Liver X Receptors: Potential Novel Targets in Cardiovascular Diseases

Author(s): Dennis Bruemmer, Ronald E. Law

Journal Name: Current Drug Targets - Cardiovascular & Hematological Disorders
Continued as Cardiovascular & Hematological Disorders-Drug Targets

Volume 5 , Issue 6 , 2005


The Liver X Receptors, LXRα and LXRβ are members of the nuclear hormone receptor superfamily which have recently been implicated as novel pharmacological targets for the treatment of cardiovascular diseases. The identification of natural and synthetic ligands for LXRs and the generation of LXR-deficient mice have been crucial for our understanding of the function of these receptors and for the identification of LXR-regulated target genes, particularly with respect to the role of LXRs in regulating cholesterol homeostasis. Synthetic LXRα/β agonists induce cholesterol efflux and reverse cholesterol transport, improve glucose metabolism, inhibit macrophage-derived inflammation, and suppress the proliferation of vascular smooth muscle cells. By regulating the expression of multiple genes involved in these pathways, LXR agonists prevent the development and progression of atherosclerosis and inhibit neointima formation following angioplasty of the arterial wall. In this review, we will summarize the important roles of LXR in metabolism and vascular biology and discuss its implications as potential molecular drug target for the treatment of cardiovascular diseases.

Keywords: high-density lipoprotein, reverse cholesterol transport (RCT), LXR-deficient mice, Lipogenesis, atherosclerosis, anti-inflammatory

Rights & PermissionsPrintExport Cite as

Article Details

Year: 2005
Page: [533 - 540]
Pages: 8
DOI: 10.2174/156800605774961988
Price: $58

Article Metrics

PDF: 3