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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
13
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pubmed:dateCreated |
2003-3-24
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pubmed:databankReference |
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pubmed:abstractText |
GPR40 is a member of a subfamily of homologous G protein-coupled receptors that include GPR41 and GPR43 and that have no current function or ligand ascribed. Ligand fishing experiments in HEK293 cells expressing human GPR40 revealed that a range of saturated and unsaturated carboxylic acids with carbon chain lengths greater than six were able to induce an elevation of [Ca(2+)](i), measured using a fluorometric imaging plate reader. 5,8,11-Eicosatriynoic acid was the most potent fatty acid tested, with a pEC(50) of 5.7. G protein coupling of GPR40 was examined in Chinese hamster ovary cells expressing the G alpha(q/i)-responsive Gal4-Elk1 reporter system. Expression of human GPR40 led to a constitutive induction of luciferase activity, which was further increased by exposure of the cells to eicosatriynoic acid. Neither the constitutive nor ligand-mediated luciferase induction was inhibited by pertussis toxin treatment, suggesting that GPR40 was coupled to G alpha(q/11.) Expression analysis by quantitative reverse transcription-PCR showed that GPR40 was specifically expressed in brain and pancreas, with expression in rodent pancreas being localized to insulin-producing beta-cells. These data suggest that some of the physiological effects of fatty acids in pancreatic islets and brain may be mediated through a cell-surface receptor.
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pubmed:commentsCorrections |
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Calcium,
http://linkedlifedata.com/resource/pubmed/chemical/DNA Primers,
http://linkedlifedata.com/resource/pubmed/chemical/FFAR1 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Fatty Acids,
http://linkedlifedata.com/resource/pubmed/chemical/Gpr40 protein, mouse,
http://linkedlifedata.com/resource/pubmed/chemical/Luciferases,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Cell Surface,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, G-Protein-Coupled
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
0021-9258
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pubmed:author |
pubmed-author:AndrewsJohn LJL,
pubmed-author:BensonWilliam GWG,
pubmed-author:BriscoeCelia PCP,
pubmed-author:ChambersJon KJK,
pubmed-author:EilertMichelle MMM,
pubmed-author:EllisCatherineC,
pubmed-author:ElshourbagyNabil ANA,
pubmed-author:GoetzAaron SAS,
pubmed-author:IgnarDiane MDM,
pubmed-author:MinnickDana TDT,
pubmed-author:MuirAlison IAI,
pubmed-author:MurdockPaul RPR,
pubmed-author:SaulsHoward RHRJr,
pubmed-author:ShabonUsmanU,
pubmed-author:SpinageLisa DLD,
pubmed-author:StrumJay CJC,
pubmed-author:SzekeresPhilip GPG,
pubmed-author:TadayyonMohammadM,
pubmed-author:TanKong BKB,
pubmed-author:WayJames MJM,
pubmed-author:WilsonShelaghS
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pubmed:issnType |
Print
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pubmed:day |
28
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pubmed:volume |
278
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
11303-11
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pubmed:dateRevised |
2006-5-26
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pubmed:meshHeading |
pubmed-meshheading:12496284-Animals,
pubmed-meshheading:12496284-Base Sequence,
pubmed-meshheading:12496284-Calcium,
pubmed-meshheading:12496284-Cell Line,
pubmed-meshheading:12496284-Cloning, Molecular,
pubmed-meshheading:12496284-Cricetinae,
pubmed-meshheading:12496284-DNA Primers,
pubmed-meshheading:12496284-Fatty Acids,
pubmed-meshheading:12496284-Humans,
pubmed-meshheading:12496284-In Situ Hybridization,
pubmed-meshheading:12496284-Luciferases,
pubmed-meshheading:12496284-Molecular Sequence Data,
pubmed-meshheading:12496284-Receptors, Cell Surface,
pubmed-meshheading:12496284-Receptors, G-Protein-Coupled
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pubmed:year |
2003
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pubmed:articleTitle |
The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids.
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pubmed:affiliation |
Department of Metabolic Diseases, GlaxoSmithKline, Research Triangle Park, North Carolina 27709, USA. cpb15172@gsk.com
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pubmed:publicationType |
Journal Article
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