Cannabidiol skews biased agonism at cannabinoid CB1 and CB2 receptors with smaller effect in CB1‐CB2 heteroreceptor complexes
Sign Up to like & getrecommendations! Published in 2018 at "Biochemical Pharmacology"
DOI: 10.1016/j.bcp.2018.08.046
Abstract: Graphical abstract Figure. No Caption available. ABSTRACT Currently, biased agonism is at the center stage of drug development approaches. We analyzed effects of a battery of cannabinoids plus/minus cannabidiol (CBD) in four functional parameters (cAMP… read more here.
Keywords: effect; cb1 cb2; biased agonism;
Biased agonism at β-adrenergic receptors.
Sign Up to like & getrecommendations! Published in 2020 at "Cellular signalling"
DOI: 10.1016/j.cellsig.2020.109905
Abstract: The β-adrenergic receptors (βARs) include three subtypes, β1, β2 and β3. These receptors are widely expressed and regulate numerous physiological processes including cardiovascular and metabolic functions and airway tone. The βARs are also important targets… read more here.
Keywords: adrenergic receptors; biased agonism; agonism adrenergic;
In vivo biased agonism at 5-HT1A receptors: characterisation by simultaneous PET/MR imaging
Sign Up to like & getrecommendations! Published in 2018 at "Neuropsychopharmacology"
DOI: 10.1038/s41386-018-0145-2
Abstract: In neuropharmacology, the recent concept of 'biased agonism' denotes the capacity of certain agonists to target-specific intracellular pathways of a given receptor in specific brain areas. In the context of serotonin pharmacotherapy, 5-HT1A receptor-biased agonists… read more here.
Keywords: biased agonism; pet imaging; ht1a; receptor ... See more keywords
Conformational signatures in β-arrestin2 reveal natural biased agonism at a G-protein-coupled receptor
Sign Up to like & getrecommendations! Published in 2018 at "Communications Biology"
DOI: 10.1038/s42003-018-0134-3
Abstract: Discovery of biased ligands and receptor mutants allows characterization of G-protein- and β-arrestin-mediated signaling mechanisms of G-protein-coupled receptors (GPCRs). However, the structural mechanisms underlying biased agonism remain unclear for many GPCRs. We show that while… read more here.
Keywords: protein; biased agonism; conformational signatures; protein coupled ... See more keywords
G protein signaling–biased agonism at the κ-opioid receptor is maintained in striatal neurons
Sign Up to like & getrecommendations! Published in 2018 at "Science Signaling"
DOI: 10.1126/scisignal.aar4309
Abstract: Triazole 1.1 is a G protein–biased agonist of the κ-opioid receptor in striatal neurons. Biasing pain treatment against side effects Stimulating opioid receptors with targeted agonists can treat pain, but such drugs often cause unwanted… read more here.
Keywords: biased agonism; opioid receptor; striatal neurons; protein signaling ... See more keywords
Biased Agonism: Lessons from Studies of Opioid Receptor Agonists.
Sign Up to like & getrecommendations! Published in 2022 at "Annual review of pharmacology and toxicology"
DOI: 10.1146/annurev-pharmtox-052120-091058
Abstract: In ligand bias different agonist drugs are thought to produce distinct signaling outputs when activating the same receptor. If these signaling outputs mediate therapeutic versus adverse drug effects, then agonists that selectively activate the therapeutic… read more here.
Keywords: toxicology; receptor agonists; opioid receptor; pharmacology ... See more keywords
Influence of Chemokine N-Terminal Modification on Biased Agonism at the Chemokine Receptor CCR1
Sign Up to like & getrecommendations! Published in 2019 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms20102417
Abstract: Leukocyte migration, a hallmark of the inflammatory response, is stimulated by the interactions between chemokines, which are expressed in injured or infected tissues, and chemokine receptors, which are G protein-coupled receptors (GPCRs) expressed in the… read more here.
Keywords: receptor; biased agonism; receptor ccr1; chemokine receptor ... See more keywords