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Relative Activation of Human Pregnane X Receptor versus Constitutive Androstane Receptor Defines Distinct Classes of
 

Summary: Relative Activation of Human Pregnane X Receptor versus
Constitutive Androstane Receptor Defines Distinct Classes of
CYP2B6 and CYP3A4 Inducers
Stephanie R. Faucette, Tong-Cun Zhang, Rick Moore, Tatsuya Sueyoshi,
Curtis J. Omiecinski, Edward L. LeCluyse, Masahiko Negishi, and Hongbing Wang
Division of Molecular Pharmaceutics, School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina (S.R.F.,
T.-C.Z.); Pharmacogenetics Section, Laboratory of Reproductive and Developmental Toxicology, National Institute of
Environmental and Health Sciences, National Institutes of Health, Research Triangle Park, North Carolina (R.M., T.S., M.N.);
Center for Molecular Toxicology and Carcinogenesis, Pennsylvania State University, University Park, Pennsylvania (C.J.O.);
CellzDirect, Inc., Pittsboro, North Carolina (E.L.L.); and Department of Pharmaceutical Sciences, School of Pharmacy,
University of Maryland, Baltimore, Maryland (H.W.)
Received August 7, 2006; accepted October 11, 2006
ABSTRACT
Both the human pregnane X receptor (hPXR) and constitutive
androstane receptor (hCAR) are capable of regulating CYP3A4
and CYP2B6 gene expression. However, the majority of cur-
rently identified CYP3A4 and CYP2B6 inducers are confirmed
activators of hPXR but not hCAR. To compare these receptors
with respect to their chemical selectivities, 16 drugs known to
induce CYP3A4 and/or CYP2B expression were evaluated for

  

Source: Andrews, Anne M. - Huck Institutes of the Life Sciences, Pennsylvania State University
Omiecinski, Curtis - Department of Veterinary and Biomedical Sciences, Pennsylvania State University

 

Collections: Biology and Medicine