GPBAR1 Identifiers Aliases GPBAR1 , BG37, GPCR19, GPR131, M-BAR, TGR5, G protein-coupled bile acid receptor, G protein-coupled bile acid receptor 1External IDs OMIM : 610147 MGI : 2653863 HomoloGene : 18125 GeneCards : GPBAR1 Gene location (Human ) Chr. Chromosome 2 (human) [1] Band 2q35 Start 218,259,496 bp [1] End 218,263,861 bp [1]
Gene location (Mouse ) Chr. Chromosome 1 (mouse)[2] Band 1 C3|1 38.53 cM Start 74,278,550 bp [2] End 74,279,624 bp [2]
Orthologs Species Human Mouse Entrez Ensembl UniProt RefSeq (mRNA) RefSeq (protein) Location (UCSC) Chr 2: 218.26 – 218.26 Mb Chr 1: 74.28 – 74.28 Mb PubMed search[3] [4] Wikidata
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 .[5]
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.[6]
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 .[7] [8]
References [ ]
^ a b c GRCh38: Ensembl release 89: ENSG00000179921 - Ensembl , May 2017
^ a b c GRCm38: Ensembl release 89: ENSMUSG00000064272 - Ensembl , May 2017
^ "Human PubMed Reference:" . National Center for Biotechnology Information, U.S. National Library of Medicine .
^ "Mouse PubMed Reference:" . National Center for Biotechnology Information, U.S. National Library of Medicine .
^ 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 .
^ "Entrez Gene: GPBAR1 G protein-coupled bile acid receptor 1" .
^ 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 .
^ 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. 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.
GPBAR1+protein,+human at the US National Library of Medicine Medical Subject Headings (MeSH)
Cell surface receptor : G protein-coupled receptors
Neurotransmitter
Adrenergic
α1 (A
B
D )
α2 (A
B
C )
β1
β2
β3
Purinergic
Adenosine (A1
A2A
A2B
A3 )
P2Y (1
2
4
5
6
8
9
10
11
12
13
14 )
Serotonin Other
Acetylcholine (M1
M2
M3
M4
M5 )
Dopamine
GHB receptor
Histamine
Melatonin (1A
1B
1C )
TAAR (1
2
5
6
8
9 )
Metabolites and signaling molecules
Eicosanoid
CysLT (1
2 )
LTB4
FPRL1
OXE
Prostaglandin
DP (1
2 ), EP (1
2
3
4 ), FP
Prostacyclin
Thromboxane
Other
Peptide
Miscellaneous
Taste , sweetOther
Calcium-sensing receptor
GABAB (1
2 )
Glutamate receptor (Metabotropic glutamate (1
2
3
4
5
6
7
8 ))
GPRC6A
GPR (156
158
179 )
RAIG (1
2
3
4 )
This article incorporates text from the United States National Library of Medicine , which is in the public domain .