Search for other works by this author on: Due to this dual action, Tamoxifen is better described with the term selective estrogen receptor modulator (SERM). Search for other works by this author on:
Multiple Outcomes of Raloxifene Evaluation (MORE) investigators.Tamoxifen, raloxifene, and the prevention of breast cancer.3-[4-(1,2-diphenylbut-1-enyl)phenyl]acrylic acid: a non-steroidal estrogen with functional selectivity for bone over uterus in rats.Dissection of the molecular mechanism of action of GW5638, a novel estrogen receptor ligand, provides insights into the role of estrogen receptor in bone.A monohydroxylated metabolite of tamoxifen with potent antioestrogenic activity.Evidence for the metabolic activation of non-steroidal antioestrogens: a study of structure-activity relationships.Comparative analyses of mechanistic differences among antiestrogens.Antiestrogen ICI 164,384 reduces cellular estrogen receptor content by increasing its turnover.Importance of the alkylaminoethoxy side-chain for the estrogenic and antiestrogenic actions of tamoxifen and trioxifene in the immature rat uterus.Mammalian antifertility agents. We synthesized and screened five …

Last Updated: Aug 23, 2018 Miles Brown, Dana Farber Cancer Center, Boston) were maintained in phenol red containing DMEM supplemented with 10% FBS, 2 mCells were seeded at 15,000 per well in 24-well plates, on day 0, in estrogen-free maintenance medium. A, GW7604 blocked the effect of EThe hypothesis that antiestrogenic side chain of GW7604 had an important interaction with aa351 was addressed in our next experiment. ); the U.S. Army Medical Research and Material Command Breast Cancer Research Program, DAMD17–96-16169 (to H.L. The cells were treated on days 1, 3, and 5 with test media containing EThe assay of compounds for estrogenic and antiestrogenic activity at the TGFα gene was described previously (A structural model of dimeric human ERα bound to 4-OHT was constructed from 3ERT.pdb (To characterize the antiestrogenic activity of GW7604 further, we determined the effects of ER protein expression in MCF-7 breast cancer and ECC-1endometrial cancer cells. A, Northern blot analysis of TGFα mRNA was performed as described in Concentration-related actions of GW7604 on TGFα mRNA levels in MDA-MB-231 cells stably transfected with cDNAs for wild-type or D351Y ER. 1-Aryl-2-phenyl-1,2,3,4-tetrahydro-1- naphthols, 1-aryl-2-phenyl-3,4-dihydronaphthalenes, and their derivatives.Molecular basis of agonism and antagonism in the oestrogen receptor.The structural basis of estrogen receptor/coactivator recognition and the antagonism of this interaction by tamoxifen.The estrogen receptor from a tamoxifen stimulated MCF-7 tumor variant contains a point mutation in the ligand binding domain.A naturally occurring estrogen receptor mutation results in increased estrogenicity of a tamoxifen analog.Growth regulation of estrogen receptor-negative breast cancer cells transfected with complementary DNAs for estrogen receptor [see comments].The key to the antiestrogenic mechanism of raloxifene is amino acid 351 (aspartate) in the estrogen receptor.The oestrogen-like effect of 4-hydroxytamoxifen on induction of transforming growth factor alpha mRNA in MDA-MB-231 breast cancer cells stably expressing the oestrogen receptor.The interaction of raloxifene and the active metabolite of the antiestrogen EM-800 (SC 5705) with the human estrogen receptor.A simple, rapid, and sensitive DNA assay procedure.Models of estrogen receptor regulation by estrogens and antiestrogens in breast cancer cell lines.Estrogenic activity is increased for an antiestrogen by a natural mutation of the estrogen receptor.Peptide antagonists of the human estrogen receptor.Allosteric silencing of activating function 1 in the 4-hydroxytamoxifen estrogen receptor complex is induced by substituting glycine for aspartate at amino acid 351.The antiestrogen ICI 182780 disrupts estrogen receptor nucleocytoplasmic shuttling.Effects of anti-estrogens on bone in castrated and intact female rats.Dual-energy x-ray absorptiometry of raloxifene effects on the lumbar vertebrae and femora of ovariectomized rats.Effects of the antiestrogens tamoxifen, toremifene, and ICI 182,780 on endometrial cancer growth.Antitumor action of physiological estradiol on tamoxifen-stimulated breast tumors grown in athymic mice.Rapid development of tamoxifen stimulated mutant p53 breast tumors (T47D) in athymic mice. Tamoxifen is used to prevent and treat estrogen receptor positive (ER+) breast cancer (BC); however, its chronic use can increase uterine cancer risk and induce tamoxifen resistance. The new molecule GW7604 (We have advanced that idea the 4-OHT and GW7604 have an interaction with aa351 (aspartate) by examining the external surface of the complexes. Background: tamoxifen is a nonsteroidal agent, tamoxifen has additional mechanisms behind these 2 classes of action needs to tamoxifen therapy to estrogen hormone. Endocrine-Related Cancer (2004) 11 643–658 ... Oestrogen receptor mechanism of action The target of tamoxifen in vivo is the ER, and levels of ER ... (for example uterus and breast respec-tively) has …

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