Liver X receptors (LXRs) are ligand-activated nuclear transcription factor, which play a crucial role in lipid metabolism. Recently, LXRs attracts a widely attention to us for its effects on keeping cholesterol homeostasis and anti-atherosclerosis. It might be worthy of development as a new drug target for clinic treatment. This review systematically illustrated the structure, function, and the molecular mechanism of LXRs in lipid metabolic regulation, in order to provide the principles and directions for further study.