The DOI matches its Crossref record; 5 of the 5 references it cites were found in a registry or an index.
The Nuclear Pregnane X Receptor: A Key Regulator of Xenobiotic Metabolism
Abstract
The nuclear pregnane X receptor (PXR; NR1I2) is an important component of the body's adaptive defense mechanism against toxic substances including foreign chemicals (xenobiotics). PXR is activated by a large number of endogenous and exogenous chemicals including steroids, antibiotics, antimycotics, bile acids, and the herbal antidepressant St. John's wort. Elucidation of the three-dimensional structure of the PXR ligand binding domain revealed that it has a large, spherical ligand binding cavity that allows it to interact with a wide range of hydrophobic chemicals. Thus, unlike other nuclear receptors that interact selectively with their physiological ligands, PXR serves as a generalized sensor of hydrophobic toxins. PXR binds as a heterodimer with the 9-cis retinoic acid receptor (NR2B) to DNA response elements in the regulatory regions of cytochrome P450 3A monooxygenase genes and a number of other genes involved in the metabolism and elimination of xenobiotics from the body. Although PXR evolved to protect the body, its activation by a variety of prescription drugs represents the molecular basis for an important class of harmful drug-drug interactions. Thus, assays that detect PXR activity will be useful in developing safer prescription drugs.
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Cites
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Endogenous Bile Acids Are Ligands for the Nuclear Receptor FXR/BAR
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COMPARISON OF RIFAMPICIN WITH PHENOBARBITONE FOR TREATMENT OF PRURITUS IN BILIARY CIRRHOSIS
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State-of-the-science of endocrine disrupting chemicals, 2012
Bergman, Å., Heindel, J., Jobling, S., Kidd, K., & Zoeller, R. T. (2012) · Toxicology Letters · doi:10.1016/j.toxlet.2012.03.020 · Cited by 1,388
Hewitt, N. J., Gómez Lechón, M. J., Houston, J. B., Hallifax, D., Brown, H. S., Maurel, P., Kenna, J. G., Gustavsson, L., Lohmann, C., Skonberg, C., et al. (2007) · Drug Metabolism Reviews · doi:10.1080/03602530601093489 · Cited by 735
Induction of Drug Metabolism: The Role of Nuclear Receptors
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A nuclear receptor-like pathway regulating multidrug resistance in fungi
Thakur, J. K., Arthanari, H., Yang, F., Pan, S.-J., Fan, X., Breger, J., Frueh, D. P., Gulshan, K., Li, D. K., Mylonakis, E., et al. (2008) · Nature · doi:10.1038/nature06836 · Cited by 343
Emerging roles of bile acids in mucosal immunity and inflammation
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Metadata
- Authors
- Kliewer, S. A., Goodwin, B., & Willson, T. M.
- Venue
- Endocrine Reviews
- Publisher
- The Endocrine Society
- Published
- 2002-10-01
- Volume
- 23
- Issue
- 5
- Pages
- 687-702
- ISSN
- 0163-769X (ISSN-L)
- 1945-7189
- OpenAlex
- W2032693719
- Cited by
- 921
- References
- 5
- FWCI
- 16.64
- Type
- journal article
- Language
- en
- Open access
- closed
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