NCIt definition : A metabolite formed during the metabolism of 17beta-estradiol by hydroxylation of
the carbon at position 2 by the CYP450 enzymes 1A1/1A2. Theoretically, 2-hydroxyestradiol
(2-OHE2) is able to undergo redox cycling, which generates active radicals and induces
DNA damage; however, this estradiol metabolite is very unstable in vivo and is quickly
inactivated by catechol-O-methyltransferase (COMT)-mediated O-methylation and converted
to 2-methoxyestradiol (2-MeE2). 2-MeE2 exerts antineoplastic activities through its
estrogen receptor antagonistic effect and the induction of apoptosis in susceptible
cancer cells.;