The DOI matches its Crossref record; 376 of the 376 references it cites were found in a registry or an index.
Bile acids and their receptors in metabolic disorders
Abstract
Bile acids are a large family of atypical steroids which exert their functions by binding to a family of ubiquitous cell membrane and nuclear receptors. There two receptors, FXR and GPBAR1, that are exclusively activated by bile acids while other receptors RORγT, S1PR2, CAR, LXRs, PXR and VDR are activated by bile acids in addition to other more selective endogenous ligands. In the intestine, activation of FXR and GPBAR1 promotes the release of FGF15/19 and GLP1 which integrate their signaling with direct effects exerted by the two receptors in target tissues. This network is tuned in a time ordered manner by circadian rhythm and is critical for the regulation of metabolic process including autophagy, fast-to-feed transition, lipid and glucose metabolism, energy balance and immune responses. In the last decade FXR ligands have entered clinical trials but development of systemic FXR agonists has been proven challenging because their side effects including increased levels of cholesterol and Low Density Lipoproteins cholesterol (LDL-c) and reduced High-Density Lipoprotein cholesterol (HDL-c). In addition, pruritus has emerged as a common, dose related, side effect of FXR ligands. Intestinal-restricted FXR and GPBAR1 agonists and dual FXR/GPBAR1 agonists have been developed. Here we review the last decade in bile acids physiology and pharmacology.
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Cites
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Cited by
Role of bile acids in inflammatory liver diseases
Evangelakos, I., Heeren, J., Verkade, E., & Kuipers, F. (2021) · Seminars in Immunopathology · doi:10.1007/s00281-021-00869-6 · Cited by 121
Bile acids activated receptors in inflammatory bowel disease
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Self-citationDeficiency of Epithelial PIEZO1 Alleviates Liver Steatosis Induced by High-Fat Diet in Mice
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Metadata
- Authors
- Fiorucci, S., Distrutti, E., Carino, A., Zampella, A., & Biagioli, M.
- Venue
- Progress in Lipid Research
- Publisher
- Elsevier BV
- Published
- 2021-04
- Volume
- 82
- Pages
- 101094
- ISSN
- 0163-7827 (ISSN-L)
- OpenAlex
- W3129439580
- Cited by
- 258
- References
- 376
- FWCI
- 13.53
- Type
- journal article
- Language
- en
- Open access
- closed
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