Results 1 to 10 of about 42,926,125 (284)

In Silico Workflow for the Discovery of Natural Products Activating the G Protein-Coupled Bile Acid Receptor 1 [PDF]

Frontiers in Chemistry, 2018
The G protein-coupled bile acid receptor (GPBAR1) has been recognized as a promising new target for the treatment of diverse diseases, including obesity, type 2 diabetes, fatty liver disease and atherosclerosis.
Benjamin Kirchweger, Jadel M. Kratz, Angela Ladurner, Ulrike Grienke, Thierry Langer, Verena M. Dirsch, Judith M. Rollinger   +6 more
doaj   +6 more sources

The G Protein-Coupled Bile Acid Receptor TGR5 (Gpbar1) Modulates Endothelin-1 Signaling in Liver [PDF]

Cells, 2019
TGR5 (Gpbar1) is a G protein-coupled receptor responsive to bile acids (BAs), which is expressed in different non-parenchymal cells of the liver, including biliary epithelial cells, liver-resident macrophages, sinusoidal endothelial cells (LSECs), and ...
Caroline Klindt, Maria Reich, Birte Hellwig, Jan Stindt, Jörg Rahnenführer, Jan G. Hengstler, Karl Köhrer, Kristina Schoonjans, Dieter Häussinger, Verena Keitel   +9 more
doaj   +10 more sources

From Structure to Dynamics: Activation Mechanism of the G Protein-Coupled Bile Acid Receptor 1‑Gs Complex [PDF]

ACS Omega
The G protein-coupled bile acid receptor 1 (GPBAR1, also known as TGR5) is a key mediator of bile acid signaling, exerting its physiological effects through coupling with the stimulatory G protein (Gs). This interaction is essential for stabilizing the receptor's active conformation and triggering downstream signaling.
Bianca Fiorillo, Federica Moraca, Francesco Saverio Di Leva, Valentina Sepe, Stefano Fiorucci, Vittorio Limongelli, Angela Zampella, Bruno Catalanotti   +7 more
doaj   +3 more sources

Evaluation of G-Protein-Coupled Bile Acid Receptor 1 (TGR5) Levels in Intrahepatic Cholestasis of Pregnancy. [PDF]

Cureus, 2021
Background and objective Intrahepatic cholestasis of pregnancy (ICP) is the most common pregnancy-related liver disease. G-protein-coupled bile acid receptor 1 (TGR5) agonists might be beneficial in ICP treatment. In this study, we aimed to investigate the relationship of serum TGR5 levels with ICP and associated itching.
Irak K, Bayram M, Cifci S, Acar Z, Kazezoglu C, Ogutmen Koc D, Arslan O.   +6 more
europepmc   +4 more sources

Chenodeoxycholic acid attenuates high-fat diet-induced obesity and hyperglycemia via the G protein-coupled bile acid receptor 1 and proliferator-activated receptor γ pathway. [PDF]

Exp Ther Med, 2017
G protein-coupled bile acid receptor 1 (TGR5) serves a key function in regulating glycometabolism. TGR5 is highly expressed in the mitochondria of brown adipose tissue (BAT) and downregulates adenosine triphosphate synthesis via the bile acid-TGR5-cyclic adenosine monophosphate-2-iodothyronine deiodinase (D2)-triiodothyronine-uncoupling protein pathway,
Chen X, Yan L, Guo Z, Chen Y, Li M, Huang C, Chen Z, Meng X.   +7 more
europepmc   +4 more sources

G protein-coupled bile acid receptor 1 reduced hepatic immune response and inhibited NFκB, PI3K/AKT, and PKC/P38 MAPK signaling pathway in hybrid grouper. [PDF]

J Anim Sci, 2023
Abstract The mammalian G protein-coupled bile acid receptor 1 (TGR5) is involved in the inflammatory response. However, the functions of TGR5 in the immune response of fish remain unclear. In this study, the full-length sequence of tgr5 from hybrid grouper (Epinephelus fuscoguttatus ♀ × E.
Xu J, Cao J, Tan B, Xie S.
europepmc   +3 more sources

Discovery of ((1,2,4-oxadiazol-5-yl)pyrrolidin-3-yl)ureidyl derivatives as selective non-steroidal agonists of the G-protein coupled bile acid receptor-1. [PDF]

Sci Rep, 2019
AbstractThe G-protein bile acid receptor 1 (GPBAR1) has emerged in the last decade as prominent target for the treatment of metabolic and inflammatory diseases including type 2 diabetes, obesity, and non-alcoholic steatohepatitis. To date numerous bile acid derivatives have been identified as GPBAR1 agonists, however their clinical application is ...
Di Leva FS, Festa C, Carino A, De Marino S, Marchianò S, Di Marino D, Finamore C, Monti MC, Zampella A, Fiorucci S, Limongelli V.   +10 more
europepmc   +8 more sources

Regulation of bile acid receptor activity

Liver Research, 2018
Many receptors can be activated by bile acids (BAs) and their derivatives. These include nuclear receptors farnesoid X receptor (FXR), pregnane X receptor (PXR), and vitamin D receptor (VDR), as well as membrane receptors Takeda G protein receptor 5 ...
Yu-Jui Yvonne Wan, Lili Sheng
doaj   +3 more sources

Mogrol stimulates G-protein-coupled bile acid receptor 1 (GPBAR1/TGR5) and insulin secretion from pancreatic β-cells and alleviates hyperglycemia in mice. [PDF]

Sci Rep
AbstractTarget identification is a crucial step in elucidating the mechanisms by which functional food components exert their functions. Here, we identified the G-protein-coupled bile acid receptor 1 (GPBAR1, also known as TGR5) as a target of the triterpenoid mogrol, a class of aglycone mogroside derivative from Siraitia grosvenorii.
Tanaka C, Harada N, Teraoka Y, Urushizaki H, Shinmori Y, Onishi T, Yotsumoto Y, Ito Y, Kitakaze T, Inui T, Murata Y, Inui H, Yamaji R.   +12 more
europepmc   +4 more sources

Bile acid-axis dysregulation in MASLD/MASH progression: from metabolic mismatch to inflammatory-fibrotic remodeling [PDF]

Frontiers in Medicine
Metabolic dysfunction-associated steatotic liver disease (MASLD) and metabolic dysfunction-associated steatohepatitis (MASH) arise from overlapping metabolic stress, gut-derived inflammatory input, immune activation, and fibrotic remodeling.
Yang Du, Lin Qi, Yunze Shi, Xingyuan Huang, Xiaopei Shi, Mingfeng Liu, Ying Fang, Xiaoyang Hu   +7 more
doaj   +2 more sources