TOXICOLOGICAL SCIENCES 120(S1), S49–S75 (2011) doi:10.1093/toxsci/kfq338 Advance Access publication November 8, 2010 Xenobiotic Metabolism, Disposition, and Regulation by Receptors: From Biochemical Phenomenon to Predictors of Major Toxicities Curtis J. Omiecinski,1 John P. Vanden Heuvel, Gary H. Perdew, and Jeffrey M. Peters Department of Veterinary and Biomedical Sciences, Center for Molecular Toxicology and Carcinogenesis, Penn State University, University Park, Pennsylvania 16802 1To whom correspondence should be addressed at Department of Veterinary and Biomedical Sciences, Center for Molecular Toxicology and Carcinogenesis, Downloaded from 101 Life Sciences Building, Penn State University, University Park, PA 16802. Fax: (814) 863-1696. E-mail:
[email protected]. Received September 1, 2010; accepted November 1, 2010 processes. Indeed, in the past 50 years, much has been gleaned To commemorate the 50th anniversary of the Society of regarding our mechanistic understanding of chemical toxicities toxsci.oxfordjournals.org Toxicology, this special edition article reviews the history and contributed by these coordinate biotransformation systems. current scope of xenobiotic metabolism and transport, with special From the early discoveries of these pathways, our scientific emphasis on the discoveries and impact of selected ‘‘xenobiotic receptors.’’ This overall research realm has witnessed dynamic perspective has witnessed extraordinary advances led by the development in the past 50 years, and several of the key milestone availability of new