Title of article
A refined agonist pharmacophore for protease activated receptor 2
Author/Authors
Grant D. Barry، نويسنده , , Jacky Y. Suen، نويسنده , , Heng Boon Low، نويسنده , , Bernhard Pfeiffer، نويسنده , , Bernadine Flanagan، نويسنده , , Maria Halili، نويسنده , , Giang T. Le، نويسنده , , David P. Fairlie، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
6
From page
5552
To page
5557
Abstract
Protease activated receptor 2 (PAR2) 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-NH2. Here we report 52 peptide agonists of PAR2, 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-NH2 were modified, pointing to a new ligand pharmacophore model that may aid development of drug-like PAR2 modulators.
Keywords
PAR2 , agonist , PAR1 , inflammation , fluorescence
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798652
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