ArticleCellular and molecular gastroenterology and hepatology2020
Inhibition of Hepatic Bile Acid Uptake by Myrcludex B Promotes Glucagon-Like Peptide-1 Release and Reduces Obesity.
Article in Cellular and molecular gastroenterology and hepatology, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 20 citations in OpenAlex.
- Glucagon-like peptide-1: a critical link between gut microbiota dysbiosis and degenerative musculoskeletal diseases.Gut microbes · 2026Review
- Bile acid signaling in health and disease.Molecular biomedicine · 2026Review
- Altered Bile Acid Transport in Liver Disease.Biomedicines · 2026Review
- Article
- The designer cytokine IC7Fc attenuates atherosclerosis development by targeting hyperlipidemia in mice.Science advances · 2025Article
- Dysregulated bile acid homeostasis: unveiling its role in metabolic diseases.Medical review (2021) · 2024Review
- Inhibition of hepatic bile salt uptake by Bulevirtide reduces atherosclerosis in Oatp1a1Journal of lipid research · 2024Article
- Bile salt signaling and bile salt-based therapies in cardiometabolic disease.Clinical science (London, England : 1979) · 2024Article
- Validation of NBD-coupled taurocholic acid for intravital analysis of bile acid transport in liver and kidney of mice.EXCLI journal · 2024Article
- Biological tuners to reshape the bile acid pool for therapeutic purposes in non-alcoholic fatty liver disease.Clinical science (London, England : 1979) · 2023Review
- Metabolic Effect of Blocking Sodium-Taurocholate Co-Transporting Polypeptide in Hypercholesterolemic Humans with a Twelve-Week Course of Bulevirtide-An Exploratory Phase I Clinical Trial.International journal of molecular sciences · 2022Article
- Article
- Multitasking NaBiomedicines · 2022Review
- Modulation of Bile Acid Metabolism to Improve Plasma Lipid and Lipoprotein Profiles.Journal of clinical medicine · 2021Review
- Chronic hepatitis B infection with concomitant hepatic steatosis: Current evidence and opinion.World journal of gastroenterology · 2021Review
- Targeting the Four Pillars of Enterohepatic Bile Salt Cycling; Lessons From Genetics and Pharmacology.Hepatology (Baltimore, Md.) · 2021Review
- A New Treatment for Chronic Hepatitis B and D Offers Novel Insights Into Obesity and Hepatic Steatosis.Cellular and molecular gastroenterology and hepatology · 2020Article
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Authors and funding
8 authors at 3 institutions in 1 country.
Funding
Abstract
BACKGROUND &
aimsBile acids are important metabolic signaling molecules. Bile acid receptor activation promotes body weight loss and improves glycemic control. The incretin hormone GLP-1 and thyroid hormone activation of T4 to T3 have been suggested as important contributors. Here, we identify the hepatic bile acid uptake transporter Na
methodsOrganic anion transporting polypeptide (OATP)1a/1b KO mice with or without reconstitution with human OATP1B1 in the liver were treated with the NTCP inhibitor Myrcludex B for 3.5 weeks after the onset of obesity induced by high fat diet-feeding. Furthermore, radiolabeled T4 was injected to determine the role of NTCP and OATPs in thyroid hormone clearance from plasma.
resultsInhibition of NTCP by Myrcludex B in obese Oatp1a/1b KO mice inhibited hepatic clearance of bile acids from portal and systemic blood, stimulated GLP-1 secretion, reduced body weight, and decreased (hepatic) adiposity. NTCP inhibition did not affect hepatic T4 uptake nor lead to increased thyroid hormone activation. Myrcludex B treatment increased fecal energy output, explaining body weight reductions amongst unaltered food intake and energy expenditure.
conclusionsPharmacologically targeting hepatic bile acid uptake to increase bile acid signaling is a novel approach to treat obesity and induce GLP1- secretion.
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