AnatomyOrganismsDiseasesChemicals and DrugsAnalytical, Diagnostic and Therapeutic Techniques and EquipmentPhenomena and ProcessesDisciplines and OccupationsInformation ScienceHealth Care
Selective Estrogen Receptor ModulatorsEstrogensRaloxifeneReceptors, EstrogenEstrogen Receptor alphaEstrogen Receptor betaTamoxifenEstradiolEstrogens, Conjugated (USP)Breast NeoplasmsEstrogen AntagonistsOvariectomyEstrogen Receptor ModulatorsThiophenesTetrahydronaphthalenesAromatase InhibitorsEstrogens, CatecholOsteoporosis, PostmenopausalPyrrolidinesEstrogens, Non-SteroidalAntineoplastic Agents, HormonalPiperidinesOsteoporosisEstradiol CongenersAromataseReceptors, ProgesteroneDiethylstilbestrolUterusEstroneClinical Trials as TopicIndolesDose-Response Relationship, DrugPostmenopauseProgesteroneEthinyl EstradiolProgestinsPhytoestrogensNeoplasms, Hormone-DependentRNA, MessengerHydroxyestronesMenopauseVitellogeninsCell Line, TumorNafoxidineCastrationGonadal Steroid HormonesTestosteroneImmunohistochemistryMedroxyprogesterone AcetatePhenolsBenzhydryl CompoundsIsoflavonesSignal TransductionRats, Sprague-DawleyResponse ElementsReceptors, EstradiolGene Expression RegulationTranscription, GeneticSex CharacteristicsEndocrine DisruptorsAndrogensGene Expression Regulation, NeoplasticEndometriumReverse Transcriptase Polymerase Chain ReactionReceptors, AndrogenTumor Cells, CulturedOvaryBreastEstrous CycleHormone Replacement TherapyOviductsPremenopauseEquileninDrug ImplantsPregnancyCell ProliferationDihydrotestosteronePromoter Regions, GeneticHexestrolEndometrial NeoplasmsMenstrual CycleMedroxyprogesteroneTranscriptional ActivationCells, CulturedMammary Neoplasms, ExperimentalReceptor, erbB-2Blotting, WesternPlant PreparationsCell DivisionEstradiol DehydrogenasesMCF-7 CellsTime FactorsLigands17-Hydroxysteroid DehydrogenasesOrgan SizeProlactinGene ExpressionMammary Glands, AnimalTransfectionCell Nucleus
ModulatorsTamoxifenRaloxifeneMenopauseAntagonistsSERMAromatase inhibitorsOsteoporosisPhytoestrogensAgonistsRisk of oestrogenBlock estrogenPostmenopausalEvistaOvariesMenopausal hormone therapyStimulateBindBindsTranscriptionalVaginal drynessResponse to estrogenUterusBehaveTissue selective estrogenDecreaseBazedoxifeneHormonalPremenopausal womenEstrogenic stimulationContain estrogenBreastEffects of estrogenCancerHormone estrogenActivateExogenousNolvadexSymptomsAndrogenDifferent tissuesGenesWomenEndometrialPrevent bone lossTherapeuticTranscription factorsBone healthIsoflavones
Modulators29
Tamoxifen12
  • SERMs are used dependent on their pattern of action in various tissues: Tamoxifen is a first-line hormonal treatment of ER-positive metastatic breast cancer. (wikipedia.org)
  • SERMs like clomifene and tamoxifen are comparatively more in the middle in their IA and their balance of estrogenic and antiestrogenic activity. (wikipedia.org)
  • In this study, we analysed the effect of the SERMs tamoxifen, raloxifene, and toremifene on the expression of lipid metabolism genes by microarrays and quantitative PCR in different cell types, and ascertained the main mechanisms involved. (ox.ac.uk)
  • Tamoxifen is a SERM that blocks the effect of estrogen on breast cancer cells. (geosalud.com)
  • But the currently available SERMs such as tamoxifen [Nolvadex] do not meet all of our needs. (cancernetwork.com)
  • Newer SERMs, such as raloxifene (Evista), may be closer to the ideal profile, but only long-term clinical trials such as STAR (Study of Tamoxifen and Raloxifene) will answer this question, he said. (cancernetwork.com)
  • Jordan's findings include application of the original SERM, the estrogen-blocking drug tamoxifen, to the treatment and prevention of breast cancer, and discovery that raloxifene prevents both osteoporosis and breast cancer. (mdanderson.org)
  • Tamoxifen and raloxifene are SERMS. (guysandstthomas.nhs.uk)
  • Osteoblast-like (ROS and U2OS) and breast cancer (MCF7) cells were transfected with a human ER alpha-GFP fusion protein, and treated with ER agonists (17 beta-estradiol, and dienestrol), antagonists (ICI 182,780 and ZK 164015) and SERMs (tamoxifen, raloxifene, 4-hydroxytamoxifen (4-HT) and hexestrol). (bath.ac.uk)
  • Tamoxifen has been used for more than 30 years to treat hormone receptor -positive breast cancer. (thecancerspecialist.com)
  • For example, tamoxifen blocks the effects of estrogen in breast tissue but acts like estrogen in the uterus and bone. (thecancerspecialist.com)
  • An example of a well known SERM is the breast cancer treatment drug tamoxifen, which stimulates estrogen receptors in the uterus and bone, but suppresses them in the breast. (nwhn.org)
Raloxifene3
  • In postmenopausal women, estrogen or estrogen plus progestogen or raloxifene should not be used for the treatment of osteoporosis. (medscape.com)
  • In contrast, the osteoporosis drug raloxifene-which is a SERM-has estrogen-like effects on bones, but anti -estrogenic effects in breast tissue. (theveganrd.com)
  • 2. Heringa M. Review on raloxifene: profile of a selective estrogen receptor modulator. (theveganrd.com)
Menopause14
  • SERMs are used for various estrogen-related diseases, including treatment of ovulatory dysfunction in the management of infertility, treatment and prevention of postmenopausal osteoporosis, treatment and reduction in risk of breast cancer and treatment of dyspareunia due to menopause. (wikipedia.org)
  • SERM is also used in combination with conjugated estrogens indicated for the treatment of estrogen deficiency symptoms, and vasomotor symptoms associated with menopause. (wikipedia.org)
  • The combination therapy is used in the treatment of moderate to severe vasomotor symptoms associated with menopause, prevention of postmenopausal osteoporosis as well as treatment of estrogen deficiency symptoms in non-hysterectomized postmenopausal women. (wikipedia.org)
  • Women also lose more bone mass after menopause with very low levels of the hormone estrogen . (womenshealth.gov)
  • Higher estrogen levels before menopause helps protect bone density. (womenshealth.gov)
  • After menopause , your ovaries make very little of the hormone estrogen . (womenshealth.gov)
  • Low estrogen levels are common after menopause . (epnet.com)
  • After menopause, oestrogen levels drop and this results in accelerated bone loss. (menopause.org.au)
  • Clinical manifestations may include hot flushes, night sweats, sleep disruption, and genitourinary syndrome of menopause (symptoms and signs due to estrogen deficiency, such as vulvovaginal atrophy). (msdmanuals.com)
  • After menopause, most of a woman's estrogen is made outside the ovaries from androgen, another hormone. (geosalud.com)
  • Women tend to be diagnosed with osteoporosis more often than men because once they reach menopause, estrogen levels decrease. (emedicinehealth.com)
  • Hormone therapy for breast cancer should not be confused with menopausal hormone therapy (MHT)-treatment with estrogen alone or in combination with progesterone to help relieve symptoms of menopause . (thecancerspecialist.com)
  • MHT boosts estrogen levels and reduces the chance of getting osteoporosis after menopause is experienced. (tigerlilyfoundation.org)
  • Most patients with breast cancer will experience symptoms of menopause or clinical manifestations of estrogen deficiency after their therapy is completed. (medscape.com)
Antagonists4
  • A characteristic that distinguishes these substances from pure ER agonists and antagonists (that is, full agonists and silent antagonists) is that their action is different in various tissues, thereby granting the possibility to selectively inhibit or stimulate estrogen-like action in various tissues. (wikipedia.org)
  • For example, ER antagonists are reported to stimulate reporter assays based on estrogen target genes in osteoblasts, contrary to their inhibitory effects in vivo. (bath.ac.uk)
  • Because SERMs bind to estrogen receptors, they can potentially not only block estrogen activity (i.e., serve as estrogen antagonists ) but also mimic estrogen effects (i.e., serve as estrogen agonists). (thecancerspecialist.com)
  • SERMs can behave as estrogen antagonists in some tissues and as estrogen agonists in other tissues. (thecancerspecialist.com)
SERM5
  • The first tissue selective estrogen complex (TSEC) combines conjugated estrogens and the SERM bazedoxifene to blend their activities. (wikipedia.org)
  • Different tissues have different degrees of sensitivity to the activity of endogenous estrogens, so SERMs produce estrogenic or antiestrogenic effects depending on the specific tissue in question as well as the percentage of intrinsic activity (IA) of the SERM. (wikipedia.org)
  • Evista is commonly referred to as a selective estrogen receptor modulator (SERM). (lincolndailynews.com)
  • This dual ligand quality characterizes what is now known as a selective estrogen receptor modulator (SERM). (umsystem.edu)
  • The authors note that the "concept of combining a SERM with an estrogen to create a TSEC has been studied intensively in the past decade. (medscape.com)
Aromatase inhibitors3
Osteoporosis4
  • Preclinical and clinical reports suggest that it is considerably less potent than estrogen for the treatment of osteoporosis. (wikipedia.org)
  • SERMs have attracted great clinical interest for the treatment of several pathologies, most notably breast cancer and osteoporosis. (ox.ac.uk)
  • SERMs are also used to treat ovulatory dysfunction and to reduce the risk of invasive breast cancer in postmenopausal women at risk or who have osteoporosis. (rxlist.com)
  • Later in life, when estrogen levels drop, bone care continues to be essential to reduce the risk of too much bone breakdown and developing osteoporosis. (tigerlilyfoundation.org)
Phytoestrogens2
  • Sometimes referred to as phytoestrogens, isoflavones have a chemical structure that is very similar to the hormone estrogen, but small variations in their structure translate to important differences in physiological effects. (theveganrd.com)
  • Phytoestrogens are estrogens that occur in some plants. (nwhn.org)
Agonists4
  • SERMs are competitive partial agonists of the ER. (wikipedia.org)
  • SERMs act as ER agonists in bone despite their antagonistic properties in other tissues. (bath.ac.uk)
  • In Particular, ERGR-mediated GRE-luc activity provides a high signal response to estrogen agonists and SERMs, in a cell context dependent manner closely resembling that observed in vivo. (bath.ac.uk)
  • AIM: The present study aims to identify selective estrogen receptor beta (ERß) agonists and to evaluate the neuroprotective mechanism in Parkinson's disease (PD) models. (bvsalud.org)
Risk of oestrogen2
  • Chemoprevention can reduce the risk of oestrogen positive cancers happening. (guysandstthomas.nhs.uk)
  • However, the benefit to people with BRCA and PALB2 gene mutation, who are at increased risk of oestrogen negative cancers, is unclear. (guysandstthomas.nhs.uk)
Block estrogen2
  • Block estrogen activity in the breast and uterus , reducing the risk of breast cancer and endometrial hyperplasia (thickening). (rxlist.com)
  • SERMs, along with kickstarting your hormone production, also block estrogen from binding to receptors. (anabolicminds.com)
Postmenopausal3
  • For example, while estrogen therapy can protect bone health in postmenopausal women, it may also raise risk for breast cancer. (theveganrd.com)
  • The treatment strategies for postmenopausal urinary incontinence are various and may include estrogens, anticholinergics, and pelvic floor muscle training. (bvsalud.org)
  • The combination of anticholinergics with local estrogens has not been shown to be more effective than anticholinergics alone in improving urinary incontinence symptoms in postmenopausal women. (bvsalud.org)
Evista1
Ovaries4
  • Estrogen, a hormone produced by the ovaries, appears to increase a woman’s risk for developing breast cancer. (geosalud.com)
  • Oestrogen is the group of hormones produced by the ovaries. (guysandstthomas.nhs.uk)
  • Because the ovaries are the main source of estrogen in premenopausal women, estrogen levels in these women can be reduced by eliminating or suppressing ovarian function. (thecancerspecialist.com)
  • These medicines interfere with signals from the pituitary gland that stimulate the ovaries to produce estrogen. (thecancerspecialist.com)
Menopausal hormone therapy1
  • Menopausal Hormone Therapy (MHT, previously known as HRT) - Women lose estrogen as they age. (tigerlilyfoundation.org)
Stimulate2
  • In men, both of these drugs act as anti-estrogens in their capacity to oppose the negative feedback of estrogens on the hypothalamus and stimulate the heightened release of GnRH (Gonadotropin Releasing Hormone). (professionalmuscle.com)
  • The authors note that the treatment of VVA "remains an area of unmet need," and while low-dose vaginal estrogen can be absorbed in small amounts without raising blood levels, it could potentially stimulate occult breast cancer cells. (medscape.com)
Bind4
  • SERMs bind to estrogen receptors and activate estrogen pathways in some tissue while blocking its effects in other types of tissue. (rxlist.com)
  • Both isoflavones and estrogen bind to and activate estrogen receptors (ERs) on cells. (theveganrd.com)
  • Both estradiol and xenoestrogens can bind two estrogen receptors (ERs), ER alpha and ER beta, to elicit biological responses. (umsystem.edu)
  • While estradiol binds both receptors equally, some xenoestrogens have been shown to bind ER beta preferentially. (umsystem.edu)
Binds2
  • That doesn't matter to estrogen, which happily binds to either type, but isoflavones are more finicky. (theveganrd.com)
  • Like SERMs, fulvestrant binds to the estrogen receptor and functions as an estrogen antagonist. (thecancerspecialist.com)
Transcriptional4
  • Furthermore, the SERMs reduced the stimulation of the transcriptional activity of the liver X receptor (LXR) by exogenous cholesterol. (ox.ac.uk)
  • The estrogen receptor is the master transcriptional regulator of breast cancer phenotype and the archetype of a molecular therapeutic target. (nature.com)
  • We examined whether evaluating global aspects of ER function Provides a more accurate reflection of ER activation in osteoblasts, based on the use of morphological and/or transcriptional read-outs with green fluorescent protein (GFP)-receptor chimeras. (bath.ac.uk)
  • Indeed, transcriptional responses to SERMs in osteoblast-like cells were considerably greater with the ERGR/GRE-luc than the ER alpha/ERE-luc system, 4-HT inducing 300 and 25% increases in reporter activity respectively. (bath.ac.uk)
Vaginal dryness1
  • Estrogen-like to relieve menopausal vasomotor symptoms and vaginal dryness. (rxlist.com)
Response to estrogen1
  • It is characterized by the presence of estrogen receptors on cancer cells, which causes the cancer cells to grow in response to estrogen 12. (wrbl.com)
Uterus1
  • If these botanicals work by exerting a hormone-like influence, we should exercise caution about long term use, which could have estrogen-like effects on the uterus and breast, until we learn more from these studies. (nwhn.org)
Behave1
  • Chemicals found in the environment have been found to behave like the body's natural estrogen, estradiol. (umsystem.edu)
Tissue selective estrogen1
  • Another approach is tissue selective estrogen complex (TSEC) agents. (medscape.com)
Decrease2
  • During the menopausal transition and postmenopause, estrogen levels fluctuate and eventually decrease significantly, but the changes in other hormones vary. (msdmanuals.com)
  • However, a decrease in overall estrogen may pose health risks for women such as increased risk for heart disease. (cancernetwork.com)
Bazedoxifene1
  • A TSEC paired with oral conjugated equine estrogen, such as bazedoxifene with conjugated estrogens ( Duavee , Pfizer) has already been approved for VVA. (medscape.com)
Hormonal2
  • SERMs have also been used as a hormonal treatment option by some transgender people. (wikipedia.org)
  • This type happens when the cancer cells don't have the right hormonal receptors. (webmd.com)
Premenopausal women1
  • This drug has the ability to block all estrogen in a patient, including premenopausal women, without the need for additional medications. (wrbl.com)
Estrogenic stimulation1
  • The combination allows for the benefits of estrogen with regard to relief of vasomotor symptoms without estrogenic stimulation of the endometrium. (wikipedia.org)
Contain estrogen3
  • The other is the mistaken idea that soyfoods contain estrogen, which I want to address here. (theveganrd.com)
  • If the tumor cells contain estrogen receptors, the cancer is called estrogen receptor positive (ER positive), estrogen sensitive, or estrogen responsive. (thecancerspecialist.com)
  • Breast tumors that contain estrogen and/or progesterone receptors are sometimes called hormone receptor positive (HR positive). (thecancerspecialist.com)
Breast17
  • It shows no breast or endometrial stimulation and in the first two years, the small increase is better in venous thromboembolism, and similar in the long term to other SERMs. (wikipedia.org)
  • We mapped all estrogen receptor and RNA polymerase II binding sites on a genome-wide scale, identifying the authentic cis binding sites and target genes, in breast cancer cells. (nature.com)
  • Furthermore, this resource has allowed the identification of cis -regulatory sites in previously unexplored regions of the genome and the cooperating transcription factors underlying estrogen signaling in breast cancer. (nature.com)
  • Estrogen levels are lower during pregnancy and breast-feeding. (geosalud.com)
  • It has been shown that lower exposure to estrogen results in a lower risk of breast cancer. (cancernetwork.com)
  • Patients with locally advanced or metastatic breast cancer that is hormone receptor-positive, HER2-negative breast cancer with 1 or more PIK3CA, AKT1, or PTEN alterations may now receive capivasertib plus fulvestrant. (cancernetwork.com)
  • Two thirds of breast cancers express the luminal estrogen receptor-positive (ERα + ) phenotype that is initially responsive to antihormonal therapies, but drug resistance emerges. (nature.com)
  • About 80% of all newly diagnosed breast cancers have luminal cell phenotype and they express estrogen receptor (ERα). (nature.com)
  • In reducing the risk of invasive breast cancer, SERMs may act by blocking estrogen receptors in the breast. (lincolndailynews.com)
  • The trial aims to include approximately 175 patients from both Canada and the U.S., all of whom have Grade 1 or 2 Estrogen Receptor positive (ER+) / Human Epidermal Growth Factor Receptor 2 negative (HER2-) breast cancer. (wrbl.com)
  • A large number of breast cancers rely on oestrogen to grow. (guysandstthomas.nhs.uk)
  • SERMs caused a modest increase in ERE-luc activity in osteoblast-like cells (but not in breast cells), and a reduction in nuclear mobility in breast (but not osteoblast-like) cells. (bath.ac.uk)
  • Interestingly, SERMs increased both cytoplasmic to nuclear translocation of ERGR-GFP, and GRE-luc reporter activity, in osteoblast-like (but not breast) cells. (bath.ac.uk)
  • To determine whether breast cancer cells contain hormone receptors, doctors test samples of tumor tissue that have been removed by surgery. (thecancerspecialist.com)
  • Breast cancers that lack estrogen receptors are called estrogen receptor negative (ER negative). (thecancerspecialist.com)
  • Breast tumors that lack progesterone receptors are called progesterone receptor negative (PR or PgR negative). (thecancerspecialist.com)
  • Breast tumors that lack both estrogen and progesterone receptors are sometimes called hormone receptor negative (HR negative). (thecancerspecialist.com)
Effects of estrogen1
  • This means that in certain tissues they can block the effects of estrogen, by altering the binding capacity of the receptor, while in others they can act as actual estrogens, activating the receptor. (professionalmuscle.com)
Cancer2
  • What sets (Z)-endoxifen apart from other SERMs is its ability to specifically target a protein called PKCβ1, known to promote cancer growth. (wrbl.com)
  • Similarly, if the tumor cells contain progesterone receptors, the cancer is called progesterone receptor positive (PR or PgR positive). (thecancerspecialist.com)
Hormone estrogen1
  • Besides functioning as an antioxidant and anthelmintic , many isoflavones have been shown to interact with animal and human estrogen receptors , causing effects in the body similar to those caused by the hormone estrogen . (wikipedia.org)
Activate2
  • Antidepressants that activate dopaminergic (bupropion (Wellbutrin), venlafaxine(Effexor)), central noradrenic receptors (mirtazepine, bupropion, venlafaxine) and 5-hydroxytriptamine (5-HT) A1 and 2C receptors (nefazodone (Serzone), mirtazepine) may augment sexual response. (healthyplace.com)
  • Those that activate other 5-HT receptors, prolactin and gamma-aminobutyric acid reduce sexual response . (healthyplace.com)
Exogenous1
  • These exogenous estrogen-mimicking compounds have been termed xenoestrogens. (umsystem.edu)
Nolvadex1
  • Clomid and Nolvadex are both anti-estrogens belonging to the same group of triphenylethylene compounds. (professionalmuscle.com)
Symptoms1
  • In most studies, no significant improvement in urinary symptoms was observed in patients treated with local estrogens, although they showed to be helpful in improving vaginal symptoms. (bvsalud.org)
Androgen1
  • Tren Ace works by binding to androgen receptors, which are found in muscle tissue. (fantasyevents.org)
Different tissues3
  • Human cells have two types of these receptors-ER-alpha and ER- beta-which have different distributions in different tissues. (theveganrd.com)
  • As a result-while estrogen always acts like estrogen-isoflavones function differently in different tissues. (theveganrd.com)
  • Dr. Cunningham's work has focused on the role of nuclear hormone receptors, particularly the estrogen receptor, which has variants and isoforms that can change the way estrogen acts in different tissues. (lupus.org)
Genes2
  • The three SERMs increased the expression of sterol regulatory element‐binding protein (SREBP) target genes, especially those targeted by SREBP-2. (ox.ac.uk)
  • Combining this unique resource with gene expression data demonstrates distinct temporal mechanisms of estrogen-mediated gene regulation, particularly in the case of estrogen-suppressed genes. (nature.com)
Women3
  • Women, and estrogen values are high well tolerated compared to other forms of anabolic steroid talks like a therapeutic good. (ncfy.com)
  • Estrogen helps maintain bone density in women. (emedicinehealth.com)
  • Although women with LCIS comprise a relatively small proportion of subjects in the relevant clinical trials, the extent of risk reduction with SERMs is similar in women at increased risk due to LCIS compared to women at increased risk for other reasons such as family history (risk reductions of 56% and 49%, respectively). (canceraustralia.gov.au)
Endometrial1
  • SERMs reduce the risk of endometrial hyperplasia that can occur with estrogen therapy. (rxlist.com)
Prevent bone loss1
  • Although this therapy indirectly helps prevent bone loss by increasing estrogen, it is associated with an increased risk of other conditions. (tigerlilyfoundation.org)
Therapeutic1
  • By correlating a ligand's tissue specific estrogenic activity with its unique ER conformation, peptide profiling will not only further elucidate tissue-specific ER activity differences but could also be used as a high-throughput screening tool for other potential environmental xenoestrogens and identify novel therapeutic SERMs. (umsystem.edu)
Transcription factors2
Bone health1
  • Estrogen is a hormone that has many important functions including the development of female secondary sexual characteristics, regulation of reproductive cycle, and maintenance of bone health. (rxlist.com)
Isoflavones4
  • And in order to understand the controversy around soyfoods, it's necessary to understand what isoflavones are-and why they aren't the same as estrogen. (theveganrd.com)
  • Because they function as SERMS, research is focused on potential health benefits of isoflavones, particularly as safe alternatives to estrogen. (theveganrd.com)
  • What we do know with certainty is that isoflavones are not estrogen and, looking at how estrogen acts in the body doesn't tell us anything about the effects of eating soyfoods. (theveganrd.com)
  • In fact, if isoflavones were the same as estrogen, there wouldn't really be any interest in studying them as alternatives to this hormone. (theveganrd.com)