P450 enzymes of estrogen metabolism

Pharmacol Ther. Feb-Mar 1993;57(2-3):237-57. doi: 10.1016/0163-7258(93)90057-k.

Abstract

Endogenous and exogenous estrogens undergo extensive oxidative metabolism by specific cytochrome P450 enzymes. Certain drugs and xenobiotics have been found to be potent inducers of estrogen hydroxylating enzymes with C-2 hydroxylase induction being greater than that of C-16 hydroxylase. Oxygenated estrogen metabolites have different biological activities, with C-2 metabolites having limited or no activity and C-4 and C-16 metabolites having similar potency to estradiol. Pathophysiological roles for some of the oxygenated estrogen metabolites have been proposed, e.g. 16 alpha-hydroxyestrone and 4-hydroxyestrone. These reactive estrogens are capable of damaging cellular proteins and DNA and may be carcinogenic in specific cells.

Publication types

  • Review

MeSH terms

  • Animals
  • Cytochrome P-450 Enzyme System / metabolism*
  • Estrogens / metabolism*
  • Humans
  • Rats

Substances

  • Estrogens
  • Cytochrome P-450 Enzyme System