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The Formyl Peptide Receptors: Diversity of Ligands and Mechanism for Recognition

by Hui-Qiong He 1,2 and Richard D. Ye 2,*
School of Pharmacy, Shanghai Jiao Tong University, Shanghai 200240, China
Institute of Chinese Medical Sciences, University of Macau, Macau SAR 999078, China
Author to whom correspondence should be addressed.
Academic Editor: Yung H. Wong
Molecules 2017, 22(3), 455;
Received: 11 February 2017 / Accepted: 9 March 2017 / Published: 13 March 2017
(This article belongs to the Special Issue G-protein Coupled Receptor Structure and Function)
The formyl peptide receptors (FPRs) are G protein-coupled receptors that transduce chemotactic signals in phagocytes and mediate host-defense as well as inflammatory responses including cell adhesion, directed migration, granule release and superoxide production. In recent years, the cellular distribution and biological functions of FPRs have expanded to include additional roles in homeostasis of organ functions and modulation of inflammation. In a prototype, FPRs recognize peptides containing N-formylated methionine such as those produced in bacteria and mitochondria, thereby serving as pattern recognition receptors. The repertoire of FPR ligands, however, has expanded rapidly to include not only N-formyl peptides from microbes but also non-formyl peptides of microbial and host origins, synthetic small molecules and an eicosanoid. How these chemically diverse ligands are recognized by the three human FPRs (FPR1, FPR2 and FPR3) and their murine equivalents is largely unclear. In the absence of crystal structures for the FPRs, site-directed mutagenesis, computer-aided ligand docking and structural simulation have led to the identification of amino acids within FPR1 and FPR2 that interact with several formyl peptides. This review article summarizes the progress made in the understanding of FPR ligand diversity as well as ligand recognition mechanisms used by these receptors. View Full-Text
Keywords: G protein-coupled receptors; formyl peptides; inflammation; phagocytes G protein-coupled receptors; formyl peptides; inflammation; phagocytes
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He, H.-Q.; Ye, R.D. The Formyl Peptide Receptors: Diversity of Ligands and Mechanism for Recognition. Molecules 2017, 22, 455.

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