S. S. Ferguson, Y. Chen, E. L. LeCluyse, M. Negishi and J. A. Goldstein, “Human CYP2C8 Is Transcriptionally Regulated by the Nuclear Receptors Constitutive Androstane Receptor, Pregnane X Receptor, Glucocorticoid Receptor, and Hepatic Nuclear Factor 4α,” Molecular Pharmacology, Vol. 68, No. 3, 2005, pp. 747-757.

has been cited by the following article:

• TITLE: Induction of Cytochrome P450 2A6 by Bilirubin in Human Hepatocytes

  AUTHORS: Hiromi Tanii, Yoshihisa Shitara, Mikako Torii, Shuichi Sekine, Hiroshi Iwata, Toshiharu Horie

  KEYWORDS: CYP2A6; Hepatocytes; Hyperbilirubinemia; RT-PCR

  JOURNAL NAME: Pharmacology & Pharmacy, Vol.4 No.2, April 15, 2013

  ABSTRACT: The influence of bilirubin on mRNA expression of cytochrome P450 (CYP), UDP-glucuronosyltransferase (UGT) and nuclear receptors in human hepatocytes was investigated. The treatment of the hepatocytes with 40 μg/mL bilirubin, which corresponds to hyperbilirubinemia, resulted in 1.7-fold increase of CYP2A6 mRNA compared to the vehicle control while CYP2A6 mRNA did not change after treatment with 1 μg/mL bilirubin, corresponding to physiologically normal level. No significant change of mRNA expression by 40 μg/mL bilirubin treatment was observed for CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP3A4 and CYP3A5, UGT1A1, UGT1A3, UGT1A6, UGT2B4, UGT2B7, UGT2B10 and UGT2B15, constitutive androstane receptor (CAR), pregnane X receptor (PXR), retinoid X receptor α (RXRα) and hepatocyte nuclear factor-4α (HNF-4α). The induction profile of bilirubin was different from that of rifampicin, a typical PXR activator. This study demonstrated that CYP2A6 can be induced by bilirubin in a concentration dependent manner.