Functional expression and characterization of the C. elegans G-protein-coupled FLP-2 Receptor (T19F4.1) in mammalian cells and yeast

被引:12
|
作者
Larsen, Martha J. [1 ]
Lancheros, Elizabeth Ruiz [2 ]
Williams, Tracey [1 ]
Lowery, David E. [1 ]
Geary, Timothy G. [1 ]
Kubiak, Teresa M. [1 ]
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
来源
INTERNATIONAL JOURNAL FOR PARASITOLOGY-DRUGS AND DRUG RESISTANCE | 2013年 / 3卷
关键词
FLP; Caenorhabditis elegans; flp2; Neuropeptide; CAENORHABDITIS-ELEGANS; SACCHAROMYCES-CEREVISIAE; DROSOPHILA-MELANOGASTER; NERVOUS-SYSTEM; GENE FAMILIES; NEUROPEPTIDE; PEPTIDES; IDENTIFICATION; CLONING; NEUROTRANSMITTERS;
D O I
10.1016/j.ijpddr.2012.10.002
中图分类号
R38 [医学寄生虫学]; Q [生物科学];
学科分类号
07 ; 0710 ; 09 ; 100103 ;
摘要
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.
引用
收藏
页码:1 / 7
页数:7
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