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.
Bishop-Bailey
David
D
Cardiac, Vascular & Inflammation Research, William Harvey Research Institute, Barts and the London, Queen Mary University London, London, UK. d.bishop-bailey@qmul.ac.uk
D000818:Animals; D004268:DNA-Binding Proteins / Q000187:drug effects / Q000627:therapeutic use*; D016503:Drug Delivery Systems / Q000639:trends*; D006801:Humans; D018160:Receptors, Cytoplasmic and Nuclear; D014157:Transcription Factors / Q000187:drug effects / Q000627:therapeutic use*; D006113:United Kingdom; D014652:Vascular Diseases / Q000188:drug therapy* / Q000235:genetics; D000099150:Receptor, Farnesoid X-Activated
D004268:DNA-Binding Proteins; D018160:Receptors, Cytoplasmic and Nuclear; D014157:Transcription Factors; D000099150:Receptor, Farnesoid X-Activated