Liver X receptors (LXRs) are nuclear receptors that regulate the metabolism of cholesterol and bile acids. LXRs function as nuclear cholesterol sensors that are activated in response to elevated intracellular cholesterol levels in multiple cell types.

Stimulation of LXR by agonists activates a number of genes that are involved in the regulation of lipid metabolism and cholesterol efflux from cells. The ability of LXRs to promote reverse cholesterol transport, to limit inflammation, and to improve glucose tolerance makes them attractive targets for drugs developed for the treatment of cardiovascular, metabolic, and/or inflammatory diseases. Synthetic LXR agonists promote cholesterol efflux and inhibit inflammation in vivo and inhibit the development of atherosclerosis in animal models. Unfortunately, known ligands share the undesirable side effect of inducing lipogenesis and hypertriglyceridemia by transactivating genes involved in fatty acid biosynthesis. 

1. Zelcer N, Tontonoz P. Liver X receptors as integrators of metabolic and inflammatory signaling. J Clin Invest. 2006 116(3) 607-14
2. Quinet EM, Savio DA, Halpern AR, Chen L, Miller CP, Nambi P. Gene-selective modulation by a synthetic oxysterol ligand of the liver X receptor. J Lipid Res. 2004 (10) 1929-42

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