A refined agonist pharmacophore for protease activated receptor 2 |
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Authors: | Barry Grant D Suen Jacky Y Low Heng Boon Pfeiffer Bernhard Flanagan Bernadine Halili Maria Le Giang T Fairlie David P |
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Institution: | Centre for Drug Design and Development, Institute for Molecular Bioscience, University of Queensland, Brisbane, Qld. 4072, Australia. |
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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. |
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