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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), reactions which are catalyzed by cytochrome P450 enzymes predominantly in the liver , but also in ...
ERα and ERβ also mediate Selective estrogen-receptor modulators' (SERMs') function, [17] but the selective ERα agitator can always cause some side effects such as breast cancer or endometrial hyperplasia, while the selective ERβ agitator may play an active effect on such diseases. So, the selective ERβ agitator has more clinical value for ...
Signs of hyperestrogenism may include heightened levels of one or more of the estrogen sex hormones (usually estradiol and/or estrone), lowered levels of follicle-stimulating hormone and/or luteinizing hormone (due to suppression of the hypothalamic–pituitary–gonadal axis by estrogen), and lowered levels of androgens such as testosterone (generally only relevant to males). [1]
[6] [11] When incubated at very high concentrations or in combination with a catechol O-methyltransferase (COMT) inhibitor to prevent its metabolism, 2-hydroxyestrone shows antiestrogenic effects in estrogen receptor-positive human breast cancer cells. [12] [13] 2-Hydroxyestrone dissociates from the estrogen receptors much more rapidly than ...
The steroid is only very weakly estrogenic, and is able to antagonize the estrogenic effects of estradiol, indicating that its intrinsic activity at the estrogen receptor is less than that of estradiol and hence that it possesses the profile of a selective estrogen receptor modulator. [1] It shows estrogenic activity in human breast cancer ...
Aromatase excess syndrome (AES or AEXS) is a rarely diagnosed genetic and endocrine syndrome which is characterized by an overexpression of aromatase, the enzyme responsible for the biosynthesis of the estrogen sex hormones from the androgens, in turn resulting in excessive levels of circulating estrogens and, accordingly, symptoms of hyperestrogenism.
Hypertryptophanemia is a rare autosomal recessive [2] metabolic disorder that results in a massive buildup of the amino acid tryptophan in the blood, with associated symptoms and tryptophanuria (-uria denotes 'in the urine'). [3] [4] Elevated levels of tryptophan are also seen in Hartnup disease, [5] a disorder of amino acid transport. [6]
Other side effects of estrogens include an increased risk of blood clots, cardiovascular disease, and, when combined with most progestogens, breast cancer. [1] In men, estrogens can cause breast development , feminization , infertility , low testosterone levels , and sexual dysfunction among others.