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β₂ -Adrenoceptor agonist profiling reveals biased signalling phenotypes for the β₂ -adrenoceptor with possible implications for the treatment of asthma.

ABSTRACT:

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 (G_s )- and β-arrestin-mediated pathways. While G_s signalling is beneficial and promotes HASM relaxation, β-arrestin activation is associated with reduced G_s efficacy. In this context, biased ligands that selectively promote β₂ -adrenoceptor coupling to G_s signalling represent a promising strategy to treat asthma. Here, we examined several β-adrenoceptor agonists to identify G_s

SUBMITTER: De Pascali F

PROVIDER: S-EPMC9474705 | biostudies-literature | 2022 Oct

REPOSITORIES: biostudies-literature

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Dataset Information

β₂ -Adrenoceptor agonist profiling reveals biased signalling phenotypes for the β₂ -adrenoceptor with possible implications for the treatment of asthma.

Background and purpose

OmicsDI is part of the ELIXIR infrastructure

Tweets

Dataset Information

β2 -Adrenoceptor agonist profiling reveals biased signalling phenotypes for the β2 -adrenoceptor with possible implications for the treatment of asthma.

Background and purpose

OmicsDI is part of the ELIXIR infrastructure

Tweets

β₂ -Adrenoceptor agonist profiling reveals biased signalling phenotypes for the β₂ -adrenoceptor with possible implications for the treatment of asthma.