G protein-coupled bile acid receptor

The G protein-coupled bile acid receptor 1 (GPBAR1) also known as G-protein coupled receptor 19 (GPCR19), membrane-type receptor for bile acids (M-BAR) or Takeda G protein-coupled receptor 5 (TGR5) is a protein that in humans is encoded by the GPBAR1 gene.

GPBAR1
Identifiers
Aliases	GPBAR1, BG37, GPCR19, GPR131, M-BAR, TGR5, G protein-coupled bile acid receptor, G protein-coupled bile acid receptor 1
External IDs	OMIM: 610147; MGI: 2653863; HomoloGene: 18125; GeneCards: GPBAR1; OMA:GPBAR1 - orthologs
Gene location (Human) Chr. Chromosome 2 (human) Band 2q35 Start 218,259,496 bp End 218,263,861 bp
Gene location (Mouse) Chr. Chromosome 1 (mouse) Band 1 C3|1 38.53 cM Start 74,317,709 bp End 74,318,783 bp
RNA expression pattern Bgee Human Mouse (ortholog) Top expressed in testicle monocyte granulocyte decidua gallbladder blood subcutaneous adipose tissue apex of heart spleen gastric mucosa Top expressed in blastocyst embryo embryo yolk sac urinary bladder placenta intestine ileum zygote duodenum More reference expression data BioGPS More reference expression data
Gene ontology Molecular function bile acid receptor activity G protein-coupled receptor activity G protein-coupled bile acid receptor activity signal transducer activity Cellular component cytoplasm integral component of membrane plasma membrane membrane Biological process signal transduction cell surface bile acid receptor signaling pathway regulation of bicellular tight junction assembly G protein-coupled receptor signaling pathway Sources:Amigo / QuickGO
Orthologs Species Human Mouse Entrez 151306 227289 Ensembl ENSG00000179921 ENSMUSG00000064272 UniProt Q8TDU6 Q80SS6 RefSeq (mRNA) NM_001077191 NM_001077194 NM_170699 NM_001321950 NM_174985 RefSeq (protein) NP_001070659 NP_001070662 NP_001308879 NP_733800 NP_778150 Location (UCSC) Chr 2: 218.26 – 218.26 Mb Chr 1: 74.32 – 74.32 Mb PubMed search
Wikidata
View/Edit Human View/Edit Mouse

Function

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.

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.

Further reading

• Takeda S, Kadowaki S, Haga T, et al. (2002). "Identification of G protein-coupled receptor genes from the human genome sequence". FEBS Lett. 520 (1–3): 97–101. doi:10.1016/S0014-5793(02)02775-8. PMID 12044878. S2CID 7116392.
• Maruyama T, Miyamoto Y, Nakamura T, et al. (2003). "Identification of membrane-type receptor for bile acids (M-BAR)". Biochem. Biophys. Res. Commun. 298 (5): 714–9. doi:10.1016/S0006-291X(02)02550-0. PMID 12419312.
• Strausberg RL, Feingold EA, Grouse LH, et al. (2003). "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences". Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–903. Bibcode:2002PNAS...9916899M. doi:10.1073/pnas.242603899. PMC 139241. PMID 12477932.
• Kawamata Y, Fujii R, Hosoya M, et al. (2003). "A G protein-coupled receptor responsive to bile acids". J. Biol. Chem. 278 (11): 9435–40. doi:10.1074/jbc.M209706200. PMID 12524422.
• Ota T, Suzuki Y, Nishikawa T, et al. (2004). "Complete sequencing and characterization of 21,243 full-length human cDNAs". Nat. Genet. 36 (1): 40–5. doi:10.1038/ng1285. PMID 14702039.
• Gerhard DS, Wagner L, Feingold EA, et al. (2004). "The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC)". Genome Res. 14 (10B): 2121–7. doi:10.1101/gr.2596504. PMC 528928. PMID 15489334.
• Watanabe M, Houten SM, Mataki C, et al. (2006). "Bile acids induce energy expenditure by promoting intracellular thyroid hormone activation". Nature. 439 (7075): 484–9. Bibcode:2006Natur.439..484W. doi:10.1038/nature04330. PMID 16400329. S2CID 4429032.
• Thomas SM, Bhola NE, Zhang Q, et al. (2007). "Cross-talk between G protein-coupled receptor and epidermal growth factor receptor signaling pathways contributes to growth and invasion of head and neck squamous cell carcinoma". Cancer Res. 66 (24): 11831–9. doi:10.1158/0008-5472.CAN-06-2876. PMID 17178880.
• Yasuda H, Hirata S, Inoue K, et al. (2007). "Involvement of membrane-type bile acid receptor M-BAR/TGR5 in bile acid-induced activation of epidermal growth factor receptor and mitogen-activated protein kinases in gastric carcinoma cells". Biochem. Biophys. Res. Commun. 354 (1): 154–9. doi:10.1016/j.bbrc.2006.12.168. PMID 17214962.
• Keitel V, Reinehr R, Gatsios P, et al. (2007). "The G-protein coupled bile salt receptor TGR5 is expressed in liver sinusoidal endothelial cells". Hepatology. 45 (3): 695–704. doi:10.1002/hep.21458. PMID 17326144. S2CID 24892239.

External links

• "Bile Acid Receptor". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Archived from the original on 2016-03-03. Retrieved 2007-11-01.
• GPBAR1+protein,+human at the U.S. National Library of Medicine Medical Subject Headings (MeSH)

This article incorporates text from the United States National Library of Medicine, which is in the public domain.