2. Academic Validation
  3. A refined agonist pharmacophore for protease activated receptor 2

A refined agonist pharmacophore for protease activated receptor 2

  • Bioorg Med Chem Lett. 2007 Oct 15;17(20):5552-7. doi: 10.1016/j.bmcl.2007.08.026.
Grant D Barry 1,  Jacky Y Suen,  Heng Boon Low,  Bernhard Pfeiffer,  Bernadine Flanagan,  Maria Halili,  Giang T Le,  David P Fairlie
Affiliations

Affiliation

  • 1 Centre for Drug Design and Development, Institute for Molecular Bioscience, University of Queensland, Brisbane, Qld. 4072, Australia.
PMID: 17765542 DOI: 10.1016/j.bmcl.2007.08.026
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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