Cited by 106Drug Transport and Resistance MechanismsLiver physiology and pathologyLiver Diseases and Immunity

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Role of TGR5 (GPBAR1) in Liver Disease

Häussinger, Dieter, Keitel, Verena·2018·Seminars in Liver Disease

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Abstract

TGR5 (GPBAR1) is a G protein–coupled receptor activated by primary and secondary bile acids, which is expressed in different nonparenchymal cells of the liver, such as sinusoidal endothelial cells, Kupffer cells, cholangiocytes as well as activated hepatic stellate cells. In liver, TGR5 modulates microcirculation, inflammation, regeneration, biliary secretion and proliferation as well as gallbladder filling. Absence of TGR5 renders mice more susceptible toward infectious, inflammatory, metabolic as well as cholestatic liver injuries. It is unknown whether TGR5 plays a role in the pathogenesis of human nonalcoholic steatohepatitis and cholestatic liver diseases such as primary sclerosing cholangitis and primary biliary cholangitis. However, overexpression of TGR5 has been detected in human intra- and extrahepatic cholangiocarcinoma as well as in cystic cholangiocytes, where the receptor promotes cell proliferation, anti-apoptosis as well as cyst growth. While TGR5 agonists may improve various aspects of metabolic, inflammatory, and cholestatic liver diseases, TGR5 inhibitors may attenuate disease progression in polycystic liver disease and cholangiocarcinoma.

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Authors: Häussinger, D., & Keitel, V.
Affiliations: Düsseldorf University Hospital (DE)
Corresponding author: Keitel, Verena
ORCID: Häussinger, Dieter
Keitel, Verena
Venue: Seminars in Liver Disease
Publisher: Georg Thieme Verlag KG
Published: 2018-10-24
Volume: 38
Issue: 04
Pages: 333-339
ISSN: 0272-8087 (ISSN-L)
1098-8971
DOI: 10.1055/s-0038-1669940
OpenAlex: W2898124054
Cited by: 106
References: 83
Citations by year: 2026: 8 · 2025: 13 · 2024: 20 · 2023: 15 · 2022: 11 · 2021: 21 · 2020: 12 · 2019: 6
FWCI: 3.66
Type: journal article
Language: en
Open access: closed
Locations: Seminars in Liver Disease (publishedVersion)
PubMed (publishedVersion)
Topics: Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
Health Sciences › Medicine › Hepatology › Liver physiology and pathology
Health Sciences › Medicine › Hepatology › Liver Diseases and Immunity
Keywords: TGR5, G protein-coupled receptors, bile acids, liver disease, cholestatic liver injury, nonalcoholic steatohepatitis, primary sclerosing cholangitis, primary biliary cirrhosis, cholangiocarcinoma, polycystic liver disease, TGR5 agonists, hepatic stellate cells, Kupffer cells, cholangiocytes, liver regeneration, inflammation
MeSH terms: Animals, Bile Acids and Salts, Bile Duct Diseases, Cholestasis, Epithelial Cells, Humans, Hypertension, Portal, Liver Diseases, Signal Transduction, Cholangiocarcinoma, Receptors, G-Protein-Coupled, Mice

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Role of TGR5 (GPBAR1) in Liver Disease

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