This is a list of selective estrogen receptor modulators (SERMs). SERMs that have been approved for medical use include ... ISBN 978-94-011-4439-1. Taylor, Hugh S. (2009). "Designing the ideal selective estrogen receptor modulator-an achievable goal ... Selective estrogen receptor modulators, Biology-related lists). ... it was subsequently found not to bind to the estrogen receptor ... anordrin (+mifepristone (Zi Yun)), bazedoxifene (+conjugated estrogens (Duavee)), broparestrol (Acnestrol), clomifene (Clomid ...
... estrogen receptor modulators Selective androgen receptor modulator Selective estrogen receptor degrader Selective receptor ... Selective estrogen receptor modulators (SERMs), also known as estrogen receptor agonist/antagonists (ERAAs), are a class of ... Feng Q, O'Malley BW (Nov 2014). "Nuclear receptor modulation--role of coregulators in selective estrogen receptor modulator ( ... Pickar JH, Komm BS (Sep 2015). "Selective estrogen receptor modulators and the combination therapy conjugated estrogens/ ...
CTA is a high-efficacy partial agonist of the estrogen receptor. As such, it is a selective estrogen receptor modulator (SERM ... CTA is an estrogen, or an agonist of the estrogen receptors, the biological target of estrogens like estradiol. It is a high- ... efficacy partial estrogen and shows some properties of a selective estrogen receptor modulator, with predominantly estrogenic ... Selective estrogen receptor modulators, Synthetic estrogens, Triphenylethylenes, Bis(4-hydroxyphenyl)methanes). ...
165-. ISBN 978-0-470-69703-0. Grese TA, Dodge JA (February 1998). "Selective estrogen receptor modulators (SERMs)". Current ... is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group that was developed originally in ... to 60-fold increased affinity for the estrogen receptor and reduced partial estrogen agonistic activity. The affinity of ... Wittliff JL, Kerr DA II, Andres SA (2005). "Estrogens IV: Estrogen-Like Pharmaceuticals". In Wexler, P. (ed.). Encyclopedia of ...
Oseni, T; Patel, R; Pyle, J; Jordan, VC (2008). "Selective Estrogen Receptor Modulators and Phytoestrogens". Planta Med. 74 (13 ... Because most naturally occurring phytoestrogens act as selective estrogen receptor modulators, or SERMs, which do not ... June 2003). "Phyto-oestrogen Database of Foods and Average Intake in Finland". British Journal of Nutrition. 89 (5): S31-S38. ... necessarily act as direct agonists of estrogen receptors, normal consumption of foods that contain these phytoestrogens should ...
... is a selective estrogen receptor modulator (SERM) and therefore a mixed agonist-antagonist of the estrogen receptor ... "Differential response of estrogen receptor alpha and estrogen receptor beta to partial estrogen agonists/antagonists". ... Duarte FH, Jallad RS, Bronstein MD (November 2016). "Estrogens and selective estrogen receptor modulators in acromegaly". ... and of invasive estrogen receptor-positive breast cancer by 84%. Conversely, it does not reduce the risk of estrogen receptor- ...
... and genistein to the beta receptor Subtype selective estrogen receptor modulators preferentially bind to either the α- or the β ... Estrogen receptors also occur within the cell nucleus, and both estrogen receptor subtypes have a DNA-binding domain and can ... As hormone receptors for sex steroids (steroid hormone receptors), ERs, androgen receptors (ARs), and progesterone receptors ( ... nuclear estrogen receptors (ERα and ERβ), which are members of the nuclear receptor family of intracellular receptors, and ...
Stone JC, Clark J, Cuneo R, Russell AW, Doi SA (June 2014). "Estrogen and selective estrogen receptor modulators (SERMs) for ... Duarte FH, Jallad RS, Bronstein MD (November 2016). "Estrogens and selective estrogen receptor modulators in acromegaly". ... Estrogens are agonists of the estrogen receptors, the biological targets of endogenous estrogens like estradiol. They have ... Li F, Dou J, Wei L, Li S, Liu J (2016). "The selective estrogen receptor modulators in breast cancer prevention". Cancer ...
Duarte FH, Jallad RS, Bronstein MD (November 2016). "Estrogens and selective estrogen receptor modulators in acromegaly". ... Estrogens are agonists of the estrogen receptors (ERs), the biological target of endogenous estrogens such as estradiol. When ... A study that used high- to very-high-dose oral estradiol to treat postmenopausal women with estrogen receptor-positive breast ... High-dose estrogen therapy (HDE) is a type of hormone therapy in which high doses of estrogens are given. When given in ...
... is a selective estrogen receptor modulator (SERM) which was being developed as an alternative to estrogen replacement therapy ... List of selective estrogen receptor modulators "Levormeloxifene - AdisInsight". Ravn P, Nielsen TF, Christiansen C (2006). " ... Selective estrogen receptor modulators, All stub articles, Genito-urinary system drug stubs). ...
Dodge JA, Richardson TI (2007). "Chapter 10 Novel Selective Estrogen Receptor Modulators (SERMs)". Annual Reports in Medicinal ... It is a "pathway-selective" estrogen receptor (ER) ligand which inhibits NF-κB with an IC50Tooltip half-maximal inhibitory ... December 2005). "The activity of pathway-selective estrogen receptor ligands in experimental septic shock". Shock. 24 (6): 535- ... WAY-204688, also known as SIM-688, is a synthetic nonsteroidal estrogen and nuclear factor κB (NF-κB) inhibitor which was ...
Duarte FH, Jallad RS, Bronstein MD (November 2016). "Estrogens and selective estrogen receptor modulators in acromegaly". ... C. acnes' ability to bind and activate a class of immune system receptors known as toll-like receptors (TLRs), especially TLR2 ... It is usually combined with an estrogen to avoid menstrual irregularities and estrogen deficiency. The medication appears to be ... peroxisome proliferator-activated receptor modulators, and inhibitors of the stearoyl-CoA desaturase-1 enzyme are also a focus ...
G Protein-Coupled Estrogen Receptor and Its Pharmacologic Modulators". Pharmacological Reviews. 67 (3): 505-540. doi:10.1124/pr ... Estrone is an estrogen, specifically an agonist of the estrogen receptors ERα and ERβ. It is a far less potent estrogen than is ... 1) (Butenandt 1931). Parl FF (2000). Estrogens, Estrogen Receptor and Breast Cancer. IOS Press. pp. 4-5. ISBN 978-0-9673355-4-4 ... In contrast to estradiol and estriol, estrone is not a ligand of the G protein-coupled estrogen receptor (affinity >10,000 nM ...
G Protein-Coupled Estrogen Receptor and Its Pharmacologic Modulators". Pharmacological Reviews. 67 (3): 505-540. doi:10.1124/pr ... or G-Protein-Coupled Estrogen Receptor (GPER)". Estrogen Receptors. Methods in Molecular Biology. Vol. 1366. pp. 11-7. doi: ... 2-Methoxyestradiol is derived from estradiol, although it interacts poorly with the estrogen receptors (2,000-fold lower ... it retains activity as a high-affinity agonist of the G protein-coupled estrogen receptor (GPER) (10 nM, relative to 3-6 nM for ...
G Protein-Coupled Estrogen Receptor and Its Pharmacologic Modulators". Pharmacol. Rev. 67 (3): 505-40. doi:10.1124/pr. ... Chimento A, Sirianni R, Casaburi I, Pezzi V (2014). "Role of estrogen receptors and g protein-coupled estrogen receptor in ... the effects of estrogens binding to these classical estrogen receptors is delayed. However, estrogens are also known to have ... G protein-coupled estrogen receptor 1 (GPER), also known as G protein-coupled receptor 30 (GPR30), is a protein that in humans ...
G Protein-Coupled Estrogen Receptor and Its Pharmacologic Modulators". Pharmacol. Rev. 67 (3): 505-40. doi:10.1124/pr. ... Estriol is an estrogen, specifically an agonist of the estrogen receptors ERα and ERβ. It is a far less potent estrogen than is ... a membrane estrogen receptor where, conversely, estradiol acts as an agonist. Estradiol increases breast cancer cell growth via ... "Estriol acts as a GPR30 antagonist in estrogen receptor-negative breast cancer cells". Molecular and Cellular Endocrinology. ...
... which include selective estrogen receptor modulators (SERM) and aromatase inhibitors. Clomiphene is a selective estrogen ... Goldstein SR, Siddhanti S, Ciaccia AV, Plouffe L (2000). "A pharmacological review of selective oestrogen receptor modulators ... Stute P, Birkhauser M (2015). "Selective estrogen receptor modulators (SERM)/Selektive Ostrogenrezeptormodulatoren (SERM)" (PDF ... receptor modulator (SERM). It is the most widely used fertility drug. Other medications in this class include tamoxifen and ...
G Protein-Coupled Estrogen Receptor and Its Pharmacologic Modulators". Pharmacol. Rev. 67 (3): 505-40. doi:10.1124/pr. ... Estrone is an estrogen, specifically an agonist of the estrogen receptors (ERs) ERα and ERβ. It is a far less potent estrogen ... Estrone is a naturally occurring and bioidentical estrogen, or an agonist of the estrogen receptor, the biological target of ... In contrast to estradiol and estriol, estrone is not a ligand of the G protein-coupled estrogen receptor (affinity >10,000 nM ...
Nath A, Sitruk-Ware R (June 2009). "Pharmacology and clinical applications of selective estrogen receptor modulators". ... Estetrol is an agonist of the estrogen receptors (ERs), and hence is an estrogen. It has moderate affinity for ERα and ERβ, ... a manner identical to that of the other estrogens and distinct from that observed with Selective Estrogen Receptor Modulators ( ... Estetrol is a naturally occurring and bioidentical estrogen, or an agonist of the estrogen receptor, the biological target of ...
G Protein-Coupled Estrogen Receptor and Its Pharmacologic Modulators". Pharmacol. Rev. 67 (3): 505-40. doi:10.1124/pr. ... In contrast to 17β-estradiol, 17α-estradiol, while it still binds to the estrogen receptor, has less or no feminizing ... "Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta". ... It is a stereoisomer of the endogenous steroid hormone and estrogen 17β-estradiol (or simply estradiol). Alfatradiol is used in ...
G Protein-Coupled Estrogen Receptor and Its Pharmacologic Modulators". Pharmacol. Rev. 67 (3): 505-40. doi:10.1124/pr. ... List of investigational sex-hormonal agents § Estrogenics List of selective estrogen receptor modulators "Afimoxifene - BHR ... Selective estrogen receptor modulators, Triphenylethylenes, Ethanolamines, All stub articles, Genito-urinary system drug stubs) ... is a selective estrogen receptor modulator (SERM) of the triphenylethylene group and an active metabolite of tamoxifen. The ...
... is a selective estrogen receptor modulator (SERM), and hence is a mixed agonist and antagonist of the estrogen ... is a selective estrogen receptor modulator (SERM) of the benzothiophene group which was never marketed. It is a potent estrogen ... Martinkovich S, Shah D, Planey SL, Arnott JA (2014). "Selective estrogen receptor modulators: tissue specificity and clinical ... 2007). "Structure-activity relationships for a family of benzothiophene selective estrogen receptor modulators including ...
Selective estrogen receptor modulators, Synthetic estrogens, Triphenylethylenes, All stub articles, Pharmacology stubs). ... TPE is the parent compound of a group of nonsteroidal estrogen receptor ligands. It includes the estrogens chlorotrianisene, ... Selective Estrogen Receptor Modulators: A New Brand of Multitarget Drugs. Springer Science & Business Media. pp. 52-. ISBN 978- ... the selective estrogen receptor modulators (SERMs) afimoxifene, brilanestrant, broparestrol, clomifene, clomifenoxide, ...
... (INN) (developmental code name ERA-923) is a nonsteroidal selective estrogen receptor modulator (SERM) that was ... Selective Estrogen Receptor Modulators: A New Brand of Multitarget Drugs. Springer Science & Business Media. pp. 58-. ISBN 978- ... Selective estrogen receptor modulators, All stub articles, Antineoplastic and immunomodulating drug stubs). ... ISBN 978-1-60805-496-1. Ottow E, Weinmann H (8 September 2008). Nuclear Receptors as Drug Targets. John Wiley & Sons. pp. 95-. ...
Cano A, Calaf i Alsina J, Duenas-Diez JL (22 September 2006). Selective Estrogen Receptor Modulators: A New Brand of ... Fispemifene (INN, USAN) (developmental code name HM-101) is a nonsteroidal selective estrogen receptor modulator (SERM) of the ... Selective estrogen receptor modulators, Triphenylethylenes, All stub articles, Genito-urinary system drug stubs). ... 52-. ISBN 978-3-540-34742-2. Ottow E, Weinmann H (8 September 2008). Nuclear Receptors as Drug Targets. John Wiley & Sons. pp. ...
Selective estrogen receptor modulators (SERMs) are a commonly used adjuvant therapy in estrogen-receptor positive (ERα+) breast ... Jordan VC, O'Malley BW (December 2007). "Selective estrogen-receptor modulators and antihormonal resistance in breast cancer". ... August 1995). "Changes in estrogen receptor, progesterone receptor, and pS2 expression in tamoxifen-resistant human breast ... These include: Loss of estrogen receptor alpha (ERα) Although this may be a mechanism of resistance in a minority of women, ...
Fabian CJ, Kimler BF (March 2005). "Selective estrogen-receptor modulators for primary prevention of breast cancer". J. Clin. ... "Testosterone inhibits estrogen-induced mammary epithelial proliferation and suppresses estrogen receptor expression". FASEB ... The medication has also been found to interact very weakly with the estrogen and progesterone receptors, and to act as an ... Likely due to increased activation of the estrogen and/or progesterone receptors, spironolactone has very weak but significant ...
Wallace OB, Richardson TI, Dodge JA (2003). "Estrogen receptor modulators: relationships of ligand structure, receptor affinity ... List of selective estrogen receptor modulators Jørgensen AS, Jacobsen P, Christiansen LB, Bury PS, Kanstrup A, Thorpe SM, et al ... NC 45-0095 is a synthetic nonsteroidal selective estrogen receptor modulator (SERM) which was under development by Novo Nordisk ... Meegan MJ, Lloyd DG (January 2005). "Understanding the Molecular Mechanism of Action of Estrogen Receptor Modulators. Frontiers ...
... is one of the selective estrogen receptor modulators, or SERMs, a class of medication which acts on the estrogen receptor. It ... Ormeloxifene is a selective estrogen receptor modulator (SERM). In some parts of the body, its action is estrogenic (e.g., ... Makker A, Tandon I, Goel MM, Singh M, Singh MM (June 2009). "Effect of ormeloxifene, a selective estrogen receptor modulator, ... Shelly W, Draper MW, Krishnan V, Wong M, Jaffe RB (March 2008). "Selective estrogen receptor modulators: an update on recent ...
The medication is a selective estrogen receptor modulator (SERM) and hence is a mixed agonist-antagonist of the estrogen ... Price N, Sartor O, Hutson T, Mariani S (2005). "Role of 5a-reductase inhibitors and selective estrogen receptor modulators as ... Toremifene is a selective estrogen receptor modulator (SERM). That is, it is a selective mixed agonist-antagonist of the ... 192-. ISBN 978-1-55009-260-8. Selective Estrogen Receptor Modulators-Advances in Research and Application: 2013 Edition: ...