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14-September-2008 18:02:43 - bile acid receptor G protein-coupled bile acid receptor 1 Identifiers Symbols GPBAR1; GPCR; BG37; GPCR19; GPR131; M-BAR; MGC40597; TGR5 External IDs OMIM: 610147 MGI: 2653863 HomoloGene: 18125 Gene ontology Molecular function: rhodopsin-like receptor activity receptor activity Cellular component: membrane integral to membrane Biological process: signal transduction G-protein coupled receptor protein signaling pathway RNA expression pattern More reference expression data Orthologs Human Mouse Entrez 151306 227289 Ensembl ENSG00000179921 ENSMUSG00000064272 Uniprot Q8TDU6 Q14AA9 Refseq NM_001077191 mRNA NP_001070659 protein NM_174985 mRNA NP_778150 protein Location Chr 2: 218.83 - 218.84 Mb Chr 1: 74.21 - 74.21 Mb Pubmed search 1 2 The G protein-coupled bile acid receptor is a G-protein coupled receptor which binds bile acids.1 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.23 This gene encodes a member of the G protein-coupled receptor GPCR superfamily. This enzyme 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. Alternative splicing results in multiple transcript variants encoding the same protein.4 References ^ 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. ^ 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. doi:10.1038/nature04330. PMID 16400329. ^ Baxter JD, Webb P 2006. Metabolism: bile acids heat things up. Nature 439 7075: 402-3. doi:10.1038/439402a. PMID 16437098. ^ Entrez Gene: GPBAR1 G protein-coupled bile acid receptor 1. 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. PMID 12044878. 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. 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. 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. 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. doi:10.1038/nature04330. PMID 16400329. 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. External links IUPHAR GPCR Database - Bile acid receptor MeSH GPBAR1+protein,+human v d e Transmembrane receptor: G protein-coupled receptors Class A: Rhodopsin like Adrenergic α1 A, B, D, α2 A, B, C, β1, β2, β3 Eicosanoid CysLT 1, 2, LTB4 1, 2, FPRL1, OXE, Prostaglandin DP, EP 1, 2, 3, 4, PGF, Prostacyclin, Thromboxane Neuropeptide B/W 1, 2, FF 1, 2, S, Y 1, 2, 4, 5 Orphan GPR 1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 79, 82, 83, 84, 85, 87, 88, 92, 101, 103, 119, 120, 132, 135, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 172, 173, 174, 176, 177, 182 Purinergics Adenosine A1, A2a, A2b, A3, P2Y, 1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14 Serotonin all but 5-HT3 5-HT1 A, B, D, E, F, 5-HT2 A, B, C, 5-HT 4, 5A, 6, 7 Other Acetylcholine M1, M2, M3, M4, M5 - Adrenomedullin - Anaphylatoxin C3a, C5a - Angiotensin 1, 2 - Apelin - Bile acid - Bombesin BRS3, GRPR, NMBR - Bradykinin B1, B2 - Cannabinoid CB1, CB2 - Chemokine - Cholecystokinin A, B - Dopamine D1, D2, D3, D4, D5 - EBI2 - Endothelin A, B - Estrogen - Formyl peptide 1, L1, L2 - Free fatty acid 1, 2, 3, 4 - FSH - Galanin 1, 2, 3 - Gonadotropin-releasing hormone 1, 2 - Ghrelin - Histamine H1, H2, H3, H4 - Kisspeptin - Luteinizing hormone/choriogonadotropin - Lysophospholipid 1, 2, 3, 4, 5, 6, 7, 8 - MAS 1, 1L, D, E, F, G, X1, X2, X3, X4 - Melanocortin 1, 2, 3, 4, 5 - MCHR 1, 2 - Melatonin 1A, 1B- Motilin - neuromedin B, U 1, 2 - Neurotensin 1, 2 - Opioid Delta, Kappa, Mu, Nociceptin, but not Sigma - Olfactory - Opsin 3, 4, 5, 1LW, 1MW, 1SW, RGR, RRH - Orexin 1, 2 - Oxytocin - Oxoglutarate - PAF - Prokineticin 1, 2 - Prolactin-releasing peptide - Protease-activated 1, 2, 3, 4 - Relaxin 1, 2, 3, 4 - Somatostatin 1, 2, 3, 4, 5 - SREB - Succinate - TAAR 1, 2, 3, 5, 6, 8, 9 - Tachykinin 1, 2, 3 - Thyrotropin - Thyrotropin-releasing hormone - Urotensin-II - Vasopressin 1A, 1B, 2 Class B: Secretin like Brain-specific angiogenesis inhibitor 1, 2, 3 - Cadherin 1, 2, 3 - Calcitonin - CD97 - Corticotropin-releasing hormone 1, 2 - EMR 1, 2, 3 - Glucagon GR, GIPR, GLP1R, GLP2R - Growth hormone releasing hormone - PACAPR1- GPR 56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 157 - Latrophilin 1, 2, 3, ELTD1 - Parathyroid hormone 1, 2 - Secretin - Vasoactive intestinal peptide 1, 2 Class C: Metabotropic glutamate / pheromone Calcium-sensing receptor - GABA B 1, 2 - Glutamate receptor Metabotropic glutamate 1, 2, 3, 4, 5, 6, 7, 8 - GPRC6A - GPR 156, 158, 179 - RAIG 1, 2, 3, 4 - Taste receptors TAS1R 1, 2, 3 TAS2R 1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 38, 39, 40, 41, 43, 44, 45, 46, 47, 48, 49, 50 Frizzled / Smoothened Frizzled 1, 2, 3, 4, 5, 6, 7, 8, 9, 10 - Smoothened This transmembrane receptor-related article is a stub. This article incorporates text from the United States National Library of Medicine, which is in the public domain. Retrieved from http://en..org/wiki/G_protein-coupled_bile_acid_receptor Categories: Genes on chromosome 2 | Human proteins | Transmembrane receptor stubs | G protein coupled receptorsHidden category: Protein pages needing a picture Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page This page was last modified on 8 July 2008, at 06:23
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