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(Arteriosclerosis, Thrombosis, and Vascular Biology. 2005;25:2020.)
© 2005 American Heart Association, Inc.

Brief Reviews

The Farnesoid X Receptor

A Molecular Link Between Bile Acid and Lipid and Glucose Metabolism

Thierry Claudel; Bart Staels; Folkert Kuipers

From the Center for Liver, Digestive, and Metabolic Diseases (T.C., F.K.), Laboratory of Pediatrics, University Medical Center Groningen, the Netherlands; Unité de Recherche 545 (B.S.), INSERM Département d’Athérosclérose, Institut Pasteur de Lille, and the Faculté de Pharmacie, Université de Lille II, Lille, France.

Correspondence to Thierry Claudel, Center for Liver, Digestive, and Metabolic Diseases, Laboratory of Pediatrics, University Medical Center Groningen, Hanzeplein 1, 9700 RB Groningen, the Netherlands. E-mail t.claudel{at}med.rug.nl

Series Editor: Daniel J. Rader
ATVB In Focus Novel Approaches to the Treatment of Dyslipidemia

Previous Brief Reviews in this Series:

•Chen HC, Farese RV Jr. Inhibition of tgriglyceride synthesis as a treatment strategy for obestiy: lessons from DGAT1-deficient mice. 2005;25:482–486.
•Zalewski A. Macphee C. Role of lipoprotein-associated phospholipase A₂ in atherosclerosis: biology, epidemiology, and possible therapeutic target. 2005;25:923–931.
•Rudel LL, Lee RG, Parini P. ACTA2 is a target for treatment of coronary heart disease associated with hypercholesterolemia. 2005;25:1112–1118.
•Navab M, Anantharamaiah GM, Reddy ST, Hama S, Hough G, Grijalva VR, Yu N, Ansell BJ, Datta G, Garber DW, Fogelman AJ. Apolipoprotein A-I mimetic peptides. 2005;25:1325–1331.

Bile acids are the end products of cholesterol metabolism. They are synthesized in the liver and secreted via bile into the intestine, where they aid in the absorption of fat-soluble vitamins and dietary fat. Subsequently, bile acids return to the liver to complete their enterohepatic circulation. The Farnesoid X receptor (FXR) is a member of the nuclear receptor superfamily and has emerged as a key player in the control of multiple metabolic pathways. On its activation by bile acids, FXR regulates bile acid synthesis, conjugation, and transport, as well as various aspects of lipid and glucose metabolism. This review summarizes recent advances in deciphering the role of FXR in the context of hepatic lipid and glucose homeostasis and discusses the potential of FXR as a pharmacological target for therapeutic applications.

The Farnesoid X receptor (FXR) is a nuclear receptor activated by bile acids. FXR regulates bile acid synthesis, conjugation, and transport, as well as various aspects of lipid and glucose metabolism that are summarized in this review. Finally, we discussed the potential of FXR as a pharmacological target.

Key Words: bile acid • FXR • glucose metabolism • lipid • nuclear receptor

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