A report on Estradiol and Estrogen receptor

Human steroidogenesis, showing estradiol at bottom right.

A dimer of the ligand-binding region of ERβ (PDB rendering based on ).

Estradiol levels across the menstrual cycle in 36 normally cycling, ovulatory women, based on 956 specimens. The horizontal dashed lines are the mean integrated levels for each curve. The vertical dashed line in the center is mid-cycle.

The domain structures of ERα and ERβ, including some of the known phosphorylation sites involved in ligand-independent regulation.

A dimer of the ligand-binding region of ERα (PDB rendering based on ).

They are receptors that are activated by the hormone estrogen (17β-estradiol).

- Estrogen receptor

The estrogen receptor, as well as the progesterone receptor, have been detected in the skin, including in keratinocytes and fibroblasts.

- Estradiol

8 related topics with Alpha

Estrone

6 links

Steroid, a weak estrogen, and a minor female sex hormone.

It is one of three major endogenous estrogens, the others being estradiol and estriol.

Estrone is an estrogen, specifically an agonist of the estrogen receptors ERα and ERβ.

Estriol

5 links

Steroid, a weak estrogen, and a minor female sex hormone.

It is one of three major endogenous estrogens, the others being estradiol and estrone.

Estriol is an estrogen, specifically an agonist of the estrogen receptors ERα and ERβ.

Estrogen

4 links

Category of sex hormone responsible for the development and regulation of the female reproductive system and secondary sex characteristics.

Reference ranges for the blood content of estradiol, the primary type of estrogen, during the menstrual cycle.

Steroidogenesis, showing estrogens at bottom right as in pink triangle.

There are three major endogenous estrogens that have estrogenic hormonal activity: estrone (E1), estradiol (E2), and estriol (E3).

Once inside the cell, they bind to and activate estrogen receptors (ERs) which in turn modulate the expression of many genes.

Estrogen receptor alpha (ERα), also known as NR3A1 (nuclear receptor subfamily 3, group A, member 1), is one of two main types of estrogen receptor, a nuclear receptor that is activated by the sex hormone estrogen.

Endogenous estrogens (e.g., estradiol, estrone, estriol, estetrol)

GPER

3 links

Protein that in humans is encoded by the GPER gene.

GPER binds to and is activated by the female sex hormone estradiol and is responsible for some of the rapid effects that estradiol has on cells.

The classical estrogen receptors first characterized in 1958 are water-soluble proteins located in the interior of cells that are activated by estrogenenic hormones such as estradiol and several of its metabolites such as estrone or estriol.

Estrogen receptor beta

3 links

Estrogen receptor beta (ERβ) also known as NR3A2 (nuclear receptor subfamily 3, group A, member 2) is one of two main types of estrogen receptor—a nuclear receptor which is activated by the sex hormone estrogen.

Whereas mammary ERα in rhesus macaques is downregulated in response to increased estradiol levels, expression of ERβ in the mammary glands is not.

Aromatase

2 links

Enzyme responsible for a key step in the biosynthesis of estrogens.

It catalyzes the last steps of estrogen biosynthesis from androgens (specifically, it transforms androstenedione to estrone and testosterone to estradiol).

Aromatase inhibitors, which stop the production of estrogen in postmenopausal women, have become useful in the management of patients with breast cancer whose lesion was found to be estrogen receptor positive.

Nuclear receptor

0 links

In the field of molecular biology, nuclear receptors are a class of proteins responsible for sensing steroids, thyroid hormones, cholesterol, and vitamins.

Structures of selected endogenous nuclear receptor ligands and the name of the receptor that each binds to.

Mechanism of class I nuclear receptor action. A class I nuclear receptor (NR), in the absence of ligand, is located in the cytosol. Hormone binding to the NR triggers dissociation of heat shock proteins (HSP), dimerization, and translocation to the nucleus, where the NR binds to a specific sequence of DNA known as a hormone response element (HRE). The nuclear receptor DNA complex in turn recruits other proteins that are responsible for transcription of downstream DNA into mRNA, which is eventually translated into protein, which results in a change in cell function.

Mechanism of class II nuclear receptor action. A class II nuclear receptor (NR), regardless of ligand-binding status, is located in the nucleus bound to DNA. For the purpose of illustration, the nuclear receptor shown here is the thyroid hormone receptor (TR) heterodimerized to the RXR. In the absence of ligand, the TR is bound to corepressor protein. Ligand binding to TR causes a dissociation of corepressor and recruitment of coactivator protein, which, in turn, recruits additional proteins such as RNA polymerase that are responsible for transcription of downstream DNA into RNA and eventually protein.

Structural basis for the mechanism of nuclear receptor agonist and antagonist action. The structures shown here are of the ligand binding domain (LBD) of the estrogen receptor (green cartoon diagram) complexed with either the agonist diethylstilbestrol (top, ) or antagonist 4-hydroxytamoxifen (bottom, ). The ligands are depicted as space filling spheres (white = carbon, red = oxygen). When an agonist is bound to a nuclear receptor, the C-terminal alpha helix of the LDB (H12; light blue) is positioned such that a coactivator protein (red) can bind to the surface of the LBD. Shown here is just a small part of the coactivator protein, the so-called NR box containing the LXXLL amino acid sequence motif. Antagonists occupy the same ligand binding cavity of the nuclear receptor. However antagonist ligands in addition have a sidechain extension which sterically displaces H12 to occupy roughly the same position in space as coactivators bind. Hence coactivator binding to the LBD is blocked.

Phylogenetic tree of human nuclear receptors

Type I nuclear receptors include members of subfamily 3, such as the androgen receptor, estrogen receptors, glucocorticoid receptor, and progesterone receptor.

The activity of endogenous ligands (such as the hormones estradiol and testosterone) when bound to their cognate nuclear receptors is normally to upregulate gene expression.