Antiestrogens. Medical search. Frequent questions

Antiestrogens include selective estrogen receptor modulators (SERMs) like tamoxifen, clomifene, and raloxifene, the ER silent antagonist and selective estrogen receptor degrader (SERD) fulvestrant, aromatase inhibitors (AIs) like anastrozole, and antigonadotropins including androgens/anabolic steroids, progestogens, and GnRH analogues. (wikipedia.org)
The absence of agonist activity may make this steroidal antiestrogen superior to tamoxifen in suppressing tumor cell growth. (regrowth.com)
To evaluate the hormonal responsiveness of tumors resistant to tamoxifen and ICI182,780, 1-mm3 segments of the tumors were transplanted onto the flanks of new recipient mice, which were then treated with estrogen or the antiestrogens-alone or in combination. (regrowth.com)
Actions of tamoxifen because they are all antiestrogens that inhibit the. (azseasonsmagazines.com)
Tamoxifen belongs to a group of drugs called antiestrogens. (azseasonsmagazines.com)
Nolvadex or Tamoxifen citrate, a non-steroidal antiestrogen for oral administration, is commonly by athletes as a post cycle therapy drug to reduce or prevent the formation of excess estrogens that can lead to oily skin, acne, fluid retention, and gynecomastia. (steroidliquid.com)

Although aromatase inhibitors and antigonadotropins can be considered antiestrogens by some definitions, they are often treated as distinct classes. (wikipedia.org)
Aromatase inhibitors and antigonadotropins reduce the production of estrogen, while the term "antiestrogen" is often reserved for agents reducing the response to estrogen. (wikipedia.org)
Antiestrogens, aromatase inhibitors, and apoptosis in breast cancer. (wikipedia.org)
There are two categories of antiestrogens: aromatase inhibitors and receptor blockers. (euroanabolex.com.mx)

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. (wikipedia.org)
The estrogen receptor (ER) is a transcription factor whose activity is normally activated by the hormone estradiol and inhibited by antiestrogen. (eurekamag.com)
The ER point mutant L540Q is activated by several antiestrogens (the more pure antiestrogens ICI 164,384 and RU 54,876 or the partial antiestrogen trans-hydroxytamoxifen) but not by estradiol. (eurekamag.com)
The introduction of two additional amino acid changes close to 540 results in receptors that are still not activated by estradiol but are now able to distinguish between partial antiestrogens (which remain agonistic) and pure antiestrogens (which show a greatly reduced stimulatory activity). (eurekamag.com)
In MCF7 and 1470 cells (but not in MDA MB-231 cells), both antiestrogens inhibited proliferation induced by acetaminophen and by estradiol. (cdc.gov)

Nolvadex is a good antiestrogen, a drug whose action prevents the formation of gynecomastia. (muscle-hunter.com)
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The first nonsteroidal antiestrogen was discovered by Lerner and coworkers in 1958. (wikipedia.org)
Toremifene is in a class of medications called nonsteroidal antiestrogens. (medlineplus.gov)

These ligand activity inversion mutants remain stable in cells in the presence of the antiestrogen ICI 164,384, as does a related ER mutant receptor that shows the normal, wild type ER ligand activity profile in which ICI 164,384 is transcriptionally inactive. (eurekamag.com)
Antiestrogens bind to estrogen receptor site on cancer cells thus blocking estrogen from going into the cancer cell. (chemocare.com)

Estrogen receptors (ER) like ERα and ERβ include activation function 1 (AF1) domain and activation function 2 (AF2) domain in which SERMS act as antagonists for the AF2 domain, while "pure" antiestrogens like ICI 182,780 and ICI 164,384 are antagonists for the AF1 and AF2 domains. (wikipedia.org)
Two antiestrogens (ICI 182,780 and 4 hydroxytamoxifen) were tested in 2 ER+ (MCF7, T47D) and 1 estrogennonresponsive, ER- (MDA-MB-231) cell lines. (cdc.gov)

In another study, one group of male mice were given a phytoecdysteroid, and another group given the popular illicit anabolic steroid, Dianabol, buy aromasin 25 mg antiestrogens aromasin. (mlgindustry.com)
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Antiestrogens are one of three types of sex hormone antagonists, the others being antiandrogens and antiprogestogens. (wikipedia.org)
Antiestrogens are used for: Estrogen deprivation therapy in the treatment of ER-positive breast cancer Ovulation induction in infertility due to anovulation Male hypogonadism Gynecomastia (breast development in men) A component of hormone replacement therapy for transgender men In women, the side effects of antiestrogens include hot flashes, osteoporosis, breast atrophy, vaginal dryness, and vaginal atrophy. (wikipedia.org)
It has been found that certain mutational changes in the activation function-2 region in the hormone-binding domain of the human ER result in ligand activity inversion mutants, i.e. receptors that are now activated by antiestrogen and inhibited by estrogen. (eurekamag.com)
An antiestrogen is a type of hormone antagonist. (adrianacristinahernandez.com)

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Antiestrogens also can reduce bloating associated with anabolic/androgenic steroid use, and may avoid health risks associated with elevated estrogen levels. (euroanabolex.com.mx)

Because of their ability to reduce risk of gynecomastia (abnormal growth of breast tissue in males) and enhance recovery of natural testosterone production after a cycle, use of antiestrogens such as aminoglutethimide (Cytadren) and clomiphene (Clomid) has become popular in bodybuilding. (euroanabolex.com.mx)

Antiestrogens are commonly used to stop steroid hormones, estrogen, from binding to the estrogen receptors leading to the decrease of estrogen levels. (wikipedia.org)
Antiestrogens act as antagonists of the estrogen receptors, ERα and ERβ. (wikipedia.org)
These findings highlight the means by which the carboxyl-terminal region in domain E functions to interpret the activity of a ligand, and they demonstrate that rather minimal changes in the ER can result in receptors with inverted response to antiestrogen and estrogen. (eurekamag.com)

however, the activating ability of antiestrogens is observed only in some cells, highlighting the important role of cell-specific factors in ligand interpretation. (eurekamag.com)
Such point mutations, if present in estrogen target cells, would result in antiestrogens being seen as growth stimulators, rather than suppressors, with potentially detrimental consequences in terms of breast cancer treatment with antiestrogens. (eurekamag.com)
Cells from men were not responsive to e2 or antiestrogens [22]. (azseasonsmagazines.com)
Effects of antiestrogens on acetaminophen-induced proliferation were assessed by flow cytometry (0/0 S phase cells) and by cell counting. (cdc.gov)

The effects of antiestrogen treatments on the process of tumorigenesis, in the absence of estrogen supplementation, were determined by initiating drug administration on the same day as tumor cell inoculation. (regrowth.com)
Crystallographic analyses reveal ligand dependent ERα conformations, characterized by specific surface docking sites for functional protein−protein interactions, whose identification is needed to understand antiestrogen effects on estrogen target tissues, in particular breast cancer (BC). (unina.it)

Dr Loibl discusses current indications for CDK 4/6 inhibitors (plus antiestrogen) as well as possible biomarkers at the 'Coming of Age for CDK 4/6 Inhibitors' symposium at ESMO 2016 . (ecancer.org)

Antiestrogens are commonly used to stop steroid hormones, estrogen, from binding to the estrogen receptors leading to the decrease of estrogen levels. (wikipedia.org)
Estrogen receptors (ER) like ERα and ERβ include activation function 1 (AF1) domain and activation function 2 (AF2) domain in which SERMS act as antagonists for the AF2 domain, while "pure" antiestrogens like ICI 182,780 and ICI 164,384 are antagonists for the AF1 and AF2 domains. (wikipedia.org)
Antiestrogens act as antagonists of the estrogen receptors, ERα and ERβ. (wikipedia.org)
At concentrations less than or equal to 4 microM, antiestrogens are also cytotoxic and they require accessible estrogen receptors for their action. (eurekamag.com)

Numerous clinically-relevant mechanisms of acquired antiestrogen resistance have been identified by in vitro studies. (elsevierpure.com)
Treatment with antibodies to HER-2/neu (Herceptin ™ ) did not affect growth of MCF-7 cells or resistant cells, indicating that in this in vitro model system, acquired antiestrogen resistance does not emerge from activation of the HER-2/neu signalling pathway. (biomedcentral.com)

2014. Hydroxychloroquine inhibits autophagy to potentiate antiestrogen responsiveness in ER+ breast cancer. (health.mil)
7:2977-87) now demonstrate that autophagy (also referred to as macroautophagy) is critical to the development of antiestrogen resistance. (elsevierpure.com)
Under conditions of compromised autophagy, including treatments with pharmacological inhibitors and RNAi targeting of the beclin 1 gene, the cytotoxicity (death-inducing effects) of the antiestrogen 4-hydroxytamoxifen (4-OHT) was significantly increased. (elsevierpure.com)
Analysis of a representative resistant cell line showed an increased ability of the cells to sustain high levels of antiestrogen-induced autophagy without progression to death. (elsevierpure.com)
These data provide strong evidence that autophagy is a key mechanism of cell survival during antiestrogen challenge and progression to antiestrogen resistance. (elsevierpure.com)
Additionally, it was known that autophagy, a process in which a cell recycles its own cytoplasmic materials, increased during antiestrogen therapies and helped cancers survive. (the-scientist.com)

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. (wikipedia.org)
This result further supports the role of estrogens in lung cancer prognosis and suggests that exposure to antiestrogens may offer some protection against tumor mortality. (medscape.com)
Molecular conformation, receptor binding, and hormone action of natural and synthetic estrogens and antiestrogens. (nih.gov)
In the presence of estrogens, antiestrogens behave as classical antihormones and their inhibition of cell proliferation is likely due to inhibition of the synthesis and release of several estrogen-induced mitogens (growth factors and proteases). (eurekamag.com)
In the absence of estrogens (cells cultured in phenol-red-free medium), antiestrogens can still inhibit the effect of growth factors (EGF, insulin). (eurekamag.com)

Antiestrogens are one of three types of sex hormone antagonists, the others being antiandrogens and antiprogestogens. (wikipedia.org)

The recent report of the structure of estrogen receptor (ER) beta with a second molecule of 4-hydroxytamoxifen (HT) bound in the coactivator-binding surface of the ligand-binding domain (LBD) represents the first direct example of a second ER ligand-binding site and provides insight into the possible origin of mixed agonist/antagonist activity of type I antiestrogens. (nih.gov)

These results indicate that subtle changes in the conformation of ERalpha upon binding to antiestrogen are at the basis of resistance to antiestrogens. (nih.gov)
A major impediment to the successful treatment of estrogen receptor α (ERα)-positive breast cancer is the development of antiestrogen resistance. (elsevierpure.com)
Development of acquired resistance against antiestrogen treatment is a serious problem in human breast cancer, and knowledge of alterations resulting in resistance is important for selection of further treatment. (biomedcentral.com)
Previous studies showed that IRF1 was downregulated in antiestrogen-resistant breast cancer cell lines, suggesting that it was the loss of IRF1's ability to induce apoptosis that led to resistance. (the-scientist.com)

Compared with the general population, the risk of developing lung cancer was 0.63 among women taking antiestrogens and 1.12 among those not taking these drugs. (medscape.com)
Antiestrogen drugs, which compete with endogenous estrogen, can prevent this. (the-scientist.com)

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Importantly, blockade of autophagosome function in the 4-OHT-treated, antiestrogen-resistant cells induced a robust death response. (elsevierpure.com)

Ask about medications such as depot leuprolide (Lupron) and antiestrogen medications used for breast cancer. (medscape.com)

However, knocking down both IRF1 and ATG7 , an experiment that mathematical modeling had suggested they try, restored antiestrogen sensitivity, which led the authors to conclude that there must be another pathway, independent of IRF1 , that can lead to apoptosis when cells are treated with antiestrogens. (the-scientist.com)

Resistant patients would benefit from treatment with other available antiestrogens. (nih.gov)
In this study, we show that overexpression of a regular component of the ERalpha transcription factor complex, cyclin D1, which occurs in approximately 40% of breast cancer patients, renders cells resistant to the new promising antiestrogen, arzoxifene. (nih.gov)
A step-wise drug selection protocol, using 4-OHT as the selecting drug, established antiestrogen-resistant breast cancer cell lines. (elsevierpure.com)
We discuss the potential benefit of blocking autophagosome function to significantly reduce the emergence of antiestrogen-resistant breast cancer cells. (elsevierpure.com)
Our antiestrogen-resistant cell lines did not express altered levels of EGFR, HER-2/neu, ErbB-3 and ErbB-4. (biomedcentral.com)
Estrogen and antiestrogen regulation of HER-2/neu expression was essentially similar in parent and resistant MCF-7 cells. (biomedcentral.com)
Stabilizing IRF1 expression might be a way to treat antiestrogen-resistant breast cancers, Clarke says. (the-scientist.com)

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Several antiestrogen compounds were studied using human breast cancer cell lines maintained in long-term tissue culture. (nih.gov)
Effects of antiestrogens on acetaminophen-induced proliferation were assessed by flow cytometry (0/0 S phase cells) and by cell counting. (cdc.gov)

Women taking antiestrogens for the prevention of breast cancer had a significantly reduced risk of dying from lung cancer, Dr. Rapiti concluded. (medscape.com)

Effect of antiestrogens. (nih.gov)
2,3,7,8-Tetrachlorodibenzo- p -dioxin as an antiestrogen: Effect on rat uterine peroxidase activity. (cdc.gov)

A variety of antiestrogens can be shown to antagonize estrogen action in animal model systems. (nih.gov)

If prospective studies confirm our results and find that antiestrogen agents improve lung cancer outcomes, this could have substantial implications for clinical practice," she said. (medscape.com)

Of these, 12 cases (and 2 deaths) were found in women taking antiestrogens and 28 cases (and 16 deaths) were found in the remaining women. (medscape.com)
Commenting on this finding, chair of the session, Patricia Ganz, MD, from the University of California in Los Angeles School of Medicine, told Medscape Oncology that the difference was not statistically significant, but that the rate was lower among women taking antiestrogens, and the "trend was clear. (medscape.com)
When the researchers calculated mortality rates from lung cancer, they found a significant decrease in the risk for death from lung cancer in women taking antiestrogens. (medscape.com)

antiestrogens that lack mixed agonist/antagonist activity. (nih.gov)

If hormones are associated with an increase in mortality from lung cancer, then maybe antiestrogens would be associated with a lower risk," Dr. Rapiti said. (medscape.com)

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