HTS018M - ChemiSCREEN™ FPR1 N-Formylpeptide Receptor Membrane Preparation

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    FPR1 is a Gi-coupled GPCR that binds and is activated by short, N-formyl peptides, such as N-Formyl-Met-Leu-Phe (fMLF). N-formyl peptides are typically derived from bacteria and mediate host recruitment of leukocytes, which highly express FPR1, to sites of bacterial infection (Gao et al., 1999). In addition, FPR1 is expressed in the vasculature, secretory epithelial cells, neurons and other tissues (Becker et al., 1998). Other ligands, such as mitochondrially encoded formyl peptides, amyloid proteins, and virus-derived peptides, have also been found to activate FPR1 and/or related GPCRs and may be important in the pathophysiology of amyloidoses, Alzheimer’s disease and HIV (Le et al., 2002). A synthetic hexapeptide ligand, WKYMVm, has also been demonstrated to bind to FPR1 (Le et al., 1999). The membrane preparations are crude membrane preparations made from our proprietary stable recombinant cell lines to ensure high-level of GPCR surface expression; thus, they are ideal HTS tools for screening of antagonists of FPR1 and its ligands. The membrane preparations exhibit a Kd of 0.39 nM for [125I]-WKYMVm. With 5 mg/well FPR1 Membrane Prep and 0.5 nM [125I]-WKYMVm, a greater than 10-fold signal-to-background is obtained.

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    Item Unit of Measure: EA
    Quantity: 200 units
    Storage: On receipt of material store at -70°C. Unopened reagent is stable for a minimum of 1 year from date of shipment when stored at recommended storage temperature. Avoid repeat freeze/thaw cycles.
    Applications: Radioligand Binding Assay
    Species: Human FPR1 (Accession number M60626)
    Host Cell: Chem-2, a suspension mammalian cell line with no detectable endogenous FPR1 expression.
    Reference 1: 1. Becker EL et al. (1998) Broad immunocytochemical localization of the formylpeptide receptor in human organs, tissues, and cells. Cell Tissue Res. 292: 129-35.
    Reference 2: 2. Gao JL et al. (1999) Impaired antibacterial host defense in mice lacking the N-formylpeptide receptor. J. Exp. Med. 189: 657-62.
    Reference 3: 3. Le Y et al. (2002) Formyl-peptide receptors revisited. Trends Immunol. 23: 541-8.
    Reference 4: 4. Le Y et al. (1999) Utilization of two seven-transmembrane, G protein-coupled receptors, formyl peptide receptor-like 1 and formyl peptide receptor, by the synthetic hexapeptide WKYMVm for human phagocyte activation. J. Immunol. 163: 6777-6784.