Abstract
The nuclear farnesoid X receptor (FXR) plays a pivotal role in maintaining bile acid homeostasis by regulating key genes involved in bile acid synthesis, metabolism and transport, including CYP7A1, UGT2B4, BSEP, MDR3, MRP2, ASBT, I-BABP, NTCP and OSTalpha-OSTbeta in humans. Altered expression or malfunction of these genes has been described in patients with cholestatic liver diseases. This review examines the rationale for the use of FXR ligand therapy in various cholestatic liver disorders and includes potential concerns.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Animals
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Cholestasis / drug therapy*
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Cholestasis / genetics
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Cholestasis / metabolism*
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DNA-Binding Proteins / biosynthesis
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DNA-Binding Proteins / genetics
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DNA-Binding Proteins / metabolism*
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DNA-Binding Proteins / physiology
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Drug Delivery Systems / methods*
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Humans
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Receptors, Cytoplasmic and Nuclear
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Syndrome
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Transcription Factors / biosynthesis
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Transcription Factors / genetics
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Transcription Factors / metabolism*
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Transcription Factors / physiology
Substances
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DNA-Binding Proteins
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Receptors, Cytoplasmic and Nuclear
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Transcription Factors
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farnesoid X-activated receptor