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Literature DB >> 16697190

Potent hFPRL1 (ALXR) agonists as potential anti-inflammatory agents.

Roland W Bürli¹, Han Xu, Xiaoming Zou, Kristine Muller, Jennifer Golden, Mike Frohn, Matthew Adlam, Matthew H Plant, Min Wong, Michele McElvain, Kelly Regal, Vellarkad N Viswanadhan, Philip Tagari, Randall Hungate.

Abstract

We report the discovery of potent agonists for the human formyl-peptide-like 1 receptor (hFPRL1). These compounds did not act at a closely related receptor denoted human formyl peptide receptor (hFPR) up to 10 microM concentration. Recent studies have indicated that agonizing this receptor may promote resolution of inflammation. In an exploratory study, a novel hFPRL1 agonist showed efficacy in a mouse ear inflammation model following oral administration.

Entities: Disease Gene Species

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Year: 2006 PMID： 16697190 DOI： 10.1016/j.bmcl.2006.04.068

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

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Cited

45 in total

1. Inhibition of neutrophil migration in mice by mouse formyl peptide receptors 1 and 2 dual agonist: indication of cross-desensitization in vivo.

Authors: Yoshitaka Sogawa; Takao Ohyama; Hiroaki Maeda; Kazuki Hirahara
Journal: Immunology Date: 2010-10-29 Impact factor: 7.397

2. Computational structure-activity relationship analysis of small-molecule agonists for human formyl peptide receptors.

Authors: Andrei I Khlebnikov; Igor A Schepetkin; Mark T Quinn
Journal: Eur J Med Chem Date: 2010-09-15 Impact factor: 6.514

3. Characterization of Quin-C1 for its anti-inflammatory property in a mouse model of bleomycin-induced lung injury.

Authors: Min He; Ni Cheng; Wei-wei Gao; Meng Zhang; Yue-yun Zhang; Richard D Ye; Ming-wei Wang
Journal: Acta Pharmacol Sin Date: 2011-04-18 Impact factor: 6.150

4. 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

10. Identification of novel small-molecule agonists for human formyl peptide receptors and pharmacophore models of their recognition.

Authors: Liliya N Kirpotina; Andrei I Khlebnikov; Igor A Schepetkin; Richard D Ye; Marie-Josèphe Rabiet; Mark A Jutila; Mark T Quinn
Journal: Mol Pharmacol Date: 2009-11-10 Impact factor: 4.436

Potent hFPRL1 (ALXR) agonists as potential anti-inflammatory agents.

1. Inhibition of neutrophil migration in mice by mouse formyl peptide receptors 1 and 2 dual agonist: indication of cross-desensitization in vivo.

2. Computational structure-activity relationship analysis of small-molecule agonists for human formyl peptide receptors.

3. Characterization of Quin-C1 for its anti-inflammatory property in a mouse model of bleomycin-induced lung injury.

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

5. Resolvin D1 binds human phagocytes with evidence for proresolving receptors.

6. Duplex high-throughput flow cytometry screen identifies two novel formylpeptide receptor family probes.

Review 7. Exploiting the Annexin A1 pathway for the development of novel anti-inflammatory therapeutics.

Review 8. Novel anti-inflammatory--pro-resolving mediators and their receptors.

9. Resolvin D1 receptor stereoselectivity and regulation of inflammation and proresolving microRNAs.

10. Identification of novel small-molecule agonists for human formyl peptide receptors and pharmacophore models of their recognition.