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Research ArticleArticle

Functional Characterization of Three Mouse Formyl Peptide Receptors

Hui-Qiong He, Dan Liao, Zhen-Guo Wang, Zhong-Li Wang, Hu-Chen Zhou, Ming-Wei Wang and Richard D. Ye
Molecular Pharmacology February 2013, 83 (2) 389-398; DOI: https://doi.org/10.1124/mol.112.081315
Hui-Qiong He
School of Pharmacy, Shanghai Jiao Tong University, Shanghai, P.R. China (H.Q.H., D.L., Z.L.W., H.C.Z., R.D.Y.); Department of Pharmacology, College of Medicine, University of Illinois, Chicago, Illinois (Z.G.W., R.D.Y.); The National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, P.R. China (M.W.W.)
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Dan Liao
School of Pharmacy, Shanghai Jiao Tong University, Shanghai, P.R. China (H.Q.H., D.L., Z.L.W., H.C.Z., R.D.Y.); Department of Pharmacology, College of Medicine, University of Illinois, Chicago, Illinois (Z.G.W., R.D.Y.); The National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, P.R. China (M.W.W.)
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Zhen-Guo Wang
School of Pharmacy, Shanghai Jiao Tong University, Shanghai, P.R. China (H.Q.H., D.L., Z.L.W., H.C.Z., R.D.Y.); Department of Pharmacology, College of Medicine, University of Illinois, Chicago, Illinois (Z.G.W., R.D.Y.); The National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, P.R. China (M.W.W.)
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Zhong-Li Wang
School of Pharmacy, Shanghai Jiao Tong University, Shanghai, P.R. China (H.Q.H., D.L., Z.L.W., H.C.Z., R.D.Y.); Department of Pharmacology, College of Medicine, University of Illinois, Chicago, Illinois (Z.G.W., R.D.Y.); The National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, P.R. China (M.W.W.)
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Hu-Chen Zhou
School of Pharmacy, Shanghai Jiao Tong University, Shanghai, P.R. China (H.Q.H., D.L., Z.L.W., H.C.Z., R.D.Y.); Department of Pharmacology, College of Medicine, University of Illinois, Chicago, Illinois (Z.G.W., R.D.Y.); The National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, P.R. China (M.W.W.)
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Ming-Wei Wang
School of Pharmacy, Shanghai Jiao Tong University, Shanghai, P.R. China (H.Q.H., D.L., Z.L.W., H.C.Z., R.D.Y.); Department of Pharmacology, College of Medicine, University of Illinois, Chicago, Illinois (Z.G.W., R.D.Y.); The National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, P.R. China (M.W.W.)
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Richard D. Ye
School of Pharmacy, Shanghai Jiao Tong University, Shanghai, P.R. China (H.Q.H., D.L., Z.L.W., H.C.Z., R.D.Y.); Department of Pharmacology, College of Medicine, University of Illinois, Chicago, Illinois (Z.G.W., R.D.Y.); The National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, P.R. China (M.W.W.)
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Abstract

The evolutionary relationship and functional correlation between human formyl peptide receptors (FPRs) and their mouse counterparts remain incompletely understood. We examined three members of the mouse formyl peptide receptor subfamily (mFprs) and found that they differ in agonist preference and cellular distributions. When stably expressed in transfected rat basophilic leukemia (RBL-2H3) cells, mFpr1 was readily activated by N-formylated peptides derived from Listeria monocytogenes (fMIVTLF), Staphylococcus aureus (fMIFL), and mitochondria (fMMYALF). In contrast, the Escherichia coli–derived fMLF was 1000-fold less potent. The aforementioned peptides were much less efficacious at mFpr2, which responded better to the synthetic hexapeptide WKYMVm, the synthetic agonists Quin-C1 (a substituted quinazolinone), and compound 43 (a nitrosylated pyrazolone derivative). Saturation binding assays showed that mFpr1 and mFpr2 were expressed at similar levels on the cell surface, although their affinity for N-formyl-Met-Leu-Phe-Ile-Ile-Lys-fluorescein isothiocyanate varied by more than 1000-fold [dissociation constant (Kd) values of 2.8 nM for mFpr1 and 4.8 μM for mFpr2]). Contrary to these receptors, mFpr-rs1 responded poorly to all the previously mentioned peptides that were tested. Fluorescent microscopy revealed an intracellular distribution pattern of mFpr-rs1. On the basis of these results, we conclude that mFpr1 is an ortholog of human FPR1 with certain pharmacologic properties of human FPR2/ALX, whereas mFpr2 has much lower affinity for formyl peptides. The intracellular distribution of mFpr-rs1 suggests an evolutionary correlation with human FPR3.

Footnotes

  • This work was supported in part by National Basic Research Program of China (973 Program) [Grant 2012CB518001] and Chinese Postdoctoral Science Fund [Grant12Z102060002] (H.Q.H.).

  • dx.doi.org/10.1124/mol.112.081315.

  • ↵Embedded ImageThis article has supplemental material available at molpharm.aspetjournals.org.

  • Received July 18, 2012.
  • Accepted November 15, 2012.
  • Copyright © 2013 by The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 83 (2)
Molecular Pharmacology
Vol. 83, Issue 2
1 Feb 2013
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Research ArticleArticle

Functional Characterization of Three Mouse Fprs

Hui-Qiong He, Dan Liao, Zhen-Guo Wang, Zhong-Li Wang, Hu-Chen Zhou, Ming-Wei Wang and Richard D. Ye
Molecular Pharmacology February 1, 2013, 83 (2) 389-398; DOI: https://doi.org/10.1124/mol.112.081315

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Research ArticleArticle

Functional Characterization of Three Mouse Fprs

Hui-Qiong He, Dan Liao, Zhen-Guo Wang, Zhong-Li Wang, Hu-Chen Zhou, Ming-Wei Wang and Richard D. Ye
Molecular Pharmacology February 1, 2013, 83 (2) 389-398; DOI: https://doi.org/10.1124/mol.112.081315
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