Open Access Articles- Top Results for G protein-coupled bile acid receptor

G protein-coupled bile acid receptor

SymbolsGPBAR1 ; BG37; GPCR19; GPR131; M-BAR; TGR5
External IDsOMIM610147 MGI2653863 HomoloGene18125 IUPHAR: 37 ChEMBL: 5409 GeneCards: GPBAR1 Gene
RNA expression pattern
File:PBB GE GPBAR1 gnf1h07596 at tn.png
More reference expression data
RefSeq (mRNA)NM_001077191NM_174985
RefSeq (protein)NP_001070659NP_778150
Location (UCSC)Chr 2:
219.12 – 219.13 Mb
Chr 1:
74.28 – 74.28 Mb
PubMed search[1][2]

The G protein-coupled bile acid receptor 1 (GPBAR1) also known G-protein coupled receptor 19 (GPCR19), membrane-type receptor for bile acids (M-BAR) or TGR5 as is a protein that in humans is encoded by the GPBAR1 gene.[1]


This gene encodes a member of the G protein-coupled receptor (GPCR) superfamily. This protein functions as a cell surface receptor for bile acids. Treatment of cells expressing this GPCR with bile acids induces the production of intracellular cAMP, activation of a MAP kinase signaling pathway, and internalization of the receptor. The receptor is implicated in the suppression of macrophage functions and regulation of energy homeostasis by bile acids.[2]

One effect of this receptor is to activate deiodinases which convert the prohormone thyroxine (T4) to the active hormone triiodothyronine (T3). T3 in turn activates the thyroid hormone receptor which increases metabolic rate.[3][4]


  1. ^ 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 (2003). "A G protein-coupled receptor responsive to bile acids". J. Biol. Chem. 278 (11): 9435–40. PMID 12524422. doi:10.1074/jbc.M209706200. 
  2. ^ "Entrez Gene: GPBAR1 G protein-coupled bile acid receptor 1". 
  3. ^ Watanabe M, Houten SM, Mataki C, Christoffolete MA, Kim BW, Sato H, Messaddeq N, Harney JW, Ezaki O, Kodama T, Schoonjans K, Bianco AC, Auwerx J (2006). "Bile acids induce energy expenditure by promoting intracellular thyroid hormone activation". Nature 439 (7075): 484–9. PMID 16400329. doi:10.1038/nature04330. 
  4. ^ Baxter JD, Webb P (2006). "Metabolism: bile acids heat things up". Nature 439 (7075): 402–3. PMID 16437098. doi:10.1038/439402a. 

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