A refined agonist pharmacophore for protease activated receptor 2.

A refined agonist pharmacophore for protease activated receptor 2. Research Abstract Details 

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A refined agonist pharmacophore for protease activated receptor 2. Abstract Text:

Grant D Barry,Jacky Y Suen,Heng Boon Low,Bernhard Pfeiffer,Bernadine Flanagan,Maria Halili,Giang T Le,David P Fairlie,Grant D Barry,Jacky Y Suen,Heng Boon Low,Bernhard Pfeiffer,Bernadine Flanagan,Maria Halili,Giang T Le,David P Fairlie,

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.

A refined agonist pharmacophore for protease activated receptor 2. Publishing Authors By Initials

GD Barry,JY Suen,HB Low,B Pfeiffer,B Flanagan,M Halili,GT Le,DP Fairlie,GD Barry,JY Suen,HB Low,B Pfeiffer,B Flanagan,M Halili,GT Le,DP Fairlie,

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A refined agonist pharmacophore for protease activated receptor 2. Journal Published:

PUBLICATION TYPE: Research Support, Non-U.S. Gov

Journal: Bioorganic & medicinal chemistry letters

VOLUME: 17

Page Numbers: 5552-7

Journal Abbreviation: Bioorg. Med. Chem. Lett.

ISSN: 0960-894X

DAY: 16

MONTH: 08

YEAR: 2007

A refined agonist pharmacophore for protease activated receptor 2. Information

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LANGUAGE: eng

NlmUniqueID: 9107377

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Grant and Affiliation Information for A refined agonist pharmacophore for protease activated receptor 2.

AFFILIATION: Centre for Drug Design and Development, Institute for Molecular Bioscience, University of Queensland, Brisbane, Qld. 4072, Australia.

Country: England

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MEDLINETA: Bioorg Med Chem Lett

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