G protein-coupled bile acid receptor

Protein-coding gene in the species Homo sapiens
GPBAR1
Identifiers
AliasesGPBAR1, BG37, GPCR19, GPR131, M-BAR, TGR5, G protein-coupled bile acid receptor, G protein-coupled bile acid receptor 1
External IDsOMIM: 610147; MGI: 2653863; HomoloGene: 18125; GeneCards: GPBAR1; OMA:GPBAR1 - orthologs
Gene location (Human)
Chromosome 2 (human)
Chr.Chromosome 2 (human)[1]
Chromosome 2 (human)
Genomic location for GPBAR1
Genomic location for GPBAR1
Band2q35Start218,259,496 bp[1]
End218,263,861 bp[1]
Gene location (Mouse)
Chromosome 1 (mouse)
Chr.Chromosome 1 (mouse)[2]
Chromosome 1 (mouse)
Genomic location for GPBAR1
Genomic location for GPBAR1
Band1 C3|1 38.53 cMStart74,317,709 bp[2]
End74,318,783 bp[2]
RNA expression pattern
Bgee
HumanMouse (ortholog)
Top expressed in
  • monocyte

  • gallbladder

  • blood

  • subcutaneous adipose tissue

  • spleen

  • gastric mucosa

  • left coronary artery

  • body of stomach

  • right coronary artery

  • fundus
Top expressed in
  • yolk sac

  • urinary bladder

  • placenta

  • blastocyst

  • intestine

  • ileum

  • duodenum

  • colon

  • proximal tubule

  • jejunum
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
SpeciesHumanMouse
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 MbChr 1: 74.32 – 74.32 Mb
PubMed search[3][4]
Wikidata
View/Edit HumanView/Edit Mouse

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.[5][6]

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.[7]

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.[8][9]

References

  1. ^ a b c GRCh38: Ensembl release 89: ENSG00000179921 – Ensembl, May 2017
  2. ^ a b c GRCm38: Ensembl release 89: ENSMUSG00000064272 – Ensembl, May 2017
  3. ^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  4. ^ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  5. ^ 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. doi:10.1074/jbc.M209706200. PMID 12524422.
  6. ^ Wang H, Tan YZ, Mu RH, Tang SS, Liu X, Xing SY, Long Y, Yuan DH, Hong H (June 2021). "Takeda G Protein-Coupled Receptor 5 Modulates Depression-like Behaviors via Hippocampal CA3 Pyramidal Neurons Afferent to Dorsolateral Septum". Biological Psychiatry. 89 (11): 1084–1095. doi:10.1016/j.biopsych.2020.11.018. PMID 33536132. S2CID 227165118.
  7. ^ "Entrez Gene: GPBAR1 G protein-coupled bile acid receptor 1".
  8. ^ 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. Bibcode:2006Natur.439..484W. doi:10.1038/nature04330. PMID 16400329. S2CID 4429032.
  9. ^ Baxter JD, Webb P (2006). "Metabolism: bile acids heat things up". Nature. 439 (7075): 402–3. Bibcode:2006Natur.439..402B. doi:10.1038/439402a. PMID 16437098. S2CID 45562883.

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)
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Neurotransmitter
Adrenergic
Purinergic
Serotonin
Other
Metabolites and
signaling molecules
Eicosanoid
Other
Peptide
Neuropeptide
Other
Miscellaneous
Taste, bitter
Orphan
Other
Adhesion
Orphan
Other
Taste, sweet
Other
Class F: Frizzled & Smoothened
Frizzled
Smoothened

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