The DOI matches its Crossref record; 170 of the 170 references it cites were found in a registry or an index.
Bile acid receptors as targets for drug development
Open accessAbstract
The intracellular nuclear receptor farnesoid X receptor and the transmembrane G protein-coupled receptor TGR5 respond to bile acids by activating transcriptional networks and/or signalling cascades. These cascades affect the expression of a great number of target genes relevant for bile acid, cholesterol, lipid and carbohydrate metabolism, as well as genes involved in inflammation, fibrosis and carcinogenesis. Pregnane X receptor, vitamin D receptor and constitutive androstane receptor are additional nuclear receptors that respond to bile acids, albeit to a more restricted set of species of bile acids. Recognition of dedicated bile acid receptors prompted the development of semi-synthetic bile acid analogues and nonsteroidal compounds that target these receptors. These agents hold promise to become a new class of drugs for the treatment of chronic liver disease, hepatocellular cancer and extrahepatic inflammatory and metabolic diseases. This Review discusses the relevant bile acid receptors, the new drugs that target bile acid signalling and their possible applications.
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“Many of the hepatic effects of FXR activation are mediated by intestinal FXR receptors, resulting in the release of FGF19, which then acts on targets in the liver136–139.”
From The gut microbiome and liver cancer: mechanisms and clinical translation (2017) · cites this paper as [136]
In the citing paper
“FXR is a receptor for bile acids that mediates their effects on the intestinal epithelial barrier as well as multiple effects on the liver, such as suppression of bile acid synthesis, inhibition of liver inflammation, promotion of liver regeneration and tumour suppression (reviewed elsewhere136).”
From The gut microbiome and liver cancer: mechanisms and clinical translation (2017) · cites this paper as [136]
Citations
Cites
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Bile acids induce energy expenditure by promoting intracellular thyroid hormone activation
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A regulatory cascade of the nuclear receptors FXR, SHP-1, and LRH-1 represses bile acid biosynthesis
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TGR5-Mediated Bile Acid Sensing Controls Glucose Homeostasis
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Research works printed but not linked: 1
- van Dijk, R., Kremer, A. F., Enemuo, V., Jansen, P. L., Beuers, U. Clinical and molecular aspects of rifampicin-mediated attenuation of severe persistent hepatocellular secretory failure. Hepatology 56, 549A (2012).
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Intestinal Crosstalk between Bile Acids and Microbiota and Its Impact on Host Metabolism
Wahlstrom, A. M., Sayin, S. I., Marschall, H., & Bäckhed, F. (2016) · Cell Metabolism · doi:10.1016/j.cmet.2016.05.005 · Cited by 2,969
Gut microbiota-derived metabolites as key actors in inflammatory bowel disease
Lavelle, A., & Sokol, H. (2020) · Nature Reviews Gastroenterology & Hepatology · doi:10.1038/s41575-019-0258-z · Cited by 2,015
Wu, H., Esteve, E., Tremaroli, V., Khan, M. T., Caesar, R., Mannerås-Holm, L., Ståhlman, M., Olsson, L. M., Serino, M., Planas-Fèlix, M., et al. (2017) · Nature Medicine · doi:10.1038/nm.4345 · Cited by 1,632
Chait, A., & den Hartigh, L. J. (2020) · Frontiers in Cardiovascular Medicine · doi:10.3389/fcvm.2020.00022 · Cited by 1,529
Hirschfield, G. M., Beuers, U., Corpechot, C., Invernizzi, P., Jones, D., Marzioni, M., & Schramm, C. (2017) · Journal of Hepatology · doi:10.1016/j.jhep.2017.03.022 · Cited by 1,480
Metadata
- Authors
- Schaap, F. G., Trauner, M., & Jansen, P. L. M.
- Affiliations
- Maastricht University (NL)
- Medical University of Vienna (AT)
- Amsterdam UMC Location University of Amsterdam (NL)
- Corresponding author
- Jansen, Peter L. M.
- Venue
- Nature Reviews Gastroenterology & Hepatology
- Published
- 2013-08-27
- Volume
- 11
- Issue
- 1
- Pages
- 55-67
- ISSN
- 1759-5045 (ISSN-L)
- 1759-5053
- OpenAlex
- W2022279737
- Cited by
- 696
- References
- 170
- Citations by year
- 2026: 40 · 2025: 36 · 2024: 50 · 2023: 58 · 2022: 74 · 2021: 80 · 2020: 67 · 2019: 61 · 2018: 62 · 2017: 49 · 2016: 56 · 2015: 32 · 2014: 30 · 2013: 1
- FWCI
- 4.27
- Type
- journal article
- Language
- en
- Open access
- green
- zenodo.org
- Licence
- other-oa
- www.springer.com/tdm (tdm)
- Locations
- Nature Reviews Gastroenterology & Hepatology (publishedVersion)
- PubMed (publishedVersion)
- Pure Amsterdam UMC (publishedVersion)
- Data Archiving and Networked Services (DANS) (submittedVersion)
- Research Publications (Maastricht University) (submittedVersion)
- Zenodo (CERN European Organization for Nuclear Research) (submittedVersion, other-oa)
- Funders
- CYTED Ciencia y Tecnología para el Desarrollo
- Topics
- Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Biochemistry › Cholesterol and Lipid Metabolism
- Health Sciences › Medicine › Hepatology › Liver physiology and pathology
- Keywords
- bile acid receptors, bile acid signaling, farnesoid X receptor, TGR5, G protein-coupled receptors, nuclear receptors, pregnane X receptor, vitamin D receptor, constitutive androstane receptor, bile acid analogues, drug development, chronic liver disease, hepatocellular carcinoma, inflammation, fibrosis, metabolic disorders, cholesterol metabolism
- MeSH terms
- Animals, Bile Acids and Salts, Disease Models, Animal, Drug Therapy, Humans, Inflammation, Liver Diseases, Liver Neoplasms, Metabolic Diseases, Signal Transduction, Receptors, Cytoplasmic and Nuclear, Mice
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