ArticleMolecular metabolism2018
Reversal of metabolic disorders by pharmacological activation of bile acid receptors TGR5 and FXR.
Article in Molecular metabolism, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 60 papers, 1 of them a synthesis that pooled it.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
60 citing papers in PubMed, 1 synthesis or guideline pooled it, 114 citations in OpenAlex.
- Gut microbiota is a potential goalkeeper of dyslipidemia.Frontiers in endocrinology · 2022Pooled it
- Phyllanthus niruri niosomes ameliorate obesity-induced hepatic steatosis in rats via modulating MALAT1/miR-206/GLP-1R signaling and hepatic lipid metabolism.Biological research · 2026Article
- The role of bile acid-activated receptor TGR5 in inflammation and liver diseases.Frontiers in physiology · 2026Review
- Advances in understanding the role of gut microbiota in fat deposition and lipid metabolism.Journal of animal science and biotechnology · 2025Review
- The association between the dietary index for gut microbiota and non-alcoholic fatty liver disease and liver fibrosis: evidence from NHANES 2017-2020.BMC gastroenterology · 2025Article
- Deoxycholic acid ameliorates obesity and insulin resistance by enhancing lipolysis and thermogenesis.Lipids in health and disease · 2025Article
- Bile acid-microbiota interactions in cardiometabolic diseases: mechanisms and emerging therapeutic approaches.Frontiers in microbiology · 2025Review
- Association of Serum Bile Acid Profile with Diet and Physical Activity Habits in Japanese Middle-Aged Men.Nutrients · 2024Article
- Review
- Bile acid metabolism and signaling in health and disease: molecular mechanisms and therapeutic targets.Signal transduction and targeted therapy · 2024Review
- Effects of Dietary Supplementation of Bile Acids on Growth, Glucose Metabolism, and Intestinal Health of Spotted Seabass (Animals : an open access journal from MDPI · 2024Article
- Therapeutic applications of gut microbes in cardiometabolic diseases: current state and perspectives.Applied microbiology and biotechnology · 2024Review
- Gut Microbiota and Metabolic Syndrome: Relationships and Opportunities for New Therapeutic Strategies.Scientifica · 2024Review
- Effects of plant natural products on metabolic-associated fatty liver disease and the underlying mechanisms: a narrative review with a focus on the modulation of the gut microbiota.Frontiers in cellular and infection microbiology · 2024Review
- Regulating bile acids signaling for NAFLD: molecular insights and novel therapeutic interventions.Frontiers in microbiology · 2024Review
- Emerging Roles of Gut Microbial Modulation of Bile Acid Composition in the Etiology of Cardiovascular Diseases.Nutrients · 2023Review
- Exercise-acclimated microbiota improves skeletal muscle metabolism via circulating bile acid deconjugation.iScience · 2023Article
- GLP-1 Receptor Agonists in Non-Alcoholic Fatty Liver Disease: Current Evidence and Future Perspectives.International journal of molecular sciences · 2023Review
- Peroxisome proliferator-activated receptors, farnesoid X receptor, and dual modulating drugs in hypertension.Frontiers in physiology · 2023Review
- Bile Acid Network and Vascular Calcification-Associated Diseases: Unraveling the Intricate Connections and Therapeutic Potential.Clinical interventions in aging · 2023Review
Corrections and comments
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Authors and funding
11 authors at 3 institutions in 2 countries.
Funding
Abstract
objectivesActivation of the bile acid (BA) receptors farnesoid X receptor (FXR) or G protein-coupled bile acid receptor (GPBAR1; TGR5) improves metabolic homeostasis. In this study, we aim to determine the impact of pharmacological activation of bile acid receptors by INT-767 on reversal of diet-induced metabolic disorders, and the relative contribution of FXR vs. TGR5 to INT-767's effects on metabolic parameters.
methodsWild-type (WT), Tgr5
resultsINT-767 reversed HFD-induced obesity dependent on activation of both TGR5 and FXR and also reversed the development of atherosclerosis and non-alcoholic fatty liver disease (NAFLD). Mechanistically, INT-767 improved hypercholesterolemia by activation of FXR and induced thermogenic genes via activation of TGR5 and/or FXR. Furthermore, INT-767 inhibited several lipogenic genes and de novo lipogenesis in the liver via activation of FXR. We identified peroxisome proliferation-activated receptor γ (PPARγ) and CCAAT/enhancer-binding protein α (CEBPα) as novel FXR-regulated genes. FXR inhibited PPARγ expression by inducing small heterodimer partner (SHP) whereas the inhibition of CEBPα by FXR was SHP-independent.
conclusionsBA receptor activation can reverse obesity, NAFLD, and atherosclerosis by specific activation of FXR or TGR5. Our data suggest that, compared to activation of FXR or TGR5 only, dual activation of both FXR and TGR5 is a more attractive strategy for treatment of common metabolic disorders.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.