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Ligand

Estrogens (ER)

Estrogens (AmE), oestrogens (BE), or œstrogens, are a group of steroid compounds, named for their importance in the estrous cycle, and functioning as the primary

female sex hormone. Their name comes from estrus/oistros (period of fertility for female mammals) + gen/gonos = to generate.

Estrogens are synthesized in all vertebrates as well as some insects. The presence of these steroids in both vertebrate and insects suggests that estrogenic sex hormones have an ancient history.

Estrogens are used as part of some oral contraceptives, in estrogen replacement therapy for postmenopausal women, and in hormone replacement therapy for trans women.

Like inside the cell, they bind to and activate estrogen receptors which in turn modulate the G protein-coupled receptor, GPR30.

Physiological effects of ER

In the absence of hormone, estrogen receptors are largely located in the cytosol. Hormone binding to the receptor triggers a number of events starting with migration of the receptor from the cytosol into the nucleus, dimerization of the receptor, and subsequent binding of the receptor dimer to specific sequences of DNA. Some of the effects in humans: Createing proliferative endometrium,breast cell stimulation, increased body fat and weight gain, salt and fluid retention, increased risk of blood clots.

Potential applications

ER LBD can be fused with different DBDs in order to get heterogenous composite nuclear receptors activating gene expression depending on the binding site of the fused DBD.

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