Cytochromes P450: A Structure-Based Summary of Biotransformations Using Representative Substrates

Abstract

Cytochromes P450 (CYPs) are a superfamily of enzymes that metabolize the majority of xenobiotics in humans. This review presents a structure-based outline of CYP-catalyzed biotransformations of selected substrates, representing diverse structural classes of chemicals, ranging from drugs to toxicants. Data are presented in a tabular format for easy reference, with visual representations of all substrates and sites-of-attack. The major metabolites, isozymes responsible, chemical classification, and other information related to the biotransformation are provided. Pharmacophores proposed for the major CYP isozymes are discussed. This visual combination of substrates and biotransformation sites can serve as a useful reference for researchers.

Key Words :

• Cytochrome P450
• CYP
• Biotransformation
• Xenobiotics
• Metabolism
• Isozyme
• Drug
• Toxicant.

ACKNOWLEDGMENTS

We thank Prof. Raymond S. H. Yang for his support. This work was supported in part by NIH grants NIEHS K25 ES11146 and NIEHS K25 ES12909.