Deciphering the nuclear bile acid receptor FXR paradigm.

Salvatore Modica, Raffaella M. Gadaleta, Antonio Moschetta

Research output: Contribution to journalReview article

151 Scopus citations

Abstract

Originally called retinoid X receptor interacting protein 14 (RIP14), the farnesoid X receptor (FXR) was renamed after the ability of its rat form to bind supra-physiological concentrations of farnesol. In 1999 FXR was de-orphanized since primary bile acids were identified as natural ligands. Strongly expressed in the liver and intestine, FXR has been shown to be the master transcriptional regulator of several entero-hepatic metabolic pathways with relevance to the pathophysiology of conditions such as cholestasis, fatty liver disease, cholesterol gallstone disease, intestinal inflammation and tumors. Furthermore, given the importance of FXR in the gut-liver axis feedbacks regulating lipid and glucose homeostasis, FXR modulation appears to have great input in diseases such as metabolic syndrome and diabetes. Exciting results from several cellular and animal models have provided the impetus to develop synthetic FXR ligands as novel pharmacological agents. Fourteen years from its discovery, FXR has gone from bench to bedside; a novel nuclear receptor ligand is going into clinical use.

Original languageEnglish (US)
Pages (from-to)e005
JournalNuclear receptor signaling
Volume8
DOIs
StatePublished - 2010

ASJC Scopus subject areas

  • Medicine(all)

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