A refined agonist pharmacophore for protease activated receptor 2

被引：21

作者：

Barry, Grant D. ^{[1
]}

Suen, Jacky Y. ^{[1
]}

Low, Heng Boon ^{[1
]}

Pfeiffer, Bernhard ^{[1
]}

Flanagan, Bernadine ^{[1
]}

Halili, Maria ^{[1
]}

Le, Giang T. ^{[1
]}

Fairlie, David P. ^{[1
]}

机构：

[1] Univ Queensland, Inst Mol Biosci, Ctr Drug Design & Dev, Brisbane, Qld 4072, Australia

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 20期

基金：

英国医学研究理事会; 澳大利亚研究理事会;

关键词：

PAR(2); agonist; PAR(1); fluorescence; inflammation;

D O I：

10.1016/j.bmcl.2007.08.026

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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-NH2. 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-NH2 were modified, pointing to a new ligand pharmacophore model that may aid development of drug-like PAR(2) modulators. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：5552 / 5557

页数：6

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