The novel PAR2 ligand C391 blocks multiple PAR2 signalling pathways in vitro and in vivo.

Abstract

BACKGROUND AND PURPOSE Proteinase-activated receptor-2 (PAR2) is a GPCR linked to diverse pathologies, including acute and chronic pain. PAR2 is one of the four PARs that are activated by proteolytic cleavage of the extracellular amino terminus, resulting in an exposed, tethered peptide agonist. Several peptide and peptidomimetic agonists, with high potency… (More)
DOI: 10.1111/bph.13238

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