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Schematic representation of PAR2 activation by trypsin. PAR2 is activated upon trypsin cleavage within the sequence N34SKGR/SLIGRLETQP48 of its extracellular -NH2 terminus. This event unmasks a tethered ligand, SLIGRLETQP, that binds the cleaved receptor activating it. Synthetic peptides mimicking the tethered ligand sequence, SLIGRLETQ …, can activate the receptor even in absence of proteolysis.
