scholarly journals The Major Leukocyte Chemotactic and Activating Factors in the Mouse Gut Lumen Are Not N-Formylpeptide Receptor 1 Agonists

2013 ◽  
Vol 5 (1) ◽  
pp. 2-14 ◽  
Author(s):  
Teresa Ojode ◽  
Erich H. Schneider ◽  
H. Lee Tiffany ◽  
Sunny Yung ◽  
Ji-Liang Gao ◽  
...  
Keyword(s):  
Formylpeptide Receptor

Differential Expansion of the N-Formylpeptide Receptor Gene Cluster in Human and Mouse

Genomics ◽  
1998 ◽  
Vol 51 (2) ◽  
pp. 270-276 ◽  
Author(s):  
Ji-Liang Gao ◽  
Hubert Chen ◽  
Jane D. Filie ◽  
Christine A. Kozak ◽  
Philip M. Murphy
Keyword(s):  
Gene Cluster ◽  
Receptor Gene ◽  
Differential Expansion ◽  
Human And Mouse ◽  
Formylpeptide Receptor

scholarly journals Humanin, a Newly Identified Neuroprotective Factor, Uses the G Protein-Coupled Formylpeptide Receptor-Like-1 as a Functional Receptor

2004 ◽  
Vol 172 (11) ◽  
pp. 7078-7085 ◽  
Author(s):  
Guoguang Ying ◽  
Pablo Iribarren ◽  
Ye Zhou ◽  
Wanghua Gong ◽  
Ning Zhang ◽  
...  
Keyword(s):  
G Protein ◽  
G Protein Coupled ◽  
Functional Receptor ◽  
Formylpeptide Receptor

scholarly journals Impaired Antibacterial Host Defense in Mice Lacking the N-formylpeptide Receptor

1999 ◽  
Vol 189 (4) ◽  
pp. 657-662 ◽  
Author(s):  
Ji-Liang Gao ◽  
Eric J. Lee ◽  
Philip M. Murphy
Keyword(s):  
Host Defense ◽  
Bacterial Load ◽  
Direct Proof ◽  
Specific Cellular Immune Response ◽  
Specific Receptors ◽  
Cellular Immune ◽  
Antibacterial Host Defense ◽  
Formylpeptide Receptor

N-formylpeptides derive from bacterial and mitochondrial proteins, and bind to specific receptors on mammalian phagocytes. Since binding induces chemotaxis and activation of phagocytes in vitro, it has been postulated that N-formylpeptide receptor signaling in vivo may be important in antimicrobial host defense, although direct proof has been lacking. Here we test this hypothesis in mice lacking the high affinity N-formylpeptide receptor (FPR), created by targeted gene disruption. FPR−/− mice developed normally, but had increased susceptibility to challenge with Listeria monocytogenes, as measured by increased mortality compared with wild-type littermates. FPR−/− mice also had increased bacterial load in spleen and liver 2 d after infection, which is before development of a specific cellular immune response, suggesting a defect in innate immunity. Consistent with this, neutrophil chemotaxis in vitro and neutrophil mobilization into peripheral blood in vivo in response to the prototype N-formylpeptide fMLF (formyl-methionyl-leucyl-phenylalanine) were both absent in FPR−/− mice. These results indicate that FPR functions in antibacterial host defense in vivo.

Biomolecular screening of formylpeptide receptor ligands with a sensitive, quantitative, high-throughput flow cytometry platform

2006 ◽  
Vol 1 (1) ◽  
pp. 59-66 ◽  
Author(s):  
Bruce S Edwards ◽  
Susan M Young ◽  
Tudor I Oprea ◽  
Cristian G Bologa ◽  
Eric R Prossnitz ◽  
...  
Keyword(s):  
Flow Cytometry ◽  
High Throughput ◽  
Receptor Ligands ◽  
Formylpeptide Receptor

High-Throughput Screening with HyperCyt® Flow Cytometry to Detect Small Molecule Formylpeptide Receptor Ligands

2005 ◽  
Vol 10 (4) ◽  
pp. 374-382 ◽  
Author(s):  
Susan M. Young ◽  
Cristian Bologa ◽  
Eric R. Prossnitz ◽  
Tudor I. Oprea ◽  
Larry A. Sklar ◽  
...  
Keyword(s):  
Flow Cytometry ◽  
High Throughput ◽  
High Throughput Screening ◽  
Receptor Ligands ◽  
Chemical Library ◽  
Assay Sensitivity ◽  
Compound Libraries ◽  
Analysis System ◽  
G Protein Coupled ◽  
Formylpeptide Receptor

High-throughput flow cytometry (HTFC), enabled by faster automated sample processing, represents a promising high- content approach for compound library screening. HyperCyt® is a recently developed automated HTFC analysis system by which cell samples are rapidly aspirated from microplate wells and delivered to the flow cytometer. The formylpeptide receptor (FPR) family of G protein–coupled receptors contributes to the localization and activation of tissue-damaging leukocytes at sites of chronic inflammation. Here, the authors describe development and application of an HTFC screening approach to detect potential anti-inflammatory compounds that block ligand binding to FPR. Using a homogeneous no-wash assay, samples were routinely processed at 1.5 s/well (~2500 cells analyzed/sample), allowing a 96-well plate to be processed in less than 2.5 min. Assay sensitivity and accuracy were validated by detection of a previously documented active compound with relatively low FPR affinity (sulfinpyrazone, inhibition constant [Ki]=14 μM) from among a collection of 880 compounds in the Prestwick Chemical Library. The HyperCyt® system was therefore demonstrated to be a robust, sensitive, and highly quantitative method with which to screen lead compound libraries in a 96-well format.

Conformational Aspects of Human Formylpeptide Receptor Antagonists

2011 ◽  
Vol 49 (10) ◽  
pp. 873-877
Author(s):  
Angelo Scatturin ◽  
Vertuani Gianni ◽  
Rita Pecoraro ◽  
Alessandro Dalpiaz ◽  
Marisa Boggian ◽  
...  
Keyword(s):  
Receptor Antagonists ◽  
Formylpeptide Receptor
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