Metabolism-based drug-drug interactions and drug-induced liver toxicity are major concerns in both drug development and clinical practice. Alteration of hepatic drug-metabolizing enzymes and transporters represents the basis for many of these drug-drug interactions and hepatotoxicities. During the past two decades, accumulating evidence has revealed that xenobiotic receptors, such as the constitutive androstane receptor (CAR), the pregnane X receptor (PXR), and the aryl hydrocarbon receptor (AhR), significantly contribute to the transcriptional regulation of many drug-metabolizing enzymes and transporters. Our laboratory is interested in studying both the regulation and function of drug-metabolizing/detoxifying enzymes and transporters in the human liver. Our specific research interests are centered on the molecular mechanisms of xenobiotic receptor-mediated transcriptional regulation of cytochrome P450s and uptake/efflux transporters in the human liver, the roles of specific P450s (e.g. CYP2B6 and CYP3A4) and/or transporters (e.g. BCRP and BSEP) in drug-induced liver toxicity, and the effects of xenobiotic receptors on energy homeostasis and cell proliferation. Primary human hepatocytes, cancer cell lines, nude mice, and transgenic animals have been utilized as major models in the laboratory to predict metabolism-mediated drug-drug interactions and cytotoxicities, nuclear receptor-regulated species-specific enzyme induction, and energy metabolism. Our research projects include aspects of cellular biology, molecular biology, toxicology, and metabolism while utilizing a wide variety of techniques ranging from subcellular approaches to the use of entire animals.