Estrogens receptors for

The increasing clinical importance of tamoxifen in the 1980s prompted development of drugs that indirectly target the estrogen receptor, for example the aromatase inhibitor anastrozole (ARIMIDEX ), a selective inhibitor of estrogen biosynthesis [28]. Progress in treatment of hormone-dependent prostate cancer followed advances in breast cancer, with demonstration that... 

The mechanisms by which thyroid hormones enhance antidepressant activity are still unknown. It is of interest that thyroid hormone increases net activity of several neurotransmitters that are putatively involved in the pathophysiology of depression in a way that is descriptively similar to that of estrogens. Receptors for the two hormones belong to the same superfamily. As was previously mentioned [Pfaff 1996], these issues are currently being explored, and clarifications are expected shortly. 

Latonnelle, K., A. Fostier, F. Le Menn and C. Bennetau-Pelissero. Binding affinities of hepatic nuclear estrogen receptors for phytoestrogens in rainbow trout (Oncorhynchus mykiss) and Siberian sturgeon (Acipenser baeri). Gen. Comp. Endocrinol. 129 69-79, 2002. 

Jordan, V.C. and Brodie, A.M.H. (2007) Development and evolution of therapies targeted to the estrogen receptor for the treatment and prevention ofbreast cancer. Steroids, 72, 7-25. 

Leclercq G, Jacquot Y. Interactions of isoflavones and other plant derived estrogens with estrogen receptors for prevention and treatment of breast cancer—Considerations concerning related efficacy and safety. J Steroid Biochem Mol Biol. 2014 139 237-244. 

The great variety of structures that have by now been shown to exhibit estrogenic activity leads to the suspicion that the estrogen receptor may be unusually nonspecific compared to receptors for other steroid hormones. 

Although estrone and estradiol (26) have both been isolated from human urine, it has recently been shown that it is the latter that is the active compound that binds to the so-called estrogen receptor protein. Reduction of estrone with any of a large number of reducing agents (for example, any of the complex metal hydrides) leads cleanly to estradiol. This high degree of stereoselectivity to afford the product of attack at the alpha side of the molecule is characteristic of many reactions of steroids. 

EM-800 is a pure estrogen receptor antagonist that has recently been used clinically for breast cancer patients who have failed tamoxifen therapy. 

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