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[1]. The FXR, besides a key regulator of cholesterol homeostasis like the LXRs, is also involved in triglyceride synthesis and lipogenesis[2]. 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.