Estrogen receptor beta

Function

ER-β is a member of the family of estrogen receptors and the superfamily of nuclear receptor transcription factors. The gene product contains an N-terminal DNA binding domain and C-terminal ligand binding domain and is localized to the nucleus, cytoplasm, and mitochondria. Upon binding to 17-β-estradiol, estriol or related ligands, the encoded protein forms homo-dimers or hetero-dimers with estrogen receptor α that interact with specific DNA sequences to activate transcription. Some isoforms dominantly inhibit the activity of other estrogen receptor family members. Several alternatively spliced transcript variants of this gene have been described, but the full-length nature of some of these variants has not been fully characterized.

ER-β may have anti-proliferative effects and therefore oppose the actions of ERα in reproductive tissue. ER-β may also have an important role in adaptive function of the lung during pregnancy.

ER-β is a potent tumor suppressor and plays a crucial role in many cancer types such as prostate cancer.

Tissue distribution

ER-β is expressed by many tissues including the uterus, blood monocytes and tissue macrophages, colonic and pulmonary epithelial cells and in prostatic epithelium and in malignant counterparts of these tissues. Also, ER-β is found throughout the brain at different concentrations in different neuron clusters.

ER-β abnormalities

ER-β function is related to various cardiovascular targets including ATP-binding cassette transporter A1 (ABCA1) and apolipoprotein A1 (ApoA-1). Polymorphism may affect ER-β function and lead to altered responses in postmenopausal women receiving hormone replacement therapy.

Agonists

Agonists of ER-β selective over ERα include:

Antagonists

Antagonists of ER-β selective over ERα include:

Interactions

Estrogen receptor beta has been shown to interact with: