ESR1 binds ESR1 agonists

Stable Identifier
Reaction [binding]
Homo sapiens
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Estrogen receptor alpha (ERα, NR3A1, nuclear receptor subfamily 3 group A member 1), encoded by the ESR1 gene, is a nuclear hormone receptor that is activated by the sex hormone estrogen. ESR1 can mediate the physiological development and function of various organ systems, including the reproductive, central nervous, skeletal, and cardiovascular systems. Accordingly, ESR1 is widely expressed throughout the body.

Synthetic nonsteroidal estrogen agonists are used to treat a variety of gynecological disorders (Stauffer et al. 2000, Sasson 1991, Kuiper et al. 1997). Diethylstilbestrol was previously used in the prevention of miscarriage or premature delivery but later only used in the treatment of prostate or breast cancer. Ethinylestradiol, when combined with progestins, is mainly used as a contraceptive and for certain menopausal conditions.

Tamoxifen has mixed estrogenic and antiestrogenic activity, dependent on tissue type. For instance, tamoxifen has predominantly antiestrogenic effects in breast tissue (Wang et al. 2004) but predominantly estrogenic effects in the uterus and liver. Tamoxifen was indicated to treat estrogen receptor positive metastatic breast cancer in adults but has since been superceded by aromatase inhibitors such as anastrozole (Howell et al. 2005). A beneficial side effect of tamoxifen is that it prevents osteoporosis by acting as an agonist in bone cells (Kassem 1997). Tibolone is an estrogen receptor agonist with a preference for ESR1 (Escande et al. 2009). It is indicated for the relief of post-menopausal symptoms and for the prevention of osteoporosis.
Literature References
PubMed ID Title Journal Year
11150164 Pyrazole ligands: structure-affinity/activity relationships and estrogen receptor-alpha-selective agonists

Katzenellenbogen, BS, Tedesco, R, Katzenellenbogen, JA, Sun, J, Carlson, K, Coletta, CJ, Nishiguchi, G, Stauffer, SR

J. Med. Chem. 2000
9048584 Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta

Grandien, K, Gustafsson, JA, Nilsson, S, Enmark, E, Häggblad, J, Kuiper, GG, Carlsson, B

Endocrinology 1997
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