Agonist efficacy at the β2AR is driven by the faster association rate of the Gs protein

Agonist efficacy at the β2AR is driven by the faster association rate of the Gs protein

IntroductionThe β2-adrenoceptor (β2AR) is a class A G protein-coupled receptor (GPCR). It is therapeutically relevant in asthma and chronic obstructive pulmonary disease (COPD), where β2AR agonists relieve bronchoconstriction. The β2AR is a prototypical GPCR for structural and biophysical studies. H...

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Bibliographic Details
Main Authors: Clare R. Harwood, David A. Sykes, Theo Redfern-Nichols, Owen Underwood, Colin Nicholson, Armin N. Khoshgrudi, Eline J. Koers, Graham Ladds, Stephen J. Briddon, Dmitry B. Veprintsev
Format: Article
Language:English
Published: Frontiers Media S.A. 2025-03-01
Series:Frontiers in Pharmacology
Subjects:
G protein-coupled receptor
β2-adrenoceptor
efficacy
kinetics
association rate kon
dissociation rate koff
Online Access:https://www.frontiersin.org/articles/10.3389/fphar.2025.1367991/full
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https://www.frontiersin.org/articles/10.3389/fphar.2025.1367991/full

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