Background: PXR (Pregnane X Receptor) and CAR (Constitutive Androstane Receptor) are termed as
xenobiotic receptors, which are known as core factors in regulation of the transcription of metabolic enzymes and
drug transporters. However, accumulating evidence has shown that PXR and CAR exert their effects on energy metabolism
through the regulation of gluconeogenesis, lipogenesis and β-oxidation. Therefore, in this review, we are
trying to summary recent advances to show how xenobiotic receptors regulate energy metabolism.
Methods: A structured search of databases has been performed by using focused review topics. According to conceptual
framework, the main idea of research literature was summarized and presented.
Results: For introduction of each receptor, the general introduction and the critical functions in hepatic glucose and
lipid metabolism have been included. Recent important studies have shown that CAR acts as a negative regulator of
lipogenesis, gluconeogenesis and β -oxidation. PXR activation induces lipogenesis, inhibits gluconeogenesis and
Conclusion: In this review, the importance of xenobiotic receptors in hepatic glucose and lipid metabolism has been
confirmed. Therefore, PXR and CAR may become new therapeutic targets for metabolic syndrome, including obesity
and diabetes. However, further research is required to promote the clinical application of this new energy metabolism
function of xenobiotic receptors.