Encyclopedia of Molecular Pharmacology

Living Edition
| Editors: Stefan Offermanns, Walter Rosenthal

Nuclear Receptor Regulation of Hepatic Cytochrome P450 Enzymes

Living reference work entry
DOI: https://doi.org/10.1007/978-3-030-21573-6_234-1

Glossary Terms

Cytochrome P450 (CYP)

Family of hemeprotein monooxygenase enzymes that plays a central role in the oxidative metabolism of structurally diverse lipophilic steroids, fatty acids, drugs, and environmental chemicals. P450-catalyzed biotransformation of drugs is primarily carried out by 10–15 distinct human P450 enzymes, each encoded by a separate P450 gene.

Lithocholic acid

3α-hydroxy-5β-cholanoic acid, a hepatotoxic and cholestatic secondary bile acid which is formed by bacterial dehydroxylation of primary bile acids in the intestine.

Orphan nuclear receptor

Receptor protein belonging to the nuclear receptor superfamily whose physiological ligand has not been identified.

P450 induction

The process whereby cellular and tissue levels of one or more cytochrome P450 enzymes are increased in response to treatment of cells, or a whole organism, with certain drugs or environmental chemicals referred to as P450 inducers. P450 induction leads to an increase in the cell’s capacity...


Drug-metabolizing enzymes Enzyme induction Gene regulation Receptor activation Receptor pharmacology 
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Supported in part by NIH grant ES024421 (D.J.W.) and the Natural Sciences and Engineering Research Council of Canada Discovery Grants Program, RGPIN-2019-05254 (T.K.H.C.).


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Authors and Affiliations

  1. 1.Department of Biology and Bioinformatics ProgramBoston UniversityBostonUSA
  2. 2.Faculty of Pharmaceutical SciencesThe University of British ColumbiaVancouverCanada