Bile-acid-activated receptors: targeting TGR5 and farnesoid-X-receptor in lipid and glucose disorders

scientific article

Bile-acid-activated receptors: targeting TGR5 and farnesoid-X-receptor in lipid and glucose disorders is …
instance of (P31):
scholarly articleQ13442814
review articleQ7318358

External links are
P356DOI10.1016/J.TIPS.2009.08.001
P3181OpenCitations bibliographic resource ID230659
P698PubMed publication ID19758712

P50authorSabrina CiprianiQ114572169
P2093author name stringAndrea Mencarelli
Giuseppe Palladino
Stefano Fiorucci
P433issue11
P407language of work or nameEnglishQ1860
P921main subjectglucoseQ37525
P304page(s)570-80
P577publication date2009-11-01
P1433published inTrends in Pharmacological SciencesQ2451474
P1476titleBile-acid-activated receptors: targeting TGR5 and farnesoid-X-receptor in lipid and glucose disorders
P478volume30

Reverse relations

cites work (P2860)
Q35109579A dysregulated acetyl/SUMO switch of FXR promotes hepatic inflammation in obesity.
Q41928187A large-scale, multi-center serum metabolite biomarkers identification study for the early detection of hepatocellular carcinoma.
Q92076849AKR1D1 is a novel regulator of metabolic phenotype in human hepatocytes and is dysregulated in non-alcoholic fatty liver disease
Q64261592Acarbose improves health and lifespan in aging HET3 mice
Q90307736An Untargeted Metabolomics Approach to Investigate the Metabolic Effect of Beetroot Juice Supplementation in Fencers-A Preliminary Study
Q35965157Associations between maternal lipid profile and pregnancy complications and perinatal outcomes: a population-based study from China
Q41996948BAR502, a dual FXR and GPBAR1 agonist, promotes browning of white adipose tissue and reverses liver steatosis and fibrosis
Q36607910Bile Acid Receptors and Liver Cancer
Q43620015Bile acid TUDCA improves insulin clearance by increasing the expression of insulin-degrading enzyme in the liver of obese mice
Q38364542Bile acid activated receptors are targets for regulation of integrity of gastrointestinal mucosa
Q28085493Bile acid nuclear receptor FXR and digestive system diseases
Q36796803Bile acid receptor activation modulates hepatic monocyte activity and improves nonalcoholic fatty liver disease.
Q35976675Bile acids acutely stimulate insulin secretion of mouse β-cells via farnesoid X receptor activation and K(ATP) channel inhibition
Q53192870Bile acids induce monocyte differentiation toward interleukin-12 hypo-producing dendritic cells via a TGR5-dependent pathway.
Q35703158Bile diversion to the distal small intestine has comparable metabolic benefits to bariatric surgery.
Q57114151Bile diversion, a bariatric surgery, and bile acid signaling reduce central cocaine reward
Q61829990Biological processes and signal transduction pathways regulated by the protein methyltransferase SETD7 and their significance in cancer
Q53065775Bone Marrow Cell Transplant From Donors With Cardiovascular Risk Factors Increases the Pro-atherosclerotic Phenotype in the Recipients.
Q93092528Bridging intestinal immunity and gut microbiota by metabolites
Q37004159C/EBPβ in bone marrow is essential for diet induced inflammation, cholesterol balance, and atherosclerosis
Q50962482Cholestyramine alters bile acid amounts and the expression of cholesterol-related genes in rabbit intestinal and hepatic tissues.
Q64917645Combined obeticholic acid and elafibranor treatment promotes additive liver histological improvements in a diet-induced ob/ob mouse model of biopsy-confirmed NASH.
Q33578547Commensal bacteria at the interface of host metabolism and the immune system
Q38186099Critical review of non-statin treatments for dyslipoproteinemia.
Q38986670Decoding the vasoregulatory activities of bile acid-activated receptors in systemic and portal circulation: role of gaseous mediators
Q39005761Design, Synthesis, and Biological Evaluation of Novel Nonsteroidal Farnesoid X Receptor (FXR) Antagonists: Molecular Basis of FXR Antagonism.
Q92461347Detection of Secondary Metabolites as Biomarkers for the Early Diagnosis and Prevention of Type 2 Diabetes
Q34729209Development of time resolved fluorescence resonance energy transfer-based assay for FXR antagonist discovery
Q28114796Diacylglycerol kinase θ couples farnesoid X receptor-dependent bile acid signalling to Akt activation and glucose homoeostasis in hepatocytes
Q37699321Digestive physiology of the pig symposium: intestinal bile acid sensing is linked to key endocrine and metabolic signaling pathways
Q64121752Discovery 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
Q27309876Discovery that theonellasterol a marine sponge sterol is a highly selective FXR antagonist that protects against liver injury in cholestasis
Q35208562Effect of Roux-en-Y gastric bypass surgery on bile acid metabolism in normal and obese diabetic rats
Q36293600Effect of tight glucose control with insulin on the thyroid axis of critically ill children and its relation with outcome
Q48247400Effects of Bariatric Surgery on Serum Bile Acid Composition and Conjugation in a Diabetic Rat Model.
Q48140222Effects of Sleeve Gastrectomy on Serum 12α-Hydroxylated Bile Acids in a Diabetic Rat Model.
Q34168512Effects of deoxycholylglycine, a conjugated secondary bile acid, on myogenic tone and agonist-induced contraction in rat resistance arteries
Q51265948Efficacy of docosahexaenoic acid-choline-vitamin E in paediatric NASH: a randomized controlled clinical trial.
Q39390970Endocrine Function after Bariatric Surgery
Q57123300Enterobacteria Modulate Intestinal Bile Acid Transport and Homeostasis through Apical Sodium-Dependent Bile Acid Transporter (SLC10A2) Expression
Q38009566Epigenomic regulation of bile acid metabolism: emerging role of transcriptional cofactors
Q58861672Epoxide functionalization on cholane side chains in the identification of G-protein coupled bile acid receptor (GPBAR1) selective agonists
Q38548688Farnesoid X receptor modulators (2011 - 2014): a patent review
Q90136397Fecal medicines used in traditional medical system of China: a systematic review of their names, original species, traditional uses, and modern investigations
Q90012752Free fatty acid receptors, G protein-coupled receptor 120 and G protein-coupled receptor 40, are essential for oil-induced gastric inhibitory polypeptide secretion
Q98952094Gut microbiota in human metabolic health and disease
Q35733648Gut permeability, its interaction with gut microflora and effects on metabolic health are mediated by the lymphatics system, liver and bile acid.
Q37590250HDL and cholesterol: life after the divorce?
Q90296417Hepatic Autophagy Deficiency Compromises Farnesoid X Receptor Functionality and Causes Cholestatic Injury
Q37707412High-density lipoproteins and cardiovascular disease: 2010 update
Q64940064Human-specific dual regulations of FXR-activation for reduction of fatty liver using in vitro cell culture model.
Q38291812IFN-γ secretion in gut of Ob/Ob mice after vertical sleeve gastrectomy and its function in weight loss mechanism
Q38897837Identification of potential dual agonists of FXR and TGR5 using e-pharmacophore based virtual screening
Q35819570Impact of Gut Microbiota on Obesity, Diabetes, and Cardiovascular Disease Risk
Q35855133Impaired Itching Perception in Murine Models of Cholestasis Is Supported by Dysregulation of GPBAR1 Signaling
Q28070321Improved glucose metabolism following bariatric surgery is associated with increased circulating bile acid concentrations and remodeling of the gut microbiome
Q55226284In Vitro Modeling of Bile Acid Processing by the Human Fecal Microbiota.
Q26752511Inflammation Meets Metabolic Disease: Gut Feeling Mediated by GLP-1
Q43102009Insights on FXR selective modulation. Speculation on bile acid chemical space in the discovery of potent and selective agonists.
Q37206952Insulin Resistance is Associated With Total Bile Acid Level in Type 2 Diabetic and Nondiabetic Population: A Cross-Sectional Study
Q37429742Intercellular Lipid Mediators and GPCR Drug Discovery
Q35904758Intestinal microbiome is related to lifetime antibiotic use in Finnish pre-school children
Q35234322Intrafollicular cortisol levels inversely correlate with cumulus cell lipid content as a possible energy source during oocyte meiotic resumption in women undergoing ovarian stimulation for in vitro fertilization
Q64084645Introduction of Nonacidic Side Chains on 6-Ethylcholane Scaffolds in the Identification of Potent Bile Acid Receptor Agonists with Improved Pharmacokinetic Properties
Q82486866Long distance calling for liver regeneration: Identification of neuroendocrine signalling pathways activated after partial hepatectomy
Q26770832Medicinal Plants Qua Glucagon-Like Peptide-1 Secretagogue via Intestinal Nutrient Sensors
Q49394966Metabolic and hepatic effects of liraglutide, obeticholic acid and elafibranor in diet-induced obese mouse models of biopsy-confirmed nonalcoholic steatohepatitis
Q97643856Microbial regulation of organismal energy homeostasis
Q42672574Molecular characterization, tissue expression profile and SNP analysis of the porcine NR1H4 gene
Q28831219Navigation in bile acid chemical space: discovery of novel FXR and GPBAR1 ligands
Q60934128Overview of Bile Acids Signaling and Perspective on the Signal of Ursodeoxycholic Acid, the Most Hydrophilic Bile Acid, in the Heart
Q34901544Peripheral reduction of FGFR4 with antisense oligonucleotides increases metabolic rate and lowers adiposity in diet-induced obese mice
Q60047622Pharmacological Applications of Bile Acids and Their Derivatives in the Treatment of Metabolic Syndrome
Q51717906Pharmacophore modeling, comprehensive 3D-QSAR, and binding mode analysis of TGR5 agonists.
Q34054283Pharmacophore-based discovery of FXR agonists. Part I: Model development and experimental validation
Q43503691Positive regulation of osteogenesis by bile acid through FXR.
Q42518451Postprandial gut hormone responses and glucose metabolism in cholecystectomized patients
Q48177243Potential Applications of Gliclazide in Treating Type 1 Diabetes Mellitus: Formulation with Bile Acids and Probiotics.
Q36972583Quantitative high-throughput profiling of environmental chemicals and drugs that modulate farnesoid X receptor
Q44964426Rectal taurocholate increases L cell and insulin secretion, and decreases blood glucose and food intake in obese type 2 diabetic volunteers
Q34694229Regulation of FXR transcriptional activity in health and disease: Emerging roles of FXR cofactors and post-translational modifications
Q57108067Rethinking Bile Acid Metabolism and Signaling for Type 2 Diabetes Treatment
Q35833255Reversal of Endothelial Dysfunction by GPBAR1 Agonism in Portal Hypertension Involves a AKT/FOXOA1 Dependent Regulation of H2S Generation and Endothelin-1.
Q92269205Role for diet in normal gut barrier function: developing guidance within the framework of food-labeling regulations
Q36497654Role of nuclear receptors in lipid dysfunction and obesity-related diseases.
Q39600541SHP-dependent and -independent induction of peroxisome proliferator-activated receptor-γ by the bile acid sensor farnesoid X receptor counter-regulates the pro-inflammatory phenotype of liver myofibroblasts
Q47238539Small Intestinal Bypass Induces a Persistent Weight-Loss Effect and Improves Glucose Tolerance in Obese Rats
Q38541491Steroidal scaffolds as FXR and GPBAR1 ligands: from chemistry to therapeutical application
Q41022676Structure based classification for bile salt export pump (BSEP) inhibitors using comparative structural modeling of human BSEP.
Q43175647Structure-based drug design targeting the cell membrane receptor GPBAR1: exploiting the bile acid scaffold towards selective agonism
Q34955918Studies in mice, hamsters, and rats demonstrate that repression of hepatic apoA-I expression by taurocholic acid in mice is not mediated by the farnesoid-X-receptor
Q42140794Studying the Differences of Bacterial Metabolome and Microbiome in the Colon between Landrace and Meihua Piglets
Q36290513Synthesis and biological evaluations of chalcones, flavones and chromenes as farnesoid x receptor (FXR) antagonists
Q44134783Synthesis and quantitative structure-property relationships of side chain-modified hyodeoxycholic acid derivatives.
Q36790557TGR5 signalling inhibits the production of pro-inflammatory cytokines by in vitro differentiated inflammatory and intestinal macrophages in Crohn's disease
Q35094206TGR5: a novel target for weight maintenance and glucose metabolism
Q37727582Targeting Bile Acid Receptors: Discovery of a Potent and Selective Farnesoid X Receptor Agonist as a New Lead in the Pharmacological Approach to Liver Diseases
Q26738730Targeting the gastrointestinal tract to treat type 2 diabetes
Q38700513The Bile Acid Receptor GPBAR1 Regulates the M1/M2 Phenotype of Intestinal Macrophages and Activation of GPBAR1 Rescues Mice from Murine Colitis.
Q30486707The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors
Q35249092The G-protein-coupled bile acid receptor, Gpbar1 (TGR5), negatively regulates hepatic inflammatory response through antagonizing nuclear factor κ light-chain enhancer of activated B cells (NF-κB) in mice
Q38115636The bile acid membrane receptor TGR5: a novel pharmacological target in metabolic, inflammatory and neoplastic disorders.
Q28590901The bile acid receptor GPBAR-1 (TGR5) modulates integrity of intestinal barrier and immune response to experimental colitis
Q37641553The bile acid receptor GPBAR1 (TGR5) is expressed in human gastric cancers and promotes epithelial-mesenchymal transition in gastric cancer cell lines.
Q22122073The genome of the hydatid tapeworm Echinococcus granulosus
Q24314242The nuclear receptor FXR regulates hepatic transport and metabolism of glutamine and glutamate
Q57107473The role of bile acids in nutritional support
Q64911067Transcriptome Analysis of Dual FXR and GPBAR1 Agonism in Rodent Model of NASH Reveals Modulation of Lipid Droplets Formation.
Q92464070Tropifexor-Mediated Abrogation of Steatohepatitis and Fibrosis Is Associated With the Antioxidative Gene Expression Profile in Rodents
Q36494764Unifying mechanisms of action of the anticancer activities of triterpenoids and synthetic analogs
Q43125212Utility of the carboxylesterase inhibitor bis-para-nitrophenylphosphate (BNPP) in the plasma unbound fraction determination for a hydrolytically unstable amide derivative and agonist of the TGR5 receptor