PT - JOURNAL ARTICLE AU - Bryan Mackowiak AU - Jessica Hodge AU - Sydney Stern AU - Hongbing Wang TI - The Roles of Xenobiotic Receptors: Beyond Chemical Disposition AID - 10.1124/dmd.118.081042 DP - 2018 Jan 01 TA - Drug Metabolism and Disposition PG - dmd.118.081042 4099 - http://dmd.aspetjournals.org/content/early/2018/05/14/dmd.118.081042.short 4100 - http://dmd.aspetjournals.org/content/early/2018/05/14/dmd.118.081042.full AB - Over the past 20 years, the ability of the xenobiotic receptors to coordinate an array of drug-metabolizing enzymes and transporters in response to endogenous and exogenous stimuli has been extensively characterized and well documented. The constitutive androstane receptor (CAR) and the pregnane X receptor (PXR) are the xenobiotic receptors that have received the most attention, as they regulate the expression of numerous proteins important to drug metabolism and clearance and formulate a central defensive mechanism to protect the body against xenobiotic challenges. However, accumulating evidence has shown that these xenobiotic sensors also control many cellular processes outside of their traditional realms of xenobiotic metabolism and disposition, including physiological and/or pathophysiological responses in energy homeostasis, cell proliferation, inflammation, tissue injury and repair, immune response, and cancer development. This review will highlight recent advances in studying the non-canonical functions of xenobiotic receptors with a particular focus placed on the roles of CAR and PXR in energy homeostasis and cancer development.