RGD Reference Report - A G protein-coupled receptor responsive to bile acids. - Rat Genome Database

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A G protein-coupled receptor responsive to bile acids.

Authors: Kawamata, Y  Fujii, R  Hosoya, M  Harada, M  Yoshida, H  Miwa, M  Fukusumi, S  Habata, Y  Itoh, T  Shintani, Y  Hinuma, S  Fujisawa, Y  Fujino, M 
Citation: Kawamata Y, etal., J Biol Chem 2003 Mar 14;278(11):9435-40.
RGD ID: 634463
Pubmed: PMID:12524422   (View Abstract at PubMed)
DOI: DOI:10.1074/jbc.M209706200   (Journal Full-text)

So far some nuclear receptors for bile acids have been identified. However, no cell surface receptor for bile acids has yet been reported. We found that a novel G protein-coupled receptor, TGR5, is responsive to bile acids as a cell-surface receptor. Bile acids specifically induced receptor internalization, the activation of extracellular signal-regulated kinase mitogen-activated protein kinase, the increase of guanosine 5'-O-3-thio-triphosphate binding in membrane fractions, and intracellular cAMP production in Chinese hamster ovary cells expressing TGR5. Our quantitative analyses for TGR5 mRNA showed that it was abundantly expressed in monocytes/macrophages in human and rabbit. Treatment with bile acids was found to suppress the functions of rabbit alveolar macrophages including phagocytosis and lipopolysaccharide-stimulated cytokine productions. We prepared a monocytic cell line expressing TGR5 by transfecting a TGR5 cDNA into THP-1 cells that did not express TGR5 originally. Treatment with bile acids suppressed the cytokine productions in the THP-1 cells expressing TGR5, whereas it did not influence those in the original THP-1 cells, suggesting that TGR5 is implicated in the suppression of macrophage functions by bile acids.



Gene Ontology Annotations    Click to see Annotation Detail View

Molecular Function

  
Object SymbolSpeciesTermQualifierEvidenceWithNotesSourceOriginal Reference(s)
Gpbar1RatG protein-coupled receptor activity  IDA  RGD 

Objects Annotated

Genes (Rattus norvegicus)
Gpbar1  (G protein-coupled bile acid receptor 1)

Objects referenced in this article
Gene Gpbar1 G protein-coupled bile acid receptor 1 Mus musculus

Additional Information