β-Arrestin-biased proteinase-activated receptor-2 antagonist C781 limits allergen-induced airway hyperresponsiveness and inflammation.

Hillary V SchiffCandy M RivasWilliam P PedersonEstevan SandovalSamuel GillmanJoy PriscoMoeno KumeGregory DussorJosef VagnerJulie G LedfordTheodore J PriceKathryn A DeFeaScott Boitano

Published in: British journal of pharmacology (2022)

Our work demonstrates the first biased PAR2 antagonist for β-arrestin/MAPK signalling. C781 is efficacious as a prophylactic treatment for allergen-induced airway hyperresponsiveness and inflammation in mice. It exemplifies a key pharmacophore for PAR2 that can be optimized for clinical development.

Keyphrases

oxidative stress
diabetic rats
high glucose
molecular dynamics
molecular docking
type diabetes
pi k akt