Alternative splicing within the human cytochrome P450 superfamily with an emphasis on the brain: The convolution continues

Expert Opin Drug Metab Toxicol. 2006 Jun;2(3):399-418. doi: 10.1517/17425255.2.3.399.


The human cytochrome P450 (CYP) superfamily of enzymes regulate hepatic phase 1 drug metabolism and subsequently play a significant role in pharmacokinetics, drug discovery and drug development. Alternative splicing of the cytochrome CYP gene transcripts enhances gene diversity and may play a role in transcriptional regulation of certain CYP proteins. Tissue-specific alternative splicing of CYPs is significant for its potential to add greater dimension to differential drug metabolism in hepatic and extrahepatic tissues, such as the brain, and to our understanding of the CYP family. This review provides an overview of tissue-specific splicing patterns, splicing types, regulation and the functional diversities between liver and splice variant CYP proteins and further explores the relevance of tissue-specific alternative splicing of CYPs in the nervous system.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Review

MeSH terms

  • Alternative Splicing*
  • Animals
  • Brain / enzymology*
  • Cytochrome P-450 CYP1A1 / genetics
  • Cytochrome P-450 CYP1A1 / metabolism*
  • Cytochrome P-450 CYP2D6 / genetics
  • Cytochrome P-450 CYP2D6 / metabolism*
  • Cytochrome P-450 Enzyme System / genetics
  • Cytochrome P-450 Enzyme System / metabolism*
  • Gene Expression Regulation, Enzymologic*
  • Humans
  • Isoenzymes / genetics
  • Isoenzymes / metabolism
  • Liver / enzymology*
  • Polymorphism, Single Nucleotide


  • Isoenzymes
  • Cytochrome P-450 Enzyme System
  • CYP2D7 protein, human
  • Cytochrome P-450 CYP1A1
  • Cytochrome P-450 CYP2D6