FXR as a novel therapeutic target for vascular disease.

Diseases such as atherosclerosis involve large blood vessel narrowing and hardening, an increase in activated and inflammatory cells, and an accumulation of lipids such as cholesterol. The farnesoid X receptor (FXR) is a recently identified steroid-like receptor. Bile acids are FXR ligands, which use FXR feedback to limit their own biosynthesis in the liver from cholesterol. FXR ligands have been proposed as novel targets in cardiovascular disease, as they affect lipid metabolism in the liver and gastrointestinal tract and lower circulating triglycerides and cholesterol. Recent evidence also suggests that FXR is expressed in the vasculature, implicating FXR as a novel potential 'direct' target for cardiovascular diseases. This review aims to introduce the FXR literature and discuss the mechanisms by which FXR may both directly and indirectly affect the progression of cardiovascular disease. (c) 2004 Prous Science. All rights reserved.