Avet et al. characterize I-287, an inhibitor to protease-activated receptor 2 using BRET-assays. They find that I-287 selectively inhibits Gαq and Gα12/13 without affecting the activation of Gi/o or the recruitment of βarrestin2 and that it blocks inflammation in vitro and in vivo.
- Charlotte Avet
- Claudio Sturino
- Michel Bouvier
