Modifiers of Cytochrome(s) P450

  • John DiGiovanni
  • Heather E. Kleiner
Part of the Cancer Drug Discovery and Development book series (CDD&D)


Cytochromes P450 (CYPs) belong to a superfamily of enzymes that have different, but overlapping, substrate specificities and tissue distribution. The highest concentration of CYPs is in the liver endoplasmic reticulum, but P450 is found in most other tissues of the body. CYPs are heme-containing enzymes that can either detoxify or bioactivate xenobiotics (foreign chemicals). The following seven types of reactions are catalyzed by CYPs: i) hydroxylation of an aliphatic or aromatic carbon; ii) epoxidation of a double bond; iii) heteroatom (S-, N-, and I-) oxygenation and N-hydroxylation; iv) heteroatom (O-, S-, and N-) dealkylation; v) oxidative group transfer; vi) cleavage of esters; and vii) dehydrogenation (1). In humans, the predominant isoform of P450 in the liver is CYP1A2. Other human liver P450s include CYP 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A4 (reviewed in ref. 1). CYP 1 A 1 is expressed in extrahepatic sites including human lung, the intestines, the skin, lymphocytes, and the placenta. Human CYP 1 B 1 catalyzes the activation of a number of diverse pro-carcinogens (2), and is expressed in a variety of extra-hepatic sites, including steroid-responsive and steroidogenic tissues (3–5).


Ursolic Acid Organosulfur Compound Rosemary Extract Mouse Epidermis Diallyl Disulfide 
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© Springer Science+Business Media New York 2004

Authors and Affiliations

  • John DiGiovanni
  • Heather E. Kleiner

There are no affiliations available

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