits an intriguing effect; it increases agonist binding, yet blocks agonist-induced CB1 signaling. Here we explored the mechanism behind this behavior, using a site-directed fluorescence labeling approach. Our results show that Org 27569 blocks conformational cha ...[more]