Recombinant Human G-protein coupled bile acid receptor 1 (GPBAR1) Protein

Function

G protein-coupled receptor for bile acid (PubMed:12419312, PubMed:12524422, PubMed:32698187, PubMed:32747649, PubMed:35858343). Bile acid-binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors, such as adenylate cyclase (PubMed:12419312, PubMed:12524422, PubMed:32698187, PubMed:32747649, PubMed:35858343). GPBAR1 is coupled to G(s) G proteins and mediates activation of adenylate cyclase activity (PubMed:12419312, PubMed:12524422, PubMed:32698187, PubMed:32747649, PubMed:35858343). Activated by bile acids, such as lithocholate, deoxycholate, chenodeoxycholate and cholate, in descending order (PubMed:12524422, PubMed:32698187). Apart from their role in lipid dietary absorption and cholesterol catabolism, bile acids act as an important signaling molecule, involved in processes, such as energy expenditure or tissue inflammation (PubMed:26541439). GPBAR1-mediated signaling promotes energy expenditure and adiposity reduction in brown adipose tissue by activating adenylate cyclase, leading to DIO2 activation (By similarity). Involved in bile acid promoted GLP-1 secretion (By similarity)

Subcellular Location

Cell membrane (Multi-pass membrane protein)

Tissue Specificity

Ubiquitously expressed. Expressed at higher level in spleen and placenta. Expressed at lower level in other tissues. In digestive tissues, it is expressed in stomach, duodenum, ileocecum, ileum, jejunum, ascending colon, transverse colon, descending colon, cecum and liver, but not in esophagus and rectum

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• Kawamata Y. et al. A G protein-coupled receptor responsive to bile acids. — J. Biol. Chem. (2003)
• Takeda S. et al. Identification of G protein-coupled receptor genes from the human genome sequence. — FEBS Lett. (2002)
• Ota T. et al. Complete sequencing and characterization of 21,243 full-length human cDNAs. — Nat. Genet. (2004)
• Mural R.J. et al. PubMed: CI-56FT96O07V0QG (JUL-)
• The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). — Genome Res. (2004)
• Perino A. et al. TGR5 and Immunometabolism: Insights from Physiology and Pharmacology. — Trends Pharmacol. Sci. (2015)
• Yang F. et al. Structural basis of GPBAR activation and bile acid recognition. — Nature (2020)