Small-molecule-biased formyl peptide receptor agonist compound 17b protects against myocardial ischaemia-reperfusion injury in mice

G Protein-Coupled Receptors (GPCRs) can adopt different conformations, each linked to distinct cellular outcomes. Here the authors show that compound 17b, a novel agonist of the GPCR family member FPR, robustly activates cardioprotective but not detrimental FPR signalling, showing beneficial therape...

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Main Authors: Cheng Xue Qin, Lauren T. May, Renming Li, Nga Cao, Sarah Rosli, Minh Deo, Amy E. Alexander, Duncan Horlock, Jane E. Bourke, Yuan H. Yang, Alastair G. Stewart, David M. Kaye, Xiao-Jun Du, Patrick M. Sexton, Arthur Christopoulos, Xiao-Ming Gao, Rebecca H. Ritchie
Format: Article
Language:English
Published: Nature Publishing Group 2017-02-01
Series:Nature Communications
Online Access:https://doi.org/10.1038/ncomms14232
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spelling doaj-662689059cf2432b82994c3add7656fb2021-05-11T07:51:25ZengNature Publishing GroupNature Communications2041-17232017-02-018111310.1038/ncomms14232Small-molecule-biased formyl peptide receptor agonist compound 17b protects against myocardial ischaemia-reperfusion injury in miceCheng Xue Qin0Lauren T. May1Renming Li2Nga Cao3Sarah Rosli4Minh Deo5Amy E. Alexander6Duncan Horlock7Jane E. Bourke8Yuan H. Yang9Alastair G. Stewart10David M. Kaye11Xiao-Jun Du12Patrick M. Sexton13Arthur Christopoulos14Xiao-Ming Gao15Rebecca H. Ritchie16Baker IDI Heart and Diabetes InstituteDepartment of Pharmacology, Division of Drug Discovery Biology, Department of Pharmacology, Monash UniversityBaker IDI Heart and Diabetes InstituteBaker IDI Heart and Diabetes InstituteBaker IDI Heart and Diabetes InstituteBaker IDI Heart and Diabetes InstituteBaker IDI Heart and Diabetes InstituteBaker IDI Heart and Diabetes InstituteDepartment of Pharmacology, Monash UniversityCentre of Inflammatory Diseases, Monash UniversityDepartment of Pharmacology, University of MelbourneBaker IDI Heart and Diabetes InstituteBaker IDI Heart and Diabetes InstituteDepartment of Pharmacology, Division of Drug Discovery Biology, Department of Pharmacology, Monash UniversityDepartment of Pharmacology, Division of Drug Discovery Biology, Department of Pharmacology, Monash UniversityBaker IDI Heart and Diabetes InstituteBaker IDI Heart and Diabetes InstituteG Protein-Coupled Receptors (GPCRs) can adopt different conformations, each linked to distinct cellular outcomes. Here the authors show that compound 17b, a novel agonist of the GPCR family member FPR, robustly activates cardioprotective but not detrimental FPR signalling, showing beneficial therapeutic effect in a mouse model of cardiac infarction.https://doi.org/10.1038/ncomms14232
collection DOAJ
language English
format Article
sources DOAJ
author Cheng Xue Qin
Lauren T. May
Renming Li
Nga Cao
Sarah Rosli
Minh Deo
Amy E. Alexander
Duncan Horlock
Jane E. Bourke
Yuan H. Yang
Alastair G. Stewart
David M. Kaye
Xiao-Jun Du
Patrick M. Sexton
Arthur Christopoulos
Xiao-Ming Gao
Rebecca H. Ritchie
spellingShingle Cheng Xue Qin
Lauren T. May
Renming Li
Nga Cao
Sarah Rosli
Minh Deo
Amy E. Alexander
Duncan Horlock
Jane E. Bourke
Yuan H. Yang
Alastair G. Stewart
David M. Kaye
Xiao-Jun Du
Patrick M. Sexton
Arthur Christopoulos
Xiao-Ming Gao
Rebecca H. Ritchie
Small-molecule-biased formyl peptide receptor agonist compound 17b protects against myocardial ischaemia-reperfusion injury in mice
Nature Communications
author_facet Cheng Xue Qin
Lauren T. May
Renming Li
Nga Cao
Sarah Rosli
Minh Deo
Amy E. Alexander
Duncan Horlock
Jane E. Bourke
Yuan H. Yang
Alastair G. Stewart
David M. Kaye
Xiao-Jun Du
Patrick M. Sexton
Arthur Christopoulos
Xiao-Ming Gao
Rebecca H. Ritchie
author_sort Cheng Xue Qin
title Small-molecule-biased formyl peptide receptor agonist compound 17b protects against myocardial ischaemia-reperfusion injury in mice
title_short Small-molecule-biased formyl peptide receptor agonist compound 17b protects against myocardial ischaemia-reperfusion injury in mice
title_full Small-molecule-biased formyl peptide receptor agonist compound 17b protects against myocardial ischaemia-reperfusion injury in mice
title_fullStr Small-molecule-biased formyl peptide receptor agonist compound 17b protects against myocardial ischaemia-reperfusion injury in mice
title_full_unstemmed Small-molecule-biased formyl peptide receptor agonist compound 17b protects against myocardial ischaemia-reperfusion injury in mice
title_sort small-molecule-biased formyl peptide receptor agonist compound 17b protects against myocardial ischaemia-reperfusion injury in mice
publisher Nature Publishing Group
series Nature Communications
issn 2041-1723
publishDate 2017-02-01
description G Protein-Coupled Receptors (GPCRs) can adopt different conformations, each linked to distinct cellular outcomes. Here the authors show that compound 17b, a novel agonist of the GPCR family member FPR, robustly activates cardioprotective but not detrimental FPR signalling, showing beneficial therapeutic effect in a mouse model of cardiac infarction.
url https://doi.org/10.1038/ncomms14232
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