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Erα
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 (mainly found as a chromatin-binding protein) that is activated by the sex hormone estrogen. In humans, ERα is encoded by the gene ''ESR1'' (EStrogen Receptor 1). Structure The estrogen receptor (ER) is a ligand-activated transcription factor composed of several domains important for hormone binding, DNA binding, and activation of transcription. Alternative splicing results in several ESR1 mRNA transcripts, which differ primarily in their 5-prime untranslated regions. The translated receptors show less variability. Ligands Agonists Non-selective * Endogenous estrogens (e.g., estradiol, estrone, estriol, estetrol) * Natural estrogens (e.g., conjugated equine estrogens) * Synthetic estrogens (e.g., ethinylestradiol, diethylstilbestrol) Selective Agonists of ERα selective over ERβ in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Estrogen Receptor
Estrogen receptors (ERs) are proteins found in cell (biology), cells that function as receptor (biochemistry), receptors for the hormone estrogen (17β-estradiol). There are two main classes of ERs. The first includes the intracellular estrogen receptors, namely ERα and ERβ, which belong to the nuclear receptor family. The second class consists of membrane estrogen receptors (mERs), such as GPER (GPR30), ER-X, and Gq-mER, Gq-mER, which are primarily G protein-coupled receptors. This article focuses on the nuclear estrogen receptors (ERα and ERβ). Upon activation by estrogen, intracellular ERs undergo protein targeting, translocation to the nucleus where they bind to specific DNA sequences. As DNA-binding transcription factors, they regulate the activity of various genes. However, ERs also exhibit functions that are independent of their DNA-binding capacity. These non-genomic actions contribute to the diverse effects of estrogen signaling in cells. Estrogen receptors (ERs) b ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Estetrol
Estetrol (E4), or oestetrol, is one of the four natural estrogenic steroid hormones found in humans, along with estrone (E1), estradiol (E2), and estriol (E3). Estetrol is a major estrogen in the body. In contrast to estrone and estradiol, estetrol is a native estrogen of fetal life. Estetrol is produced exclusively by the fetal liver and is found in detectable levels only during pregnancy, with relatively high levels in the fetus and lower levels in the maternal circulation. In addition to its physiological role as a native hormone, estetrol can be used as a medication, see estetrol (medication). Estetrol, in combination with drospirenone, has recently been approved as a new estrogenic component of a combined oral contraceptive (COC) and estetrol alone is in clinical development for the treatment of menopausal symptoms as well as breast and prostate cancer. Biological function So far, the physiological function of estetrol remains unknown. The potential role of estetrol as a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Full Agonist
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist. Etymology The word originates from the Greek word (''agōnistēs''), "contestant; champion; rival" < (''agōn''), "contest, combat; exertion, struggle" < (''agō''), "I lead, lead towards, conduct; drive." Types of agonists Receptors can be activated by either agonists (such as |
D1-like Receptor
The D1-like receptors are a subfamily of dopamine receptors that bind the endogenous neurotransmitter dopamine. The D1-like subfamily consists of two G protein–coupled receptors that are coupled to Gs and mediate excitatory neurotransmission Neurotransmission (Latin: ''transmissio'' "passage, crossing" from ''transmittere'' "send, let through") is the process by which signaling molecules called neurotransmitters are released by the axon terminal of a neuron (the presynaptic neuron ..., of which include D1 and D5. For more information, please see the respective main articles of the individual subtypes: See also * D2-like receptor References Dopamine receptors {{transmembranereceptor-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SKF-82,958
SKF-82,958 is a synthetic compound of the benzazepine class that acts as a D1/ D5 receptor full agonist. SKF-82,958 and similar D1-like-selective full agonists like SKF-81,297 and 6-Br-APB produce characteristic anorectic effects, hyperactivity and self-administration in animals, with a similar but not identical profile to that of dopaminergic stimulants such as amphetamine. SKF-82,958 was also subsequently found to act as an agonist of ERα with negligible activity at ERβ, making it a subtype-selective estrogen Estrogen (also spelled oestrogen in British English; see spelling differences) is a category of sex hormone responsible for the development and regulation of the female reproductive system and secondary sex characteristics. There are three .... References 1-Phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines Synthetic estrogens Drugs developed by GSK plc D1 receptor agonists D5 receptor agonists Hydroxyarenes Chloroarenes Allyl compounds { ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ERA-63
ERA-63, also known as ORG-37663, as well as 3-methylene-7α-methyl-17α-ethynylestra-5(10)-en-17β-ol, is a synthetic, steroidal estrogen and a selective agonist of the ERα that was under development for the treatment of rheumatoid arthritis but was never marketed. The drug produced estrogenic effects but failed to show effectiveness for rheumatoid arthritis in a phase IIa clinical study. A large clinical trial also found that prinaberel (ERB-041), a selective ERβ agonist, was ineffective in the treatment of rheumatoid arthritis in spite of activity in preclinical models. See also * 16α-LE2 16α-LE2, or 16α-lactone-estradiol, also known as 3,17β-dihydroxy-19-nor-17α-pregna-1,3,5-(10)-triene-21,16α-lactone, is a synthetic compound, synthetic, steroidal estrogen featuring an estradiol core. It is a highly potent and selective agon ... * ERA-45 * GTx-758 * Methylpiperidinopyrazole * Propylpyrazoletriol References Ethynyl compounds Estranes Synthetic estrogens ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
16α-Iodo-E2
16α-Iodo-E2, or 16α-iodoestradiol, is a synthetic compound, synthetic, steroidal, potent estrogen with slight preference for the ERα over the ERβ that is used in scientific research. The KD of 16α-iodo-E2 for the ERα is 0.6 nM and for the ERβ is 0.24 nM, a 4-fold difference in affinity (pharmacology), affinity, whereas estradiol is considered to have similar affinity for the two receptor subtypes. Unlike the case of the much weaker estriol (16α-hydroxyestradiol), 16α-iodo-E2 is considered to be equipotent with estradiol in terms of estrogenic activity. Radiolabeled [16α-125I]iodo-E2 has been employed in medical imaging, imaging to study the estrogen receptor. See also * 16α-LE2 * Clomestrone * Mytatrienediol * GTx-758 References Estranes Organoiodides Synthetic estrogens {{genito-urinary-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
16α-LE2
16α-LE2, or 16α-lactone-estradiol, also known as 3,17β-dihydroxy-19-nor-17α-pregna-1,3,5-(10)-triene-21,16α-lactone, is a synthetic compound, synthetic, steroidal estrogen featuring an estradiol core. It is a highly potent and selective agonist of the ERα that is used in scientific research to study the function of the ERα. It has 265-fold higher potency (pharmacology), potency in transactivation bioassay, assays of the ERα relative to the ERβ and 70-fold preference in binding affinity for the ERα over the ERβ. In rodents, 16α-LE2 has no effect on ovarian follicle development, whereas the highly ERβ-selective agonist 8β-VE2 stimulates follicular growth and to a comparable extent as estradiol, indicating that the ERβ and not the ERα is involved in the effects of estrogen on ovarian follicles. In contrast, 16α-LE2 stimulates uterus, uterine weight, whereas 8β-VE2 has no effect, indicating that the ERα and not the ERβ is involved in the effects of estrogen on the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Propylpyrazoletriol
Propylpyrazoletriol (PPT) is a synthetic, nonsteroidal agonist of ERα with 400-fold selectivity over ERβ that is used widely in scientific research to study the function of ERα. Though originally thought to be highly selective for ERα, PPT has subsequently been found to also act as an agonist of the GPER (GPR30). See also * ERA-45 * ERA-63 ERA-63, also known as ORG-37663, as well as 3-methylene-7α-methyl-17α-ethynylestra-5(10)-en-17β-ol, is a synthetic, steroidal estrogen and a selective agonist of the ERα that was under development for the treatment of rheumatoid arthritis bu ... * GTx-758 * Methylpiperidinopyrazole (MPP) References GPER agonists Ketones 4-Hydroxyphenyl compounds Pyrazoles Synthetic estrogens {{pharmacology-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ERβ
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. In humans ERβ is encoded by the ''ESR2'' gene. Function ERβ is a member of the family of estrogen receptors and the superfamily of nuclear receptor transcription factors. The gene product contains an N-terminus, N-terminal DNA binding domain and C-terminus, 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 alpha, 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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Diethylstilbestrol
Diethylstilbestrol (DES), also known as stilbestrol or stilboestrol, is a nonsteroidal estrogen medication, which is presently rarely used. In the past, it was widely used for a variety of indications, including pregnancy support for those with a history of recurrent miscarriage, hormone therapy for menopausal symptoms and estrogen deficiency, treatment of prostate cancer and breast cancer, and other uses. By 2007, it was only used in the treatment of prostate cancer and breast cancer. In 2011, Hoover and colleagues reported adverse reproductive health outcomes linked to DES including infertility, miscarriage, ectopic pregnancy, preeclampsia, preterm birth, stillbirth, infant death, menopause prior to age 45, breast cancer, cervical cancer, and vaginal cancer. While most commonly taken by mouth, DES was available for use by other routes as well, for instance, vaginal, topical, and by injection. DES is an estrogen, or an agonist of the estrogen receptors, the biologic ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ethinylestradiol
Ethinylestradiol (EE) is an estrogen medication which is used widely in birth control pills in combination with progestins. Ethinylestradiol was widely used for various indications such as the treatment of menopausal symptoms, gynecological disorders, and certain hormone-sensitive cancers. It is usually taken by mouth but is also used as a patch and vaginal ring. The general side effects of ethinylestradiol include breast tenderness and enlargement, headache, fluid retention, and nausea among others. In males, ethinylestradiol can additionally cause breast development, feminization in general, hypogonadism, and sexual dysfunction. Rare but serious side effects include blood clots, liver damage, and cancer of the uterus. Ethinylestradiol is an estrogen, or an agonist of the estrogen receptors, the biological target of estrogens like estradiol. It is a synthetic derivative of estradiol, a natural estrogen, and differs from it in various ways. Compared to estradiol, e ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
