The Liver X receptor-like (LXR) family of NRs (Nuclear, Class 1, Thyroid Hormone Receptor-like) hosts 3 members, including the Farnesoid X receptor (FXR). High expression of LXRα is restricted to spleen, liver, adipose tissue, intestine, kidney and lung whereas LXRβ is expressed in all tissues examined. Upon ligand-induced activation both isoforms form obligate heterodimers with the retinoid X receptor (RXR) and regulate gene expression through binding to LXR response elements (LXREs) in the promoter regions of the target genes. Identification of oxysterols as endogenous LXR ligands pointed to a role for these receptors in regulating expression of genes involved in cholesterol homeostasis, and lead to the hypothesis that activation of these receptors might have an antiatherosclerotic effect. The FXR, besides a key regulator of cholesterol homeostasis like the LXRs, is also involved in triglyceride synthesis and lipogenesis. Since the recognition that FXR has a significant role in the regulation of bile acids, numerous efforts have been undertaken to search for and design potent and selective FXR agonists.