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

Membrane estrogen receptor

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Membrane estrogen receptors (mERs) are a group of receptors which bind estrogen.

Membrane estrogen receptors (mERs) are a group of receptors which bind estrogen.

Unlike the estrogen receptor (ER), a nuclear receptor which mediates its effects via genomic mechanisms, mERs are cell surface receptors which rapidly alter cell signaling via modulation of intracellular signaling cascades.

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Phytoestrogen

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Plant-derived xenoestrogen not generated within the endocrine system, but consumed by eating phytoestrogenic plants.

Plant-derived xenoestrogen not generated within the endocrine system, but consumed by eating phytoestrogenic plants.

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Phytoestrogens exert their effects primarily through binding to estrogen receptors (ER).

Estradiol, the main active form of estrone sulfate and the major active estrogen with CEEs.

Conjugated estrogens

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Estrogen medication which is used in menopausal hormone therapy and for various other indications.

Estrogen medication which is used in menopausal hormone therapy and for various other indications.

Estradiol, the main active form of estrone sulfate and the major active estrogen with CEEs.
17β-Dihydroequilin, the main active form of equilin sulfate and the second major active estrogen with CEEs.
Testosterone levels with no treatment and with various estrogens in men with prostate cancer. Determinations were made with an early radioimmunoassay (RIA). Source was Shearer et al. (1973).

CEEs are estrogens, or agonists of the estrogen receptor, the biological target of estrogens like estradiol.

crystal structure of the human androgen receptor ligand binding domain bound with an androgen receptor nh2-terminal peptide, ar20-30, and r1881

Androgen receptor

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Type of nuclear receptor that is activated by binding any of the androgenic hormones, including testosterone and dihydrotestosterone in the cytoplasm and then translocating into the nucleus.

Type of nuclear receptor that is activated by binding any of the androgenic hormones, including testosterone and dihydrotestosterone in the cytoplasm and then translocating into the nucleus.

crystal structure of the human androgen receptor ligand binding domain bound with an androgen receptor nh2-terminal peptide, ar20-30, and r1881
Normal function of the androgen receptor. Testosterone (T) enters the cell and, if 5-alpha-reductase is present, is converted into dihydrotestosterone (DHT). Upon steroid binding, the androgen receptor (AR) undergoes a conformational change and releases heat-shock proteins (hsps). Phosphorylation (P) occurs before or after steroid binding. The AR translocates to the nucleus where dimerization, DNA binding, and the recruitment of coactivators occur. Target genes are transcribed (mRNA) and translated into proteins.
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As has been also found for other steroid hormone receptors such as estrogen receptors, androgen receptors can have actions that are independent of their interactions with DNA.

Fulvestrant

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Medication used to treat hormone receptor -positive metastatic breast cancer in postmenopausal women with disease progression as well as HR-positive, HER2-negative advanced breast cancer in combination with palbociclib in women with disease progression after endocrine therapy.

Medication used to treat hormone receptor -positive metastatic breast cancer in postmenopausal women with disease progression as well as HR-positive, HER2-negative advanced breast cancer in combination with palbociclib in women with disease progression after endocrine therapy.

It works by binding to the estrogen receptor and destabilizing it, causing the cell's normal protein degradation processes to destroy it.

Location of the human hypothalamus

Hypothalamus

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Portion of the brain that contains a number of small nuclei with a variety of functions.

Portion of the brain that contains a number of small nuclei with a variety of functions.

Location of the human hypothalamus
Median sagittal section of brain of human embryo of three months
Endocrine glands in the human head and neck and their hormones
Cross-section of the monkey hypothalamus displays two of the major hypothalamic nuclei on either side of the fluid-filled third ventricle.
Hypothalamic nuclei
Hypothalamic nuclei on one side of the hypothalamus, shown in a 3-D computer reconstruction<ref>Brain Research Bulletin 35:323–327, 1994</ref>
Human brain left dissected midsagittal view
Location of the hypothalamus

Estrogen receptor (ER) has been shown to transactivate other transcription factors in this manner, despite the absence of an estrogen response element (ERE) in the proximal promoter region of the gene.

Anastrozole, a non steroidal aromatase inhibitor and a widely used drug in the treatment of breast cancer.

Aromatase inhibitor

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Aromatase inhibitors (AIs) are a class of drugs used in the treatment of breast cancer in postmenopausal women and in men, and gynecomastia in men.

Aromatase inhibitors (AIs) are a class of drugs used in the treatment of breast cancer in postmenopausal women and in men, and gynecomastia in men.

Anastrozole, a non steroidal aromatase inhibitor and a widely used drug in the treatment of breast cancer.
Often used as a cancer treatment in postmenopausal women, AIs work by blocking the conversion of androstenedione and testosterone into estrone and estradiol, respectively, which are both crucial to the growth of developing breast cancers (AIs are also effective at treating ovarian cancer, but less commonly so). In the diagram, the adrenal gland (1) releases androstenedione (3) while the ovaries (2) secrete testosterone (4). Both hormones travel to peripheral tissues or a breast cell (5), where they would be converted into estrone (8) or estradiol (9) if not for AIs (7), which prevent the enzyme CYP19A1 (also known as aromatase or estrogen synthase) (6) from catalyzing the reaction that turns androstenedione and testosterone into estrone and estradiol. In the diagram, Part A represents the successful conversion of androstenedione and testosterone into estrone and estradiol in the liver. Part B represents the blockage of this conversion by aromatase inhibitors both in peripheral tissues and in the breast tumor itself.
Arimidex (anastrozole) 1 mg tablets

Tamoxifen (a SERM) traditionally was the drug treatment of choice, but the ATAC trial (Arimidex, Tamoxifen, Alone or in Combination) showed that in women with localized estrogen receptor-positive breast cancer, women receiving the AI anastrozole had better results than the tamoxifen group.

Anastrozole

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Medication used in addition to other treatments for breast cancer.

Medication used in addition to other treatments for breast cancer.

The trial suggested that anastrozole is the preferred medical therapy for postmenopausal women with localized estrogen receptor-positive breast cancer.

Signal molecule binds to its hormone receptor, inducing a conformational change in the receptor to begin a signaling cascade that induces a cellular response.

Hormone receptor

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Receptor molecule that binds to a specific hormone.

Receptor molecule that binds to a specific hormone.

Signal molecule binds to its hormone receptor, inducing a conformational change in the receptor to begin a signaling cascade that induces a cellular response.

These receptors include those for glucocorticoids (glucocorticoid receptors), estrogens (estrogen receptors), androgens (androgen receptors), thyroid hormone (T3) (thyroid hormone receptors), calcitriol (the active form of vitamin D) (calcitriol receptors), and the retinoids (vitamin A) (retinoid receptors).

PELP-1

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Protein that in humans is encoded by the PELP1 gene.

Protein that in humans is encoded by the PELP1 gene.

is a transcriptional corepressor for nuclear receptors such as glucocorticoid receptors and a coactivator for estrogen receptors.