Activation of procarcinogens by human cytochrome P450 enzymes.
Enzymatic transformation of most chemical carcinogens is requisite to the formation of electrophiles that cause genotoxicity, and the cytochrome P450 (P450) enzymes are the most prominent enzymes involved in such activation reactions. During the past 15 years the human P450 enzymes have been extensively characterized. Considerable evidence exists that the variation in activity of these enzymes can have important consequences in the actions of drugs. Other studies have been concerned with the activation of procarcinogens by human P450s. Assignments of roles of particular P450s in the metabolism of chemical carcinogens are discussed, along with the current state of evidence for relationships of particular P450s with human cancer.
Department of Biochemistry and Center in Molecular Toxicology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA. guengerich@toxicology.mc.vanderbilt.edu
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D000818:Animals; D001711:Biotransformation; D002273:Carcinogens / Q000009:adverse effects / Q000378:metabolism* / Q000633:toxicity; D003577:Cytochrome P-450 Enzyme System / Q000378:metabolism* / Q000502:physiology; D006801:Humans; D011355:Prodrugs / Q000009:adverse effects / Q000378:metabolism* / Q000633:toxicity
D002273:Carcinogens; D011355:Prodrugs; D003577:Cytochrome P-450 Enzyme System