Estrogen and Related Receptors

Estrogen controls many cellular processes including growth, differentiation and function of the reproductive system. In females, estrogen's main targets are the ovaries, uterus, vagina and mammary glands. In the male, target organs are the testes, prostate and epididymis. Estrogen is also responsible for the growth and maintenance of the skeleton and the normal functioning of the cardiovascular and nervous systems.

Estrogen exerts most of its actions via estrogen receptors (ER). Estrogen receptors are ligand-activated transcription factors belonging to the nuclear hormone receptor superfamily.

Today, two estrogen receptors are known, ERα and ERβ. ERα protein is highly homologous to ERβ protein, especially in the DNA and ligand binding domains, although divergence exists in the N-terminal transactivation domain. Both receptors interact with the same DNA response element and show a similar ligand binding profile. Upon ligand binding estrogen receptors undergo a conformational change allowing spontaneous dimerization to form either homo- or heterodimers. As a dimer, the estrogen receptor binds to the estrogen response element (ERE) in the promoter region of target genes. ERα and ERβ are present in a broad spectrum of tissues.

Three estrogen-related receptors (ERRs) - ERRα, ERRβ and ERRγ - have also been identified. Classified as 'orphan' nuclear receptors, they do not bind endogenous estrogens; instead, they are activated by co-regulatory proteins and bind the ERE and ERR response elements (ERREs) as homodimers, exerting transcriptional control of energy homeostasis. As a result, they may be useful therapeutic targets for metabolic diseases, such as obesity and diabetes, as well as cancer.

External sources of pharmacological information for Estrogen and Related Receptors :

• IUPHAR Receptor Code

• BJP Guide

Pathways for Estrogen and Related Receptors

Estrogen Signaling Pathway

Estrogen is a steroid hormone that is responsible for the regulation of growth, differentiation and function of the reproductive system. Estrogen signaling is often dysregulated in breast cancer and osteoporosis.

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Estrogen Receptor Gene Data