The DOI matches its Crossref record; 33 of the 33 references it cites were found in a registry or an index.
A Natural Product That Lowers Cholesterol As an Antagonist Ligand for FXR
Abstract
Extracts of the resin of the guggul tree ( Commiphora mukul ) lower LDL (low-density lipoprotein) cholesterol levels in humans. The plant sterol guggulsterone [4,17(20)-pregnadiene-3,16-dione] is the active agent in this extract. We show that guggulsterone is a highly efficacious antagonist of the farnesoid X receptor (FXR), a nuclear hormone receptor that is activated by bile acids. Guggulsterone treatment decreases hepatic cholesterol in wild-type mice fed a high-cholesterol diet but is not effective in FXR-null mice. Thus, we propose that inhibition of FXR activation is the basis for the cholesterol-lowering activity of guggulsterone. Other natural products with specific biologic effects may modulate the activity of FXR or other relatively promiscuous nuclear hormone receptors.
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Cites
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Self-citationBile Acids: Natural Ligands for an Orphan Nuclear Receptor
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Self-citationTargeted Disruption of the Nuclear Receptor FXR/BAR Impairs Bile Acid and Lipid Homeostasis
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Self-citationEndogenous Bile Acids Are Ligands for the Nuclear Receptor FXR/BAR
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Self-citationThe nuclear receptor PXR is a lithocholic acid sensor that protects against liver toxicity
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Cited by
The Enzymes, Regulation, and Genetics of Bile Acid Synthesis
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Role of Bile Acids and Bile Acid Receptors in Metabolic Regulation
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Targeting bile‐acid signalling for metabolic diseases
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Intestinal farnesoid X receptor signaling promotes nonalcoholic fatty liver disease
Jiang, C., Xie, C., Li, F., Zhang, L., Nichols, R. G., Krausz, K. W., Cai, J., Qi, Y., Fang, Z.-Z., Takahashi, S., et al. (2015) · Journal of Clinical Investigation · doi:10.1172/jci76738 · Cited by 693
Self-citation
Metadata
- Authors
- Urizar, N. L., Liverman, A. B., Dodds, D. T., Silva, F. V., Ordentlich, P., Yan, Y., Gonzalez, F. J., Heyman, R. A., Mangelsdorf, D. J., & Moore, D. D.
- Venue
- Science
- Published
- 2002-05-31
- Volume
- 296
- Issue
- 5573
- Pages
- 1703-1706
- ISSN
- 0036-8075 (ISSN-L)
- 1095-9203
- OpenAlex
- W2052725031
- Cited by
- 549
- References
- 33
- FWCI
- 32.06
- Type
- journal article
- Language
- en
- Open access
- closed
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- Urizar, N. L., Liverman, A. B., Dodds, D. T., Silva, F. V., Ordentlich, P., Yan, Y., Gonzalez, F. J., Heyman, R. A., Mangelsdorf, D. J., & Moore, D. D. (2002). A Natural Product That Lowers Cholesterol As an Antagonist Ligand for FXR. Science. https://doi.org/10.1126/science.1072891
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
