Functional expression and characterization of the C. elegans G-protein-coupled FLP-2 Receptor (T19F4.1) in mammalian cells and yeast
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作者:
Larsen, Martha J.
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Pfizer Anim Hlth Discovery Res, Vet Med Discovery Res, Kalamazoo, MI 49001 USAPfizer Anim Hlth Discovery Res, Vet Med Discovery Res, Kalamazoo, MI 49001 USA
Larsen, Martha J.
[1
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Lancheros, Elizabeth Ruiz
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McGill Univ, Inst Parasitol, Ste Anne De Bellevue, PQ H9X 3V9, CanadaPfizer Anim Hlth Discovery Res, Vet Med Discovery Res, Kalamazoo, MI 49001 USA
Lancheros, Elizabeth Ruiz
[2
]
Williams, Tracey
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Pfizer Anim Hlth Discovery Res, Vet Med Discovery Res, Kalamazoo, MI 49001 USAPfizer Anim Hlth Discovery Res, Vet Med Discovery Res, Kalamazoo, MI 49001 USA
Williams, Tracey
[1
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Lowery, David E.
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Pfizer Anim Hlth Discovery Res, Vet Med Discovery Res, Kalamazoo, MI 49001 USAPfizer Anim Hlth Discovery Res, Vet Med Discovery Res, Kalamazoo, MI 49001 USA
Lowery, David E.
[1
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Geary, Timothy G.
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Pfizer Anim Hlth Discovery Res, Vet Med Discovery Res, Kalamazoo, MI 49001 USAPfizer Anim Hlth Discovery Res, Vet Med Discovery Res, Kalamazoo, MI 49001 USA
Geary, Timothy G.
[1
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Kubiak, Teresa M.
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Pfizer Anim Hlth Discovery Res, Vet Med Discovery Res, Kalamazoo, MI 49001 USAPfizer Anim Hlth Discovery Res, Vet Med Discovery Res, Kalamazoo, MI 49001 USA
Kubiak, Teresa M.
[1
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机构:
[1] Pfizer Anim Hlth Discovery Res, Vet Med Discovery Res, Kalamazoo, MI 49001 USA
[2] McGill Univ, Inst Parasitol, Ste Anne De Bellevue, PQ H9X 3V9, Canada
Profound neuropeptide diversity characterizes the nematode nervous system, but it has proven challenging to match neuropeptide G protein-coupled receptors (GPCR) with their cognate ligands in heterologous systems. We have expressed the Caenorhabditis elegans GPCR encoded in the locus T19F4.1, previously matched with FMRFamide-like peptides encoded on the flp-2 precursor gene, in mammalian cells and in the yeast Saccharomyces cerevisiae. Pharmacological characterization revealed that the receptor is potently activated by flp-2 peptides in CHO cells (similar to 10 nM EC50) and in yeast (similar to 100 nM EC50), signaling through a G(q)alpha pathway in each system. The yeast GPCR expression system provides a robust assay for screening for agonists of the flp-2 receptor and is the target of an ongoing high-throughput screening exercise. (C) 2012 Australian Society for Parasitology. Published by Elsevier Ltd. All rights reserved.