Biology:G protein-coupled bile acid receptor
 Generic protein structure example |
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 Takeda G protein-coupled receptor 5 (TGR5) as is a protein that in humans is encoded by the GPBAR1 gene.[1][2]
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.[3]
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.[4][5]
References
- ↑ "A G protein-coupled receptor responsive to bile acids". J. Biol. Chem. 278 (11): 9435–40. 2003. doi:10.1074/jbc.M209706200. PMID 12524422.
- ↑ "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. June 2021. doi:10.1016/j.biopsych.2020.11.018. PMID 33536132.
- ↑ "Entrez Gene: GPBAR1 G protein-coupled bile acid receptor 1". https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=151306.
- ↑ "Bile acids induce energy expenditure by promoting intracellular thyroid hormone activation". Nature 439 (7075): 484–9. 2006. doi:10.1038/nature04330. PMID 16400329. Bibcode: 2006Natur.439..484W.
- ↑ "Metabolism: bile acids heat things up". Nature 439 (7075): 402–3. 2006. doi:10.1038/439402a. PMID 16437098. Bibcode: 2006Natur.439..402B.
Further reading
- "Identification of G protein-coupled receptor genes from the human genome sequence.". FEBS Lett. 520 (1–3): 97–101. 2002. doi:10.1016/S0014-5793(02)02775-8. PMID 12044878.
- "Identification of membrane-type receptor for bile acids (M-BAR).". Biochem. Biophys. Res. Commun. 298 (5): 714–9. 2003. doi:10.1016/S0006-291X(02)02550-0. PMID 12419312.
- "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. 2003. doi:10.1073/pnas.242603899. PMID 12477932. Bibcode: 2002PNAS...9916899M.
- "A G protein-coupled receptor responsive to bile acids.". J. Biol. Chem. 278 (11): 9435–40. 2003. doi:10.1074/jbc.M209706200. PMID 12524422.
- "Complete sequencing and characterization of 21,243 full-length human cDNAs.". Nat. Genet. 36 (1): 40–5. 2004. doi:10.1038/ng1285. PMID 14702039.
- "The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC).". Genome Res. 14 (10B): 2121–7. 2004. doi:10.1101/gr.2596504. PMID 15489334.
- "Bile acids induce energy expenditure by promoting intracellular thyroid hormone activation.". Nature 439 (7075): 484–9. 2006. doi:10.1038/nature04330. PMID 16400329. Bibcode: 2006Natur.439..484W.
- "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. 2007. doi:10.1158/0008-5472.CAN-06-2876. PMID 17178880.
- "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. 2007. doi:10.1016/j.bbrc.2006.12.168. PMID 17214962.
- "The G-protein coupled bile salt receptor TGR5 is expressed in liver sinusoidal endothelial cells.". Hepatology 45 (3): 695–704. 2007. doi:10.1002/hep.21458. PMID 17326144.
External links
- "Bile Acid Receptor". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. http://www.iuphar-db.org/GPCR/ChapterMenuForward?chapterID=1332.
- GPBAR1+protein,+human at the US 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.
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