Article
β2 -Adrenoceptor agonist profiling reveals biased signalling phenotypes for the β2 -adrenoceptor with possible implications for the treatment of asthma.
British journal of pharmacology - 1 Oct 2022
De Pascali Francesco, Ippolito Michael, Wolfe Emily, Komolov Konstantin E, Hopfinger Nathan, Lemenze Douglas, Kim Nicholas, Armen Roger S, An Steven S, Scott Charles P, Benovic Jeffrey L
Abstract excerpt
BACKGROUND AND PURPOSE: β-Adrenoceptor agonists relieve airflow obstruction by activating β2 -adrenoceptors, which are G protein-coupled receptors (GPCRs) expressed on human airway smooth muscle (HASM) cells. The currently available β-adrenoceptor agonists are balanced agonists, however, and signal through both the stimulatory G protein (Gs )- and β-arrestin-mediated pathways. While Gs signalling is beneficial...
Topics
- Adrenergic beta-Agonists
- Asthma
- GTP-Binding Protein alpha Subunits, Gs
- Humans
- Phenotype
- Receptors, Adrenergic, beta-2
- Signal Transduction
- beta-Arrestin 1
- beta-Arrestins