The DOI matches its Crossref record; 83 of the 83 references it cites were found in a registry or an index.
Role of TGR5 (GPBAR1) in Liver Disease
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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“Impaired TGR5 expression and signalling may contribute to the pathogenesis of cholangiopathies such as PBC and PSC, since TGR5 also protects cholangiocytes by stimulating bicarbonate secretion.48 49”
From Novel therapeutic targets for cholestatic and fatty liver disease (2022) · cites this paper as [48]
In the citing paper
“However, persistent stimulation of TGR5 may predispose to gallstone formation through changes in gallbladder motility and promotes proliferation of cholangiocellular carcinoma (CCC) cells and polycystic cholangiocytes which overexpress TGR5, thus raising safety concerns for clinical development of TGR5 agonists.48”
From Novel therapeutic targets for cholestatic and fatty liver disease (2022) · cites this paper as [48]
Citations
Cites
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TGR5-Mediated Bile Acid Sensing Controls Glucose Homeostasis
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Influence of bile acids metabolism on hepatic immunity in mice
Guinot, V. (2022) · theses.fr (ABES) · doi:10.70675/b69bb11eza30fz4874z9af2za6e31b2d5ad8
Liang, X., Liang, Y., Liu, S., Yu, L., Liang, Y., & Zhou, L. (2026) · Frontiers in Pharmacology · doi:10.3389/fphar.2026.1789551
Turner, M., Nguyen, S., Clark, D., & Wilson, E. (2024) · Bulletin of pioneering researches of medical and clinical science · doi:10.51847/au7gfacg1r
Fan, M., & Li, X. (2026) · Metabolic Brain Disease · doi:10.1007/s11011-026-01867-z
Zhou, H., Yang, J., Wu, W., Wei, S., ZHAO, Y., & Li, C. (2026) · Expert Opinion on Therapeutic Targets · doi:10.1080/14728222.2026.2695704
Li, S.-X., Gao, Z.-H., Ma, Y.-T., Zhang, J.-Q., & Wei, W. (2026) · Frontiers in Cellular and Infection Microbiology · doi:10.3389/fcimb.2026.1942882
Metadata
- Authors
- Häussinger, D., & Keitel, V.
- Affiliations
- Düsseldorf University Hospital (DE)
- Corresponding author
- 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
- 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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