The farnesoid X receptor: a novel drug target?

Authors: Thierry Claudel; Ekkehard Sturm; Folkert Kuipers; Bart Staels

Source: Expert Opinion on Investigational Drugs, Volume 13, Number 9, 1 September 2004 , pp. 1135-1148(14)

Publisher: Informa Healthcare

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Abstract:

Bile acids are end products of cholesterol metabolism. They are exclusively synthesised by the liver and subsequently secreted via the bile duct into the intestine to facilitate the absorption of dietary fat and fat-soluble vitamins. Nuclear receptors are ligand-activated transcription factors. The farnesoid X receptor (FXR) has recently been identified as a bile acid-activated nuclear receptor. FXR controls bile-acid synthesis, conjugation and transport, as well as lipid metabolism. Recent advances in FXR biology demonstrate that FXR may represent a valuable target for the identification of novel drugs to treat dyslipidaemia and cholestasis. However, for therapeutic purposes the development of selective FXR modulators, which only activate or inhibit specific FXR target genes and as such induce specific responses, will be required.

Keywords: bile acid; cholestasis; FXR; lipid metabolism; nuclear receptor

Document Type: Review article

DOI: 10.1517/13543784.13.9.1135

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