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

ABSTRACT:

Background and purpose

Asthma is a heterogenous disease strongly associated with inflammation that has many different causes and triggers. Current asthma treatments target symptoms such as bronchoconstriction and airway inflammation. Despite recent advances in biological therapies, there remains a need for new classes of therapeutic agents with novel, upstream targets. The proteinase-activated receptor-2 (PAR2) has long been implicated in allergic airway inflammation and asthma and it remains an intriguing target for novel therapies. Here, we describe the actions of C781, a newly developed low MW PAR2 biased antagonist, in vitro and in vivo in the context of acute allergen exposure.

Experimental approach

A human bronchial epithelial cell line expressing PAR2 (16HBE14o- cells

SUBMITTER: Schiff HV 

PROVIDER: S-EPMC10311467 | biostudies-literature | 2023 Mar

REPOSITORIES: biostudies-literature