GPBAR1 Membrane Protein Introduction

Introduction of GPBAR1

The G-protein coupled bile acid receptor 1 (GPBAR1) is a protein encoded by the GPBAR1 gene. It is a G-protein coupled receptor that is activated by certain bile acids and plays an important role in the regulation of bile acid synthesis, lipid metabolism, and energy homeostasis. This receptor involves the inhibition of macrophage function and the regulation of energy balance by bile acids.

Basic Information of GPBAR1
Protein Name	G-protein coupled bile acid receptor 1
Gene Name	GPBAR1
Aliases	hGPCR19, M-BAR, hBG37, BG37, TGR5
Organism	Homo sapiens (Human)
UniProt ID	Q8TDU6
Transmembrane Times	7
Length (aa)	330
Sequence	MTPNSTGEVPSPIPKGALGLSLALASLIITANLLLALGIAWDRRLRSPPAGCFFLSLLLAGLLT GLALPTLPGLWNQSRRGYWSCLLVYLAPNFSFLSLLANLLLVHGERYMAVLRPLQPPGSIRLAL LLTWAGPLLFASLPALGWNHWTPGANCSSQAIFPAPYLYLEVYGLLLPAVGAAAFLSVRVLATA HRQLQDICRLERAVCRDEPSALARALTWRQARAQAGAMLLFGLCWGPYVATLLLSVLAYEQRPP LGPGTLLSLLSLGSASAAAVPVAMGLGDQRYTAPWRAAAQRCLQGLWGRASRDSPGPSIAYHPS SQSSVDLDLN

Function of GPBAR1 Membrane Protein

GPBAR1 (also known as TGR5) is a bile acid activated receptor expressed in several adenocarcinomas that increases intestinal cell proliferation through secondary bile acid activation. The binding of bile acids to GPBAR1 induces the production of intracellular cAMP, the activation of MAP kinase signaling pathways and the internalization of receptors. This receptor is involved in the inhibition of macrophage function and lipid metabolism and the regulation of energy balance by bile acids. In addition, one of the effects of this receptor is to activate a deiodinase that converts prohormone thyroxine (T4) to the active hormone triiodothyronine (T3). T3 activates thyroid hormone receptors in turn, increasing the metabolic rate.

GPBAR1 Membrane Protein Introduction Fig.1 Service of AMSYS - abstract management with a system (Yanguas, 2015)

Application of GPBAR1 Membrane Protein in Literature

Sabrina Cipriani., et al. Activation of the bile acid receptor GPBAR1 protects against gastrointestinal injury caused by nonsteroidal anti-inflammatory drugs and aspirin in mice. Br J Pharmacol. 2013, 168(1): 225-237. PubMed ID: 22881598

This article reports that GPBAR1 is important for maintaining gastric mucosal and intestinal mucosal integrity and that GPBAR1 agonists protect gastrointestinal and NSAID-induced gastrointestinal damage through a COX-independent mechanism.
Adriana Carino., et al. Gpbar1 agonism promotes a Pgc-1α-dependent browning of white adipose tissue and energy expenditure and reverses diet-induced steatohepatitis in mice. Sci Rep. 2017. PubMed ID: 29057935

This article shows that GPBAR1 agonists improve liver histology in NASH rodent models and promote browning of white adipose tissue.
Lewis N.D., et al. A GPBAR1 (TGR5) Small Molecule Agonist Shows Specific Inhibitory Effects on Myeloid Cell Activation In Vitro and Reduces Experimental Autoimmune Encephalitis (EAE) In Vivo. PLoS One. 2014, 9(6): e100883. PubMed ID: 24967665

The article reveals that GPBAR1 is important for the control of monocyte and macrophage activation in vivo and can be used to treat inflammatory diseases.
Roed S.N., et al. Functional Consequences of Glucagon-like Peptide-1 Receptor Cross-talk and Trafficking. J Biol Chem. 2015, 290(2): 1233-43. PubMed ID: 25451942

This article shows that selective GPBAR1 activation produces a strong secretory effect on L cells, and suggests that GPBAR1 is a key player in the intestinal proximal-distal loop that mediates the early phase of nutrient-evoked L-cell secretion effects.
Carino A., et al. The bile acid receptor GPBAR1 (TGR5) is expressed in human gastric cancers and promotes epithelial-mesenchymal transition in gastric cancer cell lines. Oncotarget. 2016, 7(38): 61021. PubMed ID: 27409173

This article evaluates that GPBAR1 is expressed in advanced gastric cancer, and activation of GPBAR1 promotes EMT, so GPBAR1 antagonists may be useful for the treatment of gastric cancer.

GPBAR1 Preparation Options

To obtain the soluble and functional target protein, the versatile Magic™ membrane protein production platform in Creative Biolabs enables many flexible options, from which you can always find a better match for your particular project. Aided by our versatile Magic™ anti-membrane protein antibody discovery platform, we also provide customized anti-GPBAR1 antibody development services.

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Reference

Casás N Y,et al. (2015). Tudca skews microglia towards m2 phenotype through the g-protein coupled bile acid receptor gpbar1/tgr5.

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