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ID: ALA1137449
Journal: Bioorg Med Chem Lett
Title: A refined agonist pharmacophore for protease activated receptor 2.
Authors: Barry GD, Suen JY, Low HB, Pfeiffer B, Flanagan B, Halili M, Le GT, Fairlie DP.
Abstract: Protease activated receptor 2 (PAR(2)) is a G protein-coupled receptor implicated in inflammation and cancer. Only a few peptide agonists are known with greater potency than the native agonist SLIGRL-NH(2). Here we report 52 peptide agonists of PAR(2), 26 with activity at sub-micromolar concentrations, and one being iodinated for radioligand experiments. Potency was highest when the N- or C-termini of SLIGRL-NH(2) were modified, pointing to a new ligand pharmacophore model that may aid development of drug-like PAR(2) modulators.
CiteXplore: 17765542