Literature DB >> 21801835

FXR and PXR: potential therapeutic targets in cholestasis.

Johan W Jonker1, Christopher Liddle, Michael Downes.   

Abstract

Cholestatic liver disorders encompass hepatobiliary diseases of diverse etiologies characterized by the accumulation of bile acids, bilirubin and cholesterol as the result of impaired secretion of bile. Members of the nuclear receptor (NR) family of ligand-modulated transcription factors are implicated in the adaptive response to cholestasis. NRs coordinately regulate bile acid and phospholipid transporter genes required for hepatobiliary transport, as well as the phases I and II metabolizing enzymes involved in processing of their substrates. In this review we will focus on FXR and PXR, two members of the NR family whose activities are regulated by bile acids. In addition, we also discuss the potential of pharmacological modulators of these receptors as novel therapies for cholestatic disorders.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21801835      PMCID: PMC4750880          DOI: 10.1016/j.jsbmb.2011.06.012

Source DB:  PubMed          Journal:  J Steroid Biochem Mol Biol        ISSN: 0960-0760            Impact factor:   4.292


  138 in total

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  44 in total

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Review 4.  An updated review on drug-induced cholestasis: mechanisms and investigation of physicochemical properties and pharmacokinetic parameters.

Authors:  Kyunghee Yang; Kathleen Köck; Alexander Sedykh; Alexander Tropsha; Kim L R Brouwer
Journal:  J Pharm Sci       Date:  2013-05-07       Impact factor: 3.534

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6.  Altered Bile Acid Metabolome in Patients with Nonalcoholic Steatohepatitis.

Authors:  Brian C Ferslew; Guoxiang Xie; Curtis K Johnston; Mingming Su; Paul W Stewart; Wei Jia; Kim L R Brouwer; A Sidney Barritt
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7.  Pregnane X receptor modulates the inflammatory response in primary cultures of hepatocytes.

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Journal:  Drug Metab Rev       Date:  2013-02       Impact factor: 4.518

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10.  Expression Patterns of Organic Anion Transporting Polypeptides 1B1 and 1B3 Protein in Human Pediatric Liver.

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