Recombinant Mouse G-protein coupled bile acid receptor 1 (Gpbar1)

1. G-protein coupled bile acid receptor 1 (TGR5) is required for cold-induced beiging of subcutaneous white adipose tissue (scWAT). PMID: 29339725
2. Work is the first to provide evidence for a TGR5-inhibited inflammatory response in ischemia/reperfusion injury through suppression of the TLR4-NF-kappaB pathway. PMID: 27597295
3. contributes to hepatic cystogenesis by increasing cAMP and enhancing cholangiocyte proliferation PMID: 28543567
4. findings show GPBAR1 is essential for maintaining intestinal immune homeostasis and that its activation in the setting of inflammation reverses the immune dysfunction that occurs in rodent models of colitis PMID: 28607110
5. Data suggest that FXR and TGR5 expression is down-regulated in aging kidney; caloric restriction prevents these age-related changes. Additionally, in long-lived Ames dwarf mice, renal FXR and TGR5 expression is up-regulated. Treatment of aged mice with dual FXR/TGR5 agonist reverses age-related changes in kidney structure/function. (FXR = farnesoid X activated receptor; TGR5 = G protein-coupled bile acid receptor 1) PMID: 28596381
6. GPBAR1/TGR5 receptor agonist, tauroursodeoxycholic acid, has anti-inflammatory effects in microglial cells. PMID: 27987324
7. Vertical sleeve gastrectomy achieves its postoperative therapeutic effects through enhanced TGR5 signaling. PMID: 27312543
8. These results suggest that TGR5 contributes to the glucoregulatory benefits of vertical sleeve gastrectomy surgery by promoting metabolically favourable shifts in the circulating bile acid pool. PMID: 26511794
9. findings uncovered a novel mechanism in which INT-767 activation of FXR induces Tgr5 gene expression and increases Ca(2+) levels and cAMP activity to stimulate GLP-1 secretion and improve hepatic glucose and lipid metabolism in high-fat diet-induced obese mice. PMID: 28478385
10. The results suggest that TGR5 activation mediates cross-talk between alpha- and beta-cells by switching from glucagon to GLP-1 to restore beta- cell mass and function under hyperglycemic conditions. PMID: 26757816
11. TGR5 is an important mediator of bile acid-induced cholangiocyte proliferation in vivo and in vitro. Furthermore, TGR5 protects cholangiocytes from death receptor-mediated apoptosis. PMID: 26420419
12. miR-26a is a target gene of bile acid receptor GPBAR-1/TGR5 PMID: 26107166
13. Impaired Itching Perception in Murine Models of Cholestasis Is Supported by Dysregulation of GPBAR1 Signaling PMID: 26177448
14. Data show that the action of bile acids on -like peptide-1 (GLP-1) secretion is predominantly mediated by G protein-coupled bile acid receptor GPBAR1 (TGR5) located on the basolateral L-cell membrane. PMID: 26280129
15. TGR5 appears to be crucial for protecting the regenerating liver from bile acid overload. PMID: 26045264
16. Activation of TGR5 alleviates neuroinflammation and improves outcome in hepatic encephalopathy. PMID: 26179031
17. XGB increases BMR by TGR5-dependent mechanisms in mice PMID: 25738495
18. these studies reveal a signaling pathway downstream of TGR5 that modulates chemokine expression in response to high-fat diet PMID: 25365223
19. Bile acids induce pruritus in mice by co-activation of TGR5 and TRPA1. PMID: 25194674
20. TGR5 mediates the bile acid-induced pro-inflammatory cytokine production in murine Kupffer cells. PMID: 24755711
21. TGR5 is a critical element in testicular pathophysiology. PMID: 24798773
22. GPBAR1 is essential to maintain gastric and intestinal mucosal integrity. GPBAR1 agonists protect against gastrointestinal injury caused by ASA and NSAIDs by a COX-independent mechanism. PMID: 22881598
23. Stimulation of GPBAR1 enhances endothelial barrier function via activation of protein kinase A and Rac1. PMID: 24144793
24. The receptor TGR5 protects the liver from bile acid overload during liver regeneration in mice. PMID: 23686672
25. TGR5 agonism induces NO production via Akt activation and intracellular Ca(2+) increase in vascular endothelial cells, and this function inhibits monocyte adhesion in response to inflammatory stimuli. PMID: 23619297
26. FXR/TGR5 activation coordinates the immune phenotype of monocytes and macrophages, both in vitro and in vivo, identifying potential targeting strategies for treatment of NAFLD. PMID: 23460643
27. Bile acids activate TGR5 on sensory nerves, stimulating the release of neuropeptides in the spinal cord that transmit itch and analgesia. PMID: 23524965
28. TGR5 receptor activation on smooth muscle reveals a novel mechanism for the regulation of gut motility by bile acids PMID: 23275618
29. this study demonstrates that the TGR5 expressed in the pancreatic beta cells regulates insulin secretion and highlights the importance of ongoing therapeutic strategies targeting TGR5 in the control of glucose homeostasis. PMID: 23022524
30. The receptor TGR5 mediates the effects of bile acids on colonic motility, and deficiency of TGR5 causes constipation in mice. PMID: 23041323
31. Data suggest that TGR5 represents an essential component in the pathway mediating the enhanced GLP-1 release in response to anionic exchange resins. PMID: 22666533
32. Bile acid binding resin and bile acid have similar effects on bile acid composition and thermogenesis, suggesting that they both are mediated via TGR5 activation PMID: 22952571
33. TGR5 activation yields a significant immune modulating function in the prevention of atherosclerosis. PMID: 22152303
34. GP-BAR1 regulates intestinal barrier structure. Its expression increases in rodent models of colitis and Crohn's disease. Ciprofloxacin is a GP-BAR1 ligand. PMID: 22046243
35. These findings identify TGR5 as a negative mediator of inflammation that may serve as an attractive therapeutic tool for immune and inflammatory liver diseases. PMID: 21735468
36. The G protein-coupled bile acid receptor, TGR5, stimulates gallbladder filling PMID: 21454404
37. Activation of GPBAR1 receptors by hydrophobic bile salts leads to the opening of potassium K(ATP) channels. PMID: 20624794
38. The TGR5 is localized in the primary cilium of mouse cholangiocytes and the receptor could play an important role in coupling biliary bile acid concentration and composition to ductular bile formation. PMID: 20623999
39. Bile acids activate GpBAR1 on inhibitory motor neurons to release nitric oxide and suppress motility PMID: 20236244
40. The discovery of the bile acid receptor, GpBAR1, represented a major step forward in our understanding of how cells can sense and respond to bile acids--{REVIEW} PMID: 20553563
41. There is a gender-dependent regulation of Gpbar1 function in metabolic disease. PMID: 20354075
42. Gpbar1 may play a critical role in the evolution of bile-acid-induced pancreatitis by coupling exposure to bile acids with generation of pathological intracellular calcium transients, intra-acinar cell zymogen activation, and acinar cell injury. PMID: 19900448
43. TGR5 is implicated in the suppression of macrophage functions by bile acids PMID: 12524422
44. bile acids induce GLP-1 secretion through TGR5 and intracellular cAMP production in STC-1 cells PMID: 15721318
45. Gpbar1 plays a critical role in the formation of gallstones, possibly via a regulatory mechanism involving the cholesterol 7alpha-hydroxylase pathway. PMID: 16724960
46. Our data suggest that both oleuropein and oleanolic acid are involved in the anti-diabetic effect of olive leaves and further emphasize the potential role of TGR5 agonists to improve metabolic disorders. PMID: 17825251
47. TGR5 signaling induces intestinal glucagon-like peptide-1 release, leading to improved liver and pancreatic function and enhanced glucose tolerance in obese mice. PMID: 19723493

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KEGG: mmu:227289

STRING: 10090.ENSMUSP00000077135

UniGene: Mm.246587