Journal article

Hepta and octapeptide agonists of protease-activated receptor 2

Mark G Devlin, Bernhard Pfeiffer, Bernadine Flanagan, Renee L Beyer, Thomas M Cocks, David P Fairlie

JOURNAL OF PEPTIDE SCIENCE | JOHN WILEY & SONS LTD | Published : 2007

Abstract

Protease-activated receptor 2 (PAR(2)) is a G protein-coupled cell surface receptor for trypsin-like enzymes. Proteolytic cleavage at a specific site in the extracellular N-terminus exposes a receptor-activating sequence, the 'tethered ligand', which binds intramolecularly to initiate receptor signalling. Peptide or small molecule agonists for PAR(2), devoid of the non-specific and proteolytic effects of enzyme activators, may be promising therapeutic agents for proliferative and inflammatory diseases reportedly mediated by PAR(2). Synthetic hexapeptides that correspond to the native tethered ligand of human or rodent PAR(2) (SLIGKV and SLIGRL, respectively) can activate the receptor indepen..

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University of Melbourne Researchers