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|
|Aliases||hGPCR19, M-BAR, hBG37, BG37, TGR5|
|Organism||Homo sapiens (Human)|
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.
Fig.1 Service of AMSYS - abstract management with a system (Yanguas, 2015)
Application of GPBAR1 Membrane Protein in Literature
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.
This article shows that GPBAR1 agonists improve liver histology in NASH rodent models and promote browning of white adipose tissue.
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.
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.
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
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