Literature DB >> 21486695

Discovery of small molecule human FPR1 receptor antagonists.

John Unitt1, Malbinder Fagura, Tim Phillips, Sarah King, Matthew Perry, Andrew Morley, Cathy MacDonald, Richard Weaver, Jadeen Christie, Simon Barber, Rukhsana Mohammed, Melanie Paul, Andrew Cook, Andrew Baxter.   

Abstract

The identification of two novel series of formyl peptide receptor 1 (FPR1) antagonists are reported, represented by methionine benzimidazole 6 and diamide 7. Both series specifically inhibited the binding of labelled fMLF to hrFPR1 and selectively antagonized FPR1 function in human neutrophils, making them useful in vitro validation tools for the target.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID： 21486695     DOI： 10.1016/j.bmcl.2011.03.049

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  8 in total

1.  Selective agonists and antagonists of formylpeptide receptors: duplex flow cytometry and mixture-based positional scanning libraries.

Authors:  Clemencia Pinilla; Bruce S Edwards; Jon R Appel; Tina Yates-Gibbins; Marc A Giulianotti; Jose L Medina-Franco; Susan M Young; Radleigh G Santos; Larry A Sklar; Richard A Houghten
Journal:  Mol Pharmacol       Date:  2013-06-20       Impact factor: 4.436

2.  Antagonism of human formyl peptide receptor 1 (FPR1) by chromones and related isoflavones.

Authors:  Igor A Schepetkin; Liliya N Kirpotina; Andrei I Khlebnikov; Ni Cheng; Richard D Ye; Mark T Quinn
Journal:  Biochem Pharmacol       Date:  2014-10-17       Impact factor: 5.858

Review 3.  Development of small molecule non-peptide formyl peptide receptor (FPR) ligands and molecular modeling of their recognition.

Authors:  I A Schepetkin; A I Khlebnikov; M P Giovannoni; L N Kirpotina; A Cilibrizzi; M T Quinn
Journal:  Curr Med Chem       Date:  2014       Impact factor: 4.530

4.  Novel 3-(1H-indol-3-yl)-2-[3-(4-methoxyphenyl)ureido]propanamides as selective agonists of human formyl-peptide receptor 2.

Authors:  Enza Lacivita; Igor A Schepetkin; Madia L Stama; Liliya N Kirpotina; Nicola A Colabufo; Roberto Perrone; Andrei I Khlebnikov; Mark T Quinn; Marcello Leopoldo
Journal:  Bioorg Med Chem       Date:  2014-12-13       Impact factor: 3.641

Review 5.  Antagonism of human formyl peptide receptor 1 with natural compounds and their synthetic derivatives.

Authors:  Igor A Schepetkin; Andrei I Khlebnikov; Liliya N Kirpotina; Mark T Quinn
Journal:  Int Immunopharmacol       Date:  2015-09-15       Impact factor: 4.932

6.  Aurantiamide-related dipeptide derivatives are formyl peptide receptor 1 antagonists.

Authors:  Margherita Mastromarino; Liliya N Kirpotina; Igor A Schepetkin; Mark T Quinn; Enza Lacivita; Marcello Leopoldo
Journal:  Medchemcomm       Date:  2019-10-07       Impact factor: 3.597

Review 7.  The role of formylated peptides and formyl peptide receptor 1 in governing neutrophil function during acute inflammation.

Authors:  David A Dorward; Christopher D Lucas; Gavin B Chapman; Christopher Haslett; Kevin Dhaliwal; Adriano G Rossi
Journal:  Am J Pathol       Date:  2015-03-17       Impact factor: 4.307

Review 8.  Annexin-A1: The culprit or the solution?

Authors:  Lauren Kelly; Sarah McGrath; Lewis Rodgers; Kathryn McCall; Aysin Tulunay Virlan; Fiona Dempsey; Scott Crichton; Carl S Goodyear
Journal:  Immunology       Date:  2022-03-01       Impact factor: 7.215
  8 in total

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