Sulfotransferase genes: Regulation by nuclear receptors in response to xeno/endo-biotics

Susumu Kodama, Masahiko Negishi

Research output: Contribution to journalReview articlepeer-review

29 Citations (Scopus)


Pregnane X receptor (PXR) and constitutive active/androstane receptor (CAR), members of the nuclear receptor superfamily, are two major xeno-sensing transcription factors. They can be activated by a broad range of lipophilic xenobiotics including therapeutics drugs. In addition to xenobiotics, endogenous compounds such as steroid hormones and bile acids can also activate PXR and/or CAR. These nuclear receptors regulate genes that encode enzymes and transporters that metabolize and excrete both xenobiotics and endobiotics. Sulfotransferases (SULTs) are a group of these enzymes and sulfate xenobiotics for detoxification. In general, inactivation by sulfation constitutes the mechanism to maintain homeostasis of endobiotics. Thus, deciphering the molecular mechanism by which PXR and CAR regulate SULT genes is critical for understanding the roles of SULTs in the alterations of physiological and pathophysiological processes caused by drug treatment or environmental exposures.

Original languageEnglish
Pages (from-to)441-449
Number of pages9
JournalDrug Metabolism Reviews
Issue number4
Publication statusPublished - Nov 2013
Externally publishedYes


  • Constitutive active/androstane receptor
  • Gene regulation
  • Pregnane X receptor
  • Sulfotransferase
  • Xeno-sensing nuclear receptor

ASJC Scopus subject areas

  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Pharmacology (medical)


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