A report on Estrogen receptor

A dimer of the ligand-binding region of ERβ (PDB rendering based on ).
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 ).
Nolvadex (tamoxifen) 20 mg
Arimidex (anastrozole) 1 mg

Estrogen receptors (ERs) are a group of proteins found inside cells.

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

42 related topics with Alpha

Overall

Estrogen receptor alpha

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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.

Estrogen receptor beta

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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.

Estradiol, the major estrogen sex hormone in humans and a widely used medication.

Estrogen

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

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

Estradiol, the major estrogen sex hormone in humans and a widely used medication.
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.

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

GPER

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Protein that in humans is encoded by the GPER gene.

Protein that in humans is encoded by the GPER gene.

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.

Nolvadex (tamoxifen) 20 mg tablets.

Tamoxifen

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Selective estrogen receptor modulator used to prevent breast cancer in women and treat breast cancer in women and men.

Selective estrogen receptor modulator used to prevent breast cancer in women and treat breast cancer in women and men.

Nolvadex (tamoxifen) 20 mg tablets.
Crystallographic structure of afimoxifene (carbon = white, oxygen = red, nitrogen = blue) complexed with ligand binding domain of estrogen receptor alpha (ERα) (cyan ribbon).

Tamoxifen is used for the treatment of both early and advanced estrogen receptor-positive (ER-positive or ER+) breast cancer in pre- and postmenopausal women.

Tamoxifen, a nonsteroidal triphenylethylene antiestrogen and a widely used drug in the treatment of breast cancer.

Selective estrogen receptor modulator

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Tamoxifen, a nonsteroidal triphenylethylene antiestrogen and a widely used drug in the treatment of breast cancer.
Figure 2: Nolvadex (tamoxifen) 20-milligram tablets (UK)
Figure 3: The domain structures of ERα and ERβ, including some of the known phosphorylation sites involved in ligand-independent regulation.
Figure 4: Structural basis for the mechanism of estrogen 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 LBD (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.
Figure 5: 4-hydroxytamoxifen (red) overlaid with 17β-estradiol (black)
Figure 6: Trans-form of clomifene with the triphenylethylene structure in red.
Figure 8: Chemical structure of toremifene
Figure 9: Raloxifene has a benzothiophene group (red) and is connected with a flexible carbonyl hinge to a phenyl 4-piperidinoethoxy side chain (green).
Figure 10: Chemical structure of nafoxidine with the dihydronapthalene group in red.
Figure 11: Chemical structure of lasofoxifene shows cis-oriented phenyls.
Figure 12: Bazedoxifene includes an indole system (red) which is connected to an amine through a benzyloxyethyl chain (green).
Figure 13: Chemical structure of ospemifene. Ethoxy side chain ends with a hydroxy group (red) instead of a dimethylamino group as with first-generation SERMs.
Figure 14: The ABCD steroid ring system in 17β-estradiol.
Figure 15: "A ring" (A) and "D ring" (D) marked in raloxifene.

Selective estrogen receptor modulators (SERMs), also known as estrogen receptor agonist/antagonists (ERAAs), are a class of drugs that act on the estrogen receptor (ER).

A bottle of raloxifene.

Raloxifene

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Medication used to prevent and treat osteoporosis in postmenopausal women and those on glucocorticoids.

Medication used to prevent and treat osteoporosis in postmenopausal women and those on glucocorticoids.

A bottle of raloxifene.

Raloxifene is a selective estrogen receptor modulator (SERM) and therefore a mixed agonist–antagonist of the estrogen receptor (ER).

Human steroidogenesis, showing estradiol at bottom right.

Estradiol

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Estrogen steroid hormone and the major female sex hormone.

Estrogen steroid hormone and the major female sex hormone.

Human steroidogenesis, showing estradiol at bottom right.
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 estrogen receptor, as well as the progesterone receptor, have been detected in the skin, including in keratinocytes and fibroblasts.

Fulvestrant, a steroidal antiestrogen and a drug used in the treatment of breast cancer.

Antiestrogen

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Antiestrogens, also known as estrogen antagonists or estrogen blockers, are a class of drugs which prevent estrogens like estradiol from mediating their biological effects in the body.

Antiestrogens, also known as estrogen antagonists or estrogen blockers, are a class of drugs which prevent estrogens like estradiol from mediating their biological effects in the body.

Fulvestrant, a steroidal antiestrogen and a drug used in the treatment of breast cancer.

They act by blocking the estrogen receptor (ER) and/or inhibiting or suppressing estrogen production.

Comprehensive overview of steroidogenesis, showing estrone on the lower right among the estrogens.

Estrone

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

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

Comprehensive overview of steroidogenesis, showing estrone on the lower right among the estrogens.

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