The hydroxylation of estradiol is one of the major routes of metabolism of the estrogen steroid hormone estradiol. It is hydroxylated into the catechol estrogens 2-hydroxyestradiol and 4-hydroxyestradiol and into estriol (16α-hydroxyestradiol). 4-hydroxyestradiol (4-OH-E2), like 2-OH-E2, can be physiologically active as well as tumorigenic. 4-OH-E2 is capable of binding estrogen receptors with a reduced dissociation rate and prolonged activation, thereby inducing cellular growth and proliferation, adenohypophyseal hormone secretion, and prostaglandin production.
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