Academic literature on the topic 'G protein-coupled bile acid receptor 5'

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Journal articles on the topic "G protein-coupled bile acid receptor 5"

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Sindhu, Thangaraj, and Pappu Srinivasan. "Identification of potential dual agonists of FXR and TGR5 using e-pharmacophore based virtual screening." Molecular BioSystems 11, no. 5 (2015): 1305–18. http://dx.doi.org/10.1039/c5mb00137d.

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Chiang, John Y. L., and Jessica M. Ferrell. "Bile acid receptors FXR and TGR5 signaling in fatty liver diseases and therapy." American Journal of Physiology-Gastrointestinal and Liver Physiology 318, no. 3 (2020): G554—G573. http://dx.doi.org/10.1152/ajpgi.00223.2019.

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Bile acid synthesis is the most significant pathway for catabolism of cholesterol and for maintenance of whole body cholesterol homeostasis. Bile acids are physiological detergents that absorb, distribute, metabolize, and excrete nutrients, drugs, and xenobiotics. Bile acids also are signal molecules and metabolic integrators that activate nuclear farnesoid X receptor (FXR) and membrane Takeda G protein-coupled receptor 5 (TGR5; i.e., G protein-coupled bile acid receptor 1) to regulate glucose, lipid, and energy metabolism. The gut-to-liver axis plays a critical role in the transformation of p
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Chiang, John Y. L., Preeti Pathak, Hailiang Liu, Ajay Donepudi, Jessica Ferrell, and Shannon Boehme. "Intestinal Farnesoid X Receptor and Takeda G Protein Couple Receptor 5 Signaling in Metabolic Regulation." Digestive Diseases 35, no. 3 (2017): 241–45. http://dx.doi.org/10.1159/000450981.

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Bile acids play a critical role in the regulation of glucose, lipid and energy metabolisms by activating the nuclear bile acid receptor farnesoid X receptor (FXR) and membrane G protein-coupled bile acid receptor-1 (aka takeda G protein couple receptor 5, TGR5) signaling. Paradoxical roles of FXR in the regulation of glucose and lipid metabolism and metabolic disorder have been reported recently. The activation or inhibition of intestinal FXR signaling has been shown to improve insulin and glucose sensitivity and energy metabolism to prevent diabetes, obesity and non-alcoholic fatty liver dise
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Lin, Xiulian, Li Xia, Yuanjiao Zhou, et al. "Crosstalk Between Bile Acids and Intestinal Epithelium: Multidimensional Roles of Farnesoid X Receptor and Takeda G Protein Receptor 5." International Journal of Molecular Sciences 26, no. 9 (2025): 4240. https://doi.org/10.3390/ijms26094240.

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Bile acids and their corresponding intestinal epithelial receptors, the farnesoid X receptor (FXR), the G protein-coupled bile acid receptor (TGR5), play crucial roles in the physiological and pathological processes of intestinal epithelial cells. These acids and receptors are involved in the regulation of intestinal absorption, signal transduction, cellular proliferation and repair, cellular senescence, energy metabolism, and the modulation of gut microbiota. A comprehensive literature search was conducted using PubMed, employing keywords such as bile acid, bile acid receptor, FXR (nr1h4), TG
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Farr, Sarah, Bogdan Stankovic, Simon Hoffman, et al. "Bile acid treatment and FXR agonism lower postprandial lipemia in mice." American Journal of Physiology-Gastrointestinal and Liver Physiology 318, no. 4 (2020): G682—G693. http://dx.doi.org/10.1152/ajpgi.00386.2018.

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Postprandial dyslipidemia is a common feature of insulin-resistant states and contributes to increased cardiovascular disease risk. Recently, bile acids have been recognized beyond their emulsification properties as important signaling molecules that promote energy expenditure, improve insulin sensitivity, and lower fasting lipemia. Although bile acid receptors have become novel pharmaceutical targets, their effects on postprandial lipid metabolism remain unclear. Here, we investigated the potential role of bile acids in regulation of postprandial chylomicron production and triglyceride excurs
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Pols, Thijs W. H. "TGR5 in inflammation and cardiovascular disease." Biochemical Society Transactions 42, no. 2 (2014): 244–49. http://dx.doi.org/10.1042/bst20130279.

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TGR5 (Takeda G-protein-coupled receptor 5) [also known as GPBAR1 (G-protein-coupled bile acid receptor 1), M-BAR (membrane-type receptor for bile acids) or GPR131 (G-protein-coupled receptor 131)] is a G-protein-coupled receptor that was discovered as a bile acid receptor. TGR5 has specific roles in several tissues, among which are the regulation of energy expenditure, GLP-1 (glucagon-like peptide 1) secretion and gall bladder filling. An accumulating body of evidence now demonstrates that TGR5 also acts in a number of processes important in inflammation. Most striking in this context are seve
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Gou, Xianmei, Lin Qin, Di Wu, et al. "Research Progress of Takeda G Protein-Coupled Receptor 5 in Metabolic Syndrome." Molecules 28, no. 15 (2023): 5870. http://dx.doi.org/10.3390/molecules28155870.

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Bile acids are acknowledged as signaling molecules involved in metabolic syndrome. The Takeda G protein-coupled receptor 5 (TGR5) functions as a significant bile acid receptor. The accumulated evidence suggests that TGR5 involves lipid homeostasis, glucose metabolism, and inflammation regulation. In line with this, recent preclinical studies also demonstrate that TGR5 plays a significant role in the generation and progression of metabolic syndrome, encompassing type 2 diabetes mellitus, obesity, atherosclerosis, and non-alcoholic fatty liver disease (NAFLD). In this review, we discuss the role
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Hanafi, Noorul Izzati, Anis Syamimi Mohamed, Siti Hamimah Sheikh Abdul Kadir, and Mohd Hafiz Dzarfan Othman. "Overview of Bile Acids Signaling and Perspective on the Signal of Ursodeoxycholic Acid, the Most Hydrophilic Bile Acid, in the Heart." Biomolecules 8, no. 4 (2018): 159. http://dx.doi.org/10.3390/biom8040159.

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Bile acids (BA) are classically known as an important agent in lipid absorption and cholesterol metabolism. Nowadays, their role in glucose regulation and energy homeostasis are widely reported. BAs are involved in various cellular signaling pathways, such as protein kinase cascades, cyclic AMP (cAMP) synthesis, and calcium mobilization. They are ligands for several nuclear hormone receptors, including farnesoid X-receptor (FXR). Recently, BAs have been shown to bind to muscarinic receptor and Takeda G-protein-coupled receptor 5 (TGR5), both G-protein-coupled receptor (GPCR), independent of th
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Slijepcevic, Davor, and Stan F. J. van de Graaf. "Bile Acid Uptake Transporters as Targets for Therapy." Digestive Diseases 35, no. 3 (2017): 251–58. http://dx.doi.org/10.1159/000450983.

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Background: Bile acids are potent signaling molecules that regulate glucose, lipid and energy homeostasis predominantly via the bile acid receptors farnesoid X receptor (FXR) and transmembrane G protein-coupled receptor 5 (TGR5). The sodium taurocholate cotransporting polypeptide (NTCP) and the apical sodium dependent bile acid transporter (ASBT) ensure an effective circulation of (conjugated) bile acids. The modulation of these transport proteins affects bile acid localization, dynamics and signaling. The NTCP-specific pharmacological inhibitor myrcludex B inhibits hepatic uptake of conjugate
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Li, Zhonglin, Hang Yuan, Huikuan Chu, and Ling Yang. "The Crosstalk between Gut Microbiota and Bile Acids Promotes the Development of Non-Alcoholic Fatty Liver Disease." Microorganisms 11, no. 8 (2023): 2059. http://dx.doi.org/10.3390/microorganisms11082059.

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Recently the roles of gut microbiota are highly regarded in the pathogenesis of nonalcoholic fatty liver disease (NAFLD). The intestinal bacteria regulate the metabolism of bile acids depending on bile salt hydrolase (BSH), 7-dehydroxylation, hydroxysteroid dehydrogenase (HSDH), or amide conjugation reaction, thus exerting effects on NAFLD development through bile acid receptors such as farnesoid X receptor (FXR), Takeda G-protein-coupled bile acid protein 5 (TGR5), and vitamin D receptor (VDR), which modulate nutrient metabolism and insulin sensitivity via interacting with downstream molecule
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Dissertations / Theses on the topic "G protein-coupled bile acid receptor 5"

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Prasanna, Kumar Divya. "Regulation of Pancreatic α and β Cell Function by the Bile Acid Receptor TGR5". VCU Scholars Compass, 2014. http://scholarscompass.vcu.edu/etd/3591.

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The discovery that bile acids act as endogenous ligands of the membrane receptor TGR5 and the nuclear receptor FXR increased their significance as regulators of cholesterol, glucose and energy metabolism. Activation of TGR5, expressed on enteroendocrine L cells, by bile acids caused secretion of GLP-1, which stimulates insulin secretion from pancreatic β cells. Expression of TGR5 on pancreatic islet cells and the direct effect of bile acids on the endocrine functions of pancreas, however, are not fully understood. The aim of this study was to identify expression of TGR5 in pancreatic islet cel
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Gertzen, Christoph Gerhard Wilhelm [Verfasser], Holger [Akademischer Betreuer] Gohlke, and Anselmino Verena [Gutachter] Keitel-. "Integrative Modeling to Determine the Activity, Molecular Recognition, and Membrane Trafficking of the G-Protein Coupled Bile Acid Receptor TGR5 / Christoph Gerhard Wilhelm Gertzen ; Gutachter: Verena Keitel- Anselmino ; Betreuer: Holger Gohlke." Düsseldorf : Universitäts- und Landesbibliothek der Heinrich-Heine-Universität Düsseldorf, 2017. http://d-nb.info/1123713170/34.

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Cedernaes, Jonathan. "Intestinal Gene Expression Profiling and Fatty Acid Responses to a High-fat Diet." Doctoral thesis, Uppsala universitet, Funktionell farmakologi, 2013. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-196207.

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The gastrointestinal tract (GIT) regulates nutrient uptake, secretes hormones and has a crucial gut flora and enteric nervous system. Of relevance for these functions are the G protein-coupled receptors (GPCRs) and the solute carriers (SLCs). The Adhesion GPCR subfamily is known to mediate neural development and immune system functioning, whereas SLCs transport e.g. amino acids, fatty acids (FAs) and drugs over membranes. We aimed to comprehensively characterize Adhesion GPCR and SLC gene expression along the rat GIT. Using qPCR we measured expression of 78 SLCs as well as all 30 Adhesion GPCR
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Mohammed, Kader Hamno. "Development of a label-free biosensor method for the identification of sticky compounds which disturb GPCR-assays." Thesis, Uppsala universitet, Institutionen för biologisk grundutbildning, 2013. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-220645.

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It is widely known that early estimates about the binding properties of drug candidates are important in the drug discovery process. Surface plasmon resonance (SPR) biosensors have become a standard tool for characterizing interactions between a great variety of biomolecules and it offers a unique opportunity to study binding activity. The aim of this project was to develop a SPR based assay for pre-screening of low molecular weight (LMW) drug compounds, to enable filtering away disturbing compounds when interacting with drugs. The interaction between 47 LMW compounds and biological ligands we
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Mohib, Mohammad Mohabbulla. "Targeting bile acid-activated receptors for preventing non-alcoholic fatty liver disease progression." Master's thesis, 2018. http://hdl.handle.net/10451/40031.

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Tese de mestrado, Ciências Biofarmacêuticas, Universidade de Lisboa, Faculdade de Farmácia, 2018<br>Non-alcoholic fatty liver disease (NAFLD) comprises a range of liver lesions from simple steatosis to non-alcoholic steatohepatitis (NASH) and remains a major cause of mortality when progressing to cirrhosis and hepatocellular carcinoma (HCC). Although risk factors relate with the metabolic syndrome, the biological mechanisms of disease are not entirely known. Therefore, a better understanding of NAFLD pathogenesis may help finding new treatments for patients with liver damage. In that regard, m
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Book chapters on the topic "G protein-coupled bile acid receptor 5"

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Tobin, Andrew B., Angela Rae,, and David C. Budd. "G protein-coupled receptor phosphorylation and desensitization." In Signal Transduction. Oxford University PressOxford, 1999. http://dx.doi.org/10.1093/oso/9780199637218.003.0004.

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Abstract Phosphorylation of G protein-coupled receptors (GPCRs) has been linked with receptor desensitization, primarily through work on the 13-adrenergic receptor(l-3). Extensive studies have demonstrated that agonist stimulation of the !3-adrenergic receptor results in phosphorylation of the receptor by two kinases; protein kinase A (PKA), and the receptor-specific kinase !3-adrenergic receptor kinase (GRK-2) (1-3). Each of these kinases phosphorylates distinct sites on the receptor. PKA sites are at RRSS motifs in the third intracellular loop and C-terminal tail (4), and GRK-2 sites are in
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Schöneberg, Torsten. "GPCR superfamily and its structural characterization." In Understanding G protein-coupled receptors and their role in the CNS. Oxford University PressOxford, 2002. http://dx.doi.org/10.1093/oso/9780198509165.003.0001.

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Abstract The diversity of receptor groups within the GPCR superfamily is the result of a long evolutionary process. It has been suggested that serotonin (5-HT) receptors have existed for more than 750 million years (Peroutka and Howell 1994). The tendency towards protein diversification depends upon gene duplications and the continuous accumulation of mutations. The maintenance of vital functions in organisms, however, strictly requires enough structural conservation to ensure the functionality of the corresponding proteins. Despite the remarkable structural variety of natural GPCR agonists, h
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Conference papers on the topic "G protein-coupled bile acid receptor 5"

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Ahmed, Sumaya, and Nasser Rizk. "The Expression of Bile Acid Receptor TGR5 in Adipose Tissue in Diet-Induced Obese Mice." In Qatar University Annual Research Forum & Exhibition. Qatar University Press, 2020. http://dx.doi.org/10.29117/quarfe.2020.0212.

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Bile acids are significant physiological factors for digestion, solubilization, absorption, toxic metabolites and xenobiotics. In addition, bile acids are responsible of signal transduction as well as metabolic regulation that activate several receptors such as farnesoid X receptor (FXR) and the membrane G-protein receptor 5 (TGR5). Activation of TGR5 by bile acids is associated with prevention of obesity as well as ameliorating the resistance to insulin via increasing energy expenditure. The objective of this research is to investigate TGR5 gene expression level in different fat depots includ
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Klindt, C., M. Reich, B. Hellweg, et al. "The G protein coupled bile acid receptor TGR5 (Gpbar1) modulates endothelin-1 signaling in liver." In 36. Jahrestagung der Deutschen Arbeitsgemeinschaft zum Studium der Leber. Georg Thieme Verlag KG, 2020. http://dx.doi.org/10.1055/s-0039-3402102.

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Reports on the topic "G protein-coupled bile acid receptor 5"

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Rafaeli, Ada, and Russell Jurenka. Molecular Characterization of PBAN G-protein Coupled Receptors in Moth Pest Species: Design of Antagonists. United States Department of Agriculture, 2012. http://dx.doi.org/10.32747/2012.7593390.bard.

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The proposed research was directed at determining the activation/binding domains and gene regulation of the PBAN-R’s thereby providing information for the design and screening of potential PBAN-R-blockers and to indicate possible ways of preventing the process from proceeding to its completion. Our specific aims included: (1) The identification of the PBAN-R binding domain by a combination of: (a) in silico modeling studies for identifying specific amino-acid side chains that are likely to be involved in binding PBAN with the receptor and; (b) bioassays to verify the modeling studies using mut
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