Nuclear receptors in bile acid metabolism
Open accessAbstract
Bile acids are signaling molecules that activate nuclear receptors, such as farnesoid X receptor, pregnane X receptor, constitutive androstane receptor, and vitamin D receptor, and play a critical role in the regulation of lipid, glucose, energy, and drug metabolism. These xenobiotic/endobiotic-sensing nuclear receptors regulate phase I oxidation, phase II conjugation, and phase III transport in bile acid and drug metabolism in the digestive system. Integration of bile acid metabolism with drug metabolism controls absorption, transport, and metabolism of nutrients and drugs to maintain metabolic homeostasis and also protects against liver injury, inflammation, and related metabolic diseases, such as nonalcoholic fatty liver disease, diabetes, and obesity. Bile-acid-based drugs targeting nuclear receptors are in clinical trials for treating cholestatic liver diseases and fatty liver disease.
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Most BBAA activators of human FXR were conjugates of CDCA (5 of 8, P < 0.0001).
“Most of the BBAA activators of the human bile acid receptor FXR were conjugates of CDCA (5 of 8, P < 0.0001), probably reflecting the potency of CDCA as an FXR agonist26.”
From Bile Acids Are Substrates for Amine N-Acyl Transferase Activity by Bile Salt Hydrolase (2022) · cites this paper as [26]
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References 96 · Cited by 176
- Authors
- Li, T., & Chiang, J. Y. L.
- Affiliations
- Northeast Ohio Medical University (US)
- Corresponding author
- Chiang, John Y. L.
- Venue
- Drug Metabolism Reviews
- Publisher
- Informa UK Limited
- Published
- 2013-01-21
- Volume
- 45
- Issue
- 1
- Pages
- 145-155
- ISSN
- 0360-2532 (ISSN-L)
- 1097-9883
- PMC
- PMC3676171
- OpenAlex
- W2031686588
- Cited by
- 176
- References
- 96
- Citations by year
- 2026: 12 · 2025: 14 · 2024: 14 · 2023: 12 · 2022: 8 · 2021: 14 · 2020: 17 · 2019: 10 · 2018: 11 · 2017: 14 · 2016: 13 · 2015: 12 · 2014: 21 · 2013: 4
- FWCI
- 1.80
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- Drug Metabolism Reviews (publishedVersion)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- Funders
- National Institutes of Health (5r01dk044442-26)
- National Institute of Diabetes and Digestive and Kidney Diseases (DK 58379, DK44442, R01-DK-044442, R01DK058379, R56DK044442, R37DK058379)
- Topics
- Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
- Health Sciences › Medicine › Surgery › Cholesterol and Lipid Metabolism
- Keywords
- nuclear receptors, bile acids, farnesoid X receptor, pregnane X receptor, constitutive androstane receptor, vitamin D receptor, drug metabolism, phase II conjugation, bile acid transport, metabolic homeostasis, non-alcoholic fatty liver disease, cholestatic liver disease, liver injury
- MeSH terms
- Animals, Bile Acids and Salts, Biological Transport, Humans, Inactivation, Metabolic, Xenobiotics, Receptors, Cytoplasmic and Nuclear
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