کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2055134 1543806 2013 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Functional expression and characterization of the C. elegans G-protein-coupled FLP-2 Receptor (T19F4.1) in mammalian cells and yeast
موضوعات مرتبط
علوم زیستی و بیوفناوری علوم کشاورزی و بیولوژیک علوم کشاورزی و بیولوژیک (عمومی)
پیش نمایش صفحه اول مقاله
Functional expression and characterization of the C. elegans G-protein-coupled FLP-2 Receptor (T19F4.1) in mammalian cells and yeast
چکیده انگلیسی

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 (∼10 nM EC50) and in yeast (∼100 nM EC50), signaling through a Gqα 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.

Figure optionsDownload as PowerPoint slideHighlights
► Nematode neuropeptide G protein-coupled receptors are good targets for anthelmintic discovery.
► Neuropeptides encoded on the Caenorhabditis elegans flp-2 gene are bioactive in parasite assays.
► The receptor for flp-2 peptides has been functionally expressed in mammalian cells and yeast.
► The recombinant yeast expressing this receptor is the focus of an ongoing drug discovery effort.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: International Journal for Parasitology: Drugs and Drug Resistance - Volume 3, December 2013, Pages 1–7
نویسندگان
, , , , , ,