PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 15084463-4 2004 DeltaNbeta-cateninER was expressed in the epidermis of transgenic mice under the control of the keratin 14 promoter and beta-catenin activity was induced in adult epidermis by topical application of 4-hydroxytamoxifen (4OHT). hydroxytamoxifen 199-217 catenin (cadherin associated protein), beta 1 Mus musculus 6-18 14967725-4 2004 Application of 4-hydroxytamoxifen (4-OHT) induced Cre-ER(T)-mediated deletion of the floxed Cx43 allele. hydroxytamoxifen 15-33 gap junction protein, alpha 1 Mus musculus 92-96 14751226-2 2004 However, 4-hydroxytamoxifen and diethylstilbestrol were recently shown to bind to and inhibit ERRgamma activity. hydroxytamoxifen 9-27 estrogen related receptor gamma Homo sapiens 94-102 14617632-2 2004 In transient transfections of ER-positive HepG2-ER7 cells, PI-9 was strongly induced by estrogen, moxestrol (MOX), and 4-hydroxytamoxifen (OHT). hydroxytamoxifen 119-137 estrogen receptor 1 Homo sapiens 30-32 14617632-2 2004 In transient transfections of ER-positive HepG2-ER7 cells, PI-9 was strongly induced by estrogen, moxestrol (MOX), and 4-hydroxytamoxifen (OHT). hydroxytamoxifen 119-137 serpin family B member 9 Homo sapiens 59-63 14673139-0 2004 Selective estrogen receptor modulators 4-hydroxytamoxifen and raloxifene impact the stability and function of SRC-1 and SRC-3 coactivator proteins. hydroxytamoxifen 39-57 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 110-115 14715875-0 2004 Differential recruitment of coregulator proteins steroid receptor coactivator-1 and silencing mediator for retinoid and thyroid receptors to the estrogen receptor-estrogen response element by beta-estradiol and 4-hydroxytamoxifen in human breast cancer. hydroxytamoxifen 211-229 nuclear receptor coactivator 1 Homo sapiens 49-79 14715875-0 2004 Differential recruitment of coregulator proteins steroid receptor coactivator-1 and silencing mediator for retinoid and thyroid receptors to the estrogen receptor-estrogen response element by beta-estradiol and 4-hydroxytamoxifen in human breast cancer. hydroxytamoxifen 211-229 nuclear receptor corepressor 2 Homo sapiens 84-137 14734052-4 2004 To ablate Cx43 in adult mice in all cells that express Cx43 at a certain time, we targeted the 4-hydroxytamoxifen inducible Cre recombinase, Cre-ER(T), into the endogenous Cx43 locus. hydroxytamoxifen 95-113 gap junction protein, alpha 1 Mus musculus 10-14 14673139-0 2004 Selective estrogen receptor modulators 4-hydroxytamoxifen and raloxifene impact the stability and function of SRC-1 and SRC-3 coactivator proteins. hydroxytamoxifen 39-57 nuclear receptor coactivator 3 Homo sapiens 120-125 14673139-3 2004 Here, we examined the effects that different ERalpha ligands have on coactivator protein steady-state levels and demonstrate that the selective ER modulators (SERMs) 4-hydroxytamoxifen (4HT) and raloxifene are able to elevate SRC-1 and SRC-3 protein levels. hydroxytamoxifen 166-184 estrogen receptor 1 Homo sapiens 45-52 14673139-3 2004 Here, we examined the effects that different ERalpha ligands have on coactivator protein steady-state levels and demonstrate that the selective ER modulators (SERMs) 4-hydroxytamoxifen (4HT) and raloxifene are able to elevate SRC-1 and SRC-3 protein levels. hydroxytamoxifen 166-184 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 226-231 14673139-3 2004 Here, we examined the effects that different ERalpha ligands have on coactivator protein steady-state levels and demonstrate that the selective ER modulators (SERMs) 4-hydroxytamoxifen (4HT) and raloxifene are able to elevate SRC-1 and SRC-3 protein levels. hydroxytamoxifen 166-184 nuclear receptor coactivator 3 Homo sapiens 236-241 14709801-5 2003 In transfection experiments BPA and NPH activated in a direct manner the endogenous ERalpha in MCF7wt and MCF7SH cells, as the antiestrogen hydroxytamoxifen was able to reverse both responses. hydroxytamoxifen 140-156 estrogen receptor 1 Homo sapiens 84-91 14553828-4 2003 RESULTS: The treatment of CM and CF with either 4-OH tamoxifen or ICI 182,780 decreased DNA synthesis in the absence of apoptosis via an estrogen receptor-independent pathway. hydroxytamoxifen 48-62 estrogen receptor 1 Rattus norvegicus 137-154 14672741-0 2003 Mechanisms governing the accumulation of estrogen receptor alpha in MCF-7 breast cancer cells treated with hydroxytamoxifen and related antiestrogens. hydroxytamoxifen 107-123 estrogen receptor 1 Homo sapiens 41-64 14629178-0 2003 Simple and efficient production of (Z)-4-hydroxytamoxifen, a potent estrogen receptor modulator. hydroxytamoxifen 35-57 estrogen receptor 1 Homo sapiens 68-85 14665721-7 2003 Co-treatment with 4-hydroxytamoxifen partially reverses the suppressive effect of estrogen on MIP-1alpha levels. hydroxytamoxifen 18-36 chemokine (C-C motif) ligand 3 Mus musculus 94-104 12907598-3 2003 We now show that in hydroxytamoxifen-treated cells, transduction of the cell cycle inhibitor p27(Kip1) induces quiescence and insensitivity to growth stimulation by insulin/insulin-like growth factor I and epidermal growth factor/transforming growth factor alpha. hydroxytamoxifen 20-36 interferon alpha inducible protein 27 Homo sapiens 93-96 12907598-3 2003 We now show that in hydroxytamoxifen-treated cells, transduction of the cell cycle inhibitor p27(Kip1) induces quiescence and insensitivity to growth stimulation by insulin/insulin-like growth factor I and epidermal growth factor/transforming growth factor alpha. hydroxytamoxifen 20-36 cyclin dependent kinase inhibitor 1B Homo sapiens 97-101 12907598-3 2003 We now show that in hydroxytamoxifen-treated cells, transduction of the cell cycle inhibitor p27(Kip1) induces quiescence and insensitivity to growth stimulation by insulin/insulin-like growth factor I and epidermal growth factor/transforming growth factor alpha. hydroxytamoxifen 20-36 tumor necrosis factor Homo sapiens 230-262 12907598-4 2003 Furthermore, reinitiation of cell cycle progression by insulin/insulin-like growth factor I in hydroxytamoxifen-arrested cells involves dissociation of the corepressors nuclear receptor corepressor (N-CoR) and silencing mediator for retinoid and thyroid hormone receptor (SMRT) from nuclear estrogen receptor alpha and redistribution to the cytoplasm, a process that is inhibited by mitogen-activated protein/extracellular signal-regulated kinase, but not phosphatidylinositol 3"-kinase, inhibitors. hydroxytamoxifen 95-111 nuclear receptor corepressor 1 Homo sapiens 169-197 12907598-4 2003 Furthermore, reinitiation of cell cycle progression by insulin/insulin-like growth factor I in hydroxytamoxifen-arrested cells involves dissociation of the corepressors nuclear receptor corepressor (N-CoR) and silencing mediator for retinoid and thyroid hormone receptor (SMRT) from nuclear estrogen receptor alpha and redistribution to the cytoplasm, a process that is inhibited by mitogen-activated protein/extracellular signal-regulated kinase, but not phosphatidylinositol 3"-kinase, inhibitors. hydroxytamoxifen 95-111 nuclear receptor corepressor 1 Homo sapiens 199-204 12907598-4 2003 Furthermore, reinitiation of cell cycle progression by insulin/insulin-like growth factor I in hydroxytamoxifen-arrested cells involves dissociation of the corepressors nuclear receptor corepressor (N-CoR) and silencing mediator for retinoid and thyroid hormone receptor (SMRT) from nuclear estrogen receptor alpha and redistribution to the cytoplasm, a process that is inhibited by mitogen-activated protein/extracellular signal-regulated kinase, but not phosphatidylinositol 3"-kinase, inhibitors. hydroxytamoxifen 95-111 estrogen receptor 1 Homo sapiens 291-314 12738788-6 2003 In vivo and in vitro binding assays revealed that whereas 4-hydroxytamoxifen (OHT) induced binding of ERalpha to both an AF-1 coactivator complex (p68/p72 and p300) and corepressor complexes (N-CoR/SMRT), BBP selectively enhanced the binding to the AF-1 coactivators. hydroxytamoxifen 58-76 estrogen receptor 1 Homo sapiens 102-109 12738788-6 2003 In vivo and in vitro binding assays revealed that whereas 4-hydroxytamoxifen (OHT) induced binding of ERalpha to both an AF-1 coactivator complex (p68/p72 and p300) and corepressor complexes (N-CoR/SMRT), BBP selectively enhanced the binding to the AF-1 coactivators. hydroxytamoxifen 58-76 GATA zinc finger domain containing 2B Homo sapiens 147-150 12738788-6 2003 In vivo and in vitro binding assays revealed that whereas 4-hydroxytamoxifen (OHT) induced binding of ERalpha to both an AF-1 coactivator complex (p68/p72 and p300) and corepressor complexes (N-CoR/SMRT), BBP selectively enhanced the binding to the AF-1 coactivators. hydroxytamoxifen 58-76 DEAD-box helicase 17 Homo sapiens 151-154 12738788-6 2003 In vivo and in vitro binding assays revealed that whereas 4-hydroxytamoxifen (OHT) induced binding of ERalpha to both an AF-1 coactivator complex (p68/p72 and p300) and corepressor complexes (N-CoR/SMRT), BBP selectively enhanced the binding to the AF-1 coactivators. hydroxytamoxifen 58-76 E1A binding protein p300 Homo sapiens 159-163 12738788-6 2003 In vivo and in vitro binding assays revealed that whereas 4-hydroxytamoxifen (OHT) induced binding of ERalpha to both an AF-1 coactivator complex (p68/p72 and p300) and corepressor complexes (N-CoR/SMRT), BBP selectively enhanced the binding to the AF-1 coactivators. hydroxytamoxifen 58-76 nuclear receptor corepressor 1 Homo sapiens 192-197 12738788-6 2003 In vivo and in vitro binding assays revealed that whereas 4-hydroxytamoxifen (OHT) induced binding of ERalpha to both an AF-1 coactivator complex (p68/p72 and p300) and corepressor complexes (N-CoR/SMRT), BBP selectively enhanced the binding to the AF-1 coactivators. hydroxytamoxifen 58-76 nuclear receptor corepressor 2 Homo sapiens 198-202 12738788-6 2003 In vivo and in vitro binding assays revealed that whereas 4-hydroxytamoxifen (OHT) induced binding of ERalpha to both an AF-1 coactivator complex (p68/p72 and p300) and corepressor complexes (N-CoR/SMRT), BBP selectively enhanced the binding to the AF-1 coactivators. hydroxytamoxifen 58-76 TM2 domain containing 1 Homo sapiens 205-208 12767224-6 2003 Our results show that the Y295A/T333I/Y365L triple mutant is significantly suppressed by the known ERR inverse agonists 4-hydroxytamoxifen (OHT) and diethylstilbestrol (DES), in comparison to the wild-type dERR receptor, which was inefficiently suppressed by these substances. hydroxytamoxifen 120-138 estrogen-related receptor Drosophila melanogaster 99-102 12767224-6 2003 Our results show that the Y295A/T333I/Y365L triple mutant is significantly suppressed by the known ERR inverse agonists 4-hydroxytamoxifen (OHT) and diethylstilbestrol (DES), in comparison to the wild-type dERR receptor, which was inefficiently suppressed by these substances. hydroxytamoxifen 120-138 estrogen-related receptor Drosophila melanogaster 206-210 12591955-5 2003 When such transfectants were treated with an estrogen analogue, 4-hydroxytamoxifen (OHT), CSR was induced within 1 h. Cycloheximide or puromycin drastically suppressed OHT-induced CSR in AID-ER expressing AID-/- B cells when added 1 h before OHT but not after OHT, suggesting that de novo protein synthesis is required for an event downstream to AID expression in CSR. hydroxytamoxifen 64-82 activation induced cytidine deaminase Homo sapiens 187-190 12576490-2 2003 17Beta-estradiol (E2) and the antiestrogens 4-hydroxytamoxifen and ICI 182,780 induced reporter gene activity in MCF-7 and MDA-MB-231 cells cotransfected with human or mouse ERalpha (hERalpha or MOR), but not ERbeta and GC-rich constructs containing three tandem Sp1 binding sites (pSp13) or other E2-responsive GC-rich promoters. hydroxytamoxifen 44-62 estrogen receptor 1 (alpha) Mus musculus 174-181 12576490-2 2003 17Beta-estradiol (E2) and the antiestrogens 4-hydroxytamoxifen and ICI 182,780 induced reporter gene activity in MCF-7 and MDA-MB-231 cells cotransfected with human or mouse ERalpha (hERalpha or MOR), but not ERbeta and GC-rich constructs containing three tandem Sp1 binding sites (pSp13) or other E2-responsive GC-rich promoters. hydroxytamoxifen 44-62 Era like 12S mitochondrial rRNA chaperone 1 Homo sapiens 183-191 12576490-2 2003 17Beta-estradiol (E2) and the antiestrogens 4-hydroxytamoxifen and ICI 182,780 induced reporter gene activity in MCF-7 and MDA-MB-231 cells cotransfected with human or mouse ERalpha (hERalpha or MOR), but not ERbeta and GC-rich constructs containing three tandem Sp1 binding sites (pSp13) or other E2-responsive GC-rich promoters. hydroxytamoxifen 44-62 opioid receptor, mu 1 Mus musculus 195-198 12576490-2 2003 17Beta-estradiol (E2) and the antiestrogens 4-hydroxytamoxifen and ICI 182,780 induced reporter gene activity in MCF-7 and MDA-MB-231 cells cotransfected with human or mouse ERalpha (hERalpha or MOR), but not ERbeta and GC-rich constructs containing three tandem Sp1 binding sites (pSp13) or other E2-responsive GC-rich promoters. hydroxytamoxifen 44-62 estrogen receptor 2 (beta) Mus musculus 209-215 12725382-8 2003 The determined hormonal activities of estrogens on the interaction of YFP-hERalpha with ERE were as follows in their decreasing order: diethylstilbestrol (DES) > 17beta-estradiol (E2) <==> ethynylestradiol (EE2) > 4-hydroxy tamoxifen (OHT) > clomiphene (Clo). hydroxytamoxifen 226-245 Era like 12S mitochondrial rRNA chaperone 1 Homo sapiens 74-82 12769667-10 2003 The formation 4-hydroxytamoxifen is catalyzed by CYP2D6 and at a much lower level by CYP2C19. hydroxytamoxifen 14-32 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 49-55 12769667-10 2003 The formation 4-hydroxytamoxifen is catalyzed by CYP2D6 and at a much lower level by CYP2C19. hydroxytamoxifen 14-32 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 85-92 12611887-4 2003 First, an estrogen receptor-E2F1 fusion protein (ER-E2F1) potently activates the endogenous cyclin D3 mRNA upon treatment with 4-hydroxytamoxifen, which induces nuclear accumulation of the otherwise cytosolic fusion protein. hydroxytamoxifen 127-145 E2F transcription factor 1 L homeolog Xenopus laevis 28-32 12611887-4 2003 First, an estrogen receptor-E2F1 fusion protein (ER-E2F1) potently activates the endogenous cyclin D3 mRNA upon treatment with 4-hydroxytamoxifen, which induces nuclear accumulation of the otherwise cytosolic fusion protein. hydroxytamoxifen 127-145 E2F transcription factor 1 L homeolog Xenopus laevis 52-56 12554772-6 2003 Similarly, treatment with the antagonists 4-hydroxytamoxifen and EM-652 abolished all interactions between ERalpha and the SRC RIDs. hydroxytamoxifen 42-60 estrogen receptor 1 Homo sapiens 107-114 12591955-5 2003 When such transfectants were treated with an estrogen analogue, 4-hydroxytamoxifen (OHT), CSR was induced within 1 h. Cycloheximide or puromycin drastically suppressed OHT-induced CSR in AID-ER expressing AID-/- B cells when added 1 h before OHT but not after OHT, suggesting that de novo protein synthesis is required for an event downstream to AID expression in CSR. hydroxytamoxifen 64-82 activation induced cytidine deaminase Homo sapiens 205-208 12591955-5 2003 When such transfectants were treated with an estrogen analogue, 4-hydroxytamoxifen (OHT), CSR was induced within 1 h. Cycloheximide or puromycin drastically suppressed OHT-induced CSR in AID-ER expressing AID-/- B cells when added 1 h before OHT but not after OHT, suggesting that de novo protein synthesis is required for an event downstream to AID expression in CSR. hydroxytamoxifen 64-82 activation induced cytidine deaminase Homo sapiens 205-208 12623757-7 2003 CYP2D6 was the prime catalyst of tam-4-hydroxylation, whereas CYP2B6, 2C9 and 2C19 yielded only low levels of 4-OH-tam; nevertheless, in all cases the 4-OH-tam was radioactive, apparently resulting from reactions involving an NIH shift. hydroxytamoxifen 151-159 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 0-6 12732288-4 2003 To study the effect of 4EM on ER-alpha and ER-beta activity, we performed transient transfection assays and showed that 4EM activated ER-dependent gene transcription in a dose-dependent manner on both ER subtypes and this activity was inhibited by trans-4-hydroxytamoxifen (4HT). hydroxytamoxifen 248-272 estrogen receptor 1 Homo sapiens 30-38 12732288-4 2003 To study the effect of 4EM on ER-alpha and ER-beta activity, we performed transient transfection assays and showed that 4EM activated ER-dependent gene transcription in a dose-dependent manner on both ER subtypes and this activity was inhibited by trans-4-hydroxytamoxifen (4HT). hydroxytamoxifen 248-272 estrogen receptor 2 Homo sapiens 43-50 12124303-0 2002 Metabolism of tamoxifen by recombinant human cytochrome P450 enzymes: formation of the 4-hydroxy, 4"-hydroxy and N-desmethyl metabolites and isomerization of trans-4-hydroxytamoxifen. hydroxytamoxifen 158-182 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 45-60 12475720-6 2003 Tamoxifen and 4-hydroxytamoxifen showed partial ERalpha agonistic effects with a maximal response of 12% and raloxifene of 3-5%. hydroxytamoxifen 14-32 estrogen receptor 1 Rattus norvegicus 48-55 12409264-4 2002 A novel 4-hydroxytamoxifen (4-OHT)-dependent transcriptional regulator (called HEA-3) was constructed by fusing in-frame the DNA binding domain of the human hepatocyte nuclear factor-1alpha (HNF1alpha), which is not expressed in muscle cells, a G(521)R mutant of the ligand binding domain of human estrogen receptor-alpha (ERalpha), and the activation domain derived from human nuclear factor-kappaB p65 subunit (NF-kappaB p65). hydroxytamoxifen 8-26 HNF1 homeobox A Homo sapiens 157-189 12409264-4 2002 A novel 4-hydroxytamoxifen (4-OHT)-dependent transcriptional regulator (called HEA-3) was constructed by fusing in-frame the DNA binding domain of the human hepatocyte nuclear factor-1alpha (HNF1alpha), which is not expressed in muscle cells, a G(521)R mutant of the ligand binding domain of human estrogen receptor-alpha (ERalpha), and the activation domain derived from human nuclear factor-kappaB p65 subunit (NF-kappaB p65). hydroxytamoxifen 8-26 HNF1 homeobox A Homo sapiens 191-200 12409264-4 2002 A novel 4-hydroxytamoxifen (4-OHT)-dependent transcriptional regulator (called HEA-3) was constructed by fusing in-frame the DNA binding domain of the human hepatocyte nuclear factor-1alpha (HNF1alpha), which is not expressed in muscle cells, a G(521)R mutant of the ligand binding domain of human estrogen receptor-alpha (ERalpha), and the activation domain derived from human nuclear factor-kappaB p65 subunit (NF-kappaB p65). hydroxytamoxifen 8-26 estrogen receptor 1 Homo sapiens 298-321 12409264-4 2002 A novel 4-hydroxytamoxifen (4-OHT)-dependent transcriptional regulator (called HEA-3) was constructed by fusing in-frame the DNA binding domain of the human hepatocyte nuclear factor-1alpha (HNF1alpha), which is not expressed in muscle cells, a G(521)R mutant of the ligand binding domain of human estrogen receptor-alpha (ERalpha), and the activation domain derived from human nuclear factor-kappaB p65 subunit (NF-kappaB p65). hydroxytamoxifen 8-26 estrogen receptor 1 Homo sapiens 323-330 12409264-4 2002 A novel 4-hydroxytamoxifen (4-OHT)-dependent transcriptional regulator (called HEA-3) was constructed by fusing in-frame the DNA binding domain of the human hepatocyte nuclear factor-1alpha (HNF1alpha), which is not expressed in muscle cells, a G(521)R mutant of the ligand binding domain of human estrogen receptor-alpha (ERalpha), and the activation domain derived from human nuclear factor-kappaB p65 subunit (NF-kappaB p65). hydroxytamoxifen 8-26 RELA proto-oncogene, NF-kB subunit Homo sapiens 378-411 12409264-4 2002 A novel 4-hydroxytamoxifen (4-OHT)-dependent transcriptional regulator (called HEA-3) was constructed by fusing in-frame the DNA binding domain of the human hepatocyte nuclear factor-1alpha (HNF1alpha), which is not expressed in muscle cells, a G(521)R mutant of the ligand binding domain of human estrogen receptor-alpha (ERalpha), and the activation domain derived from human nuclear factor-kappaB p65 subunit (NF-kappaB p65). hydroxytamoxifen 8-26 RELA proto-oncogene, NF-kB subunit Homo sapiens 413-426 12419016-6 2002 Tamoxifen, N-desmethyltamoxifen, 4-hydroxytamoxifen and 3-hydroxytamoxifen also reversibly inhibited the activity of cDNA-expressed CYP3A4, CYP3A5 and CYP1B1. hydroxytamoxifen 33-51 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 132-138 12419016-6 2002 Tamoxifen, N-desmethyltamoxifen, 4-hydroxytamoxifen and 3-hydroxytamoxifen also reversibly inhibited the activity of cDNA-expressed CYP3A4, CYP3A5 and CYP1B1. hydroxytamoxifen 33-51 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 140-146 12419016-6 2002 Tamoxifen, N-desmethyltamoxifen, 4-hydroxytamoxifen and 3-hydroxytamoxifen also reversibly inhibited the activity of cDNA-expressed CYP3A4, CYP3A5 and CYP1B1. hydroxytamoxifen 33-51 cytochrome P450 family 1 subfamily B member 1 Homo sapiens 151-157 12154049-2 2002 We have developed an in vitro system in which some SERMs (4-hydroxytamoxifen and resveratrol) demonstrate estrogenic response through wild-type (wt) ER, whereas others (raloxifene and GW7604) remain antiestrogenic. hydroxytamoxifen 58-76 estrogen receptor 1 Homo sapiens 52-54 12354757-4 2002 By terminal deoxynucleotidyltransferase-mediated dUTP-biotin nick end labeling and cytoplasmic nucleosome enzyme-linked immunosorbent assay, we demonstrated that 4-hydroxytamoxifen-induced apoptosis was totally lost in PTPL1/FAP-1 antisense transfectants in which enzyme expression was abrogated, revealing the crucial role of this phosphatase in the apoptotic process in human breast cancer cells. hydroxytamoxifen 162-180 protein tyrosine phosphatase non-receptor type 13 Homo sapiens 219-224 12354757-4 2002 By terminal deoxynucleotidyltransferase-mediated dUTP-biotin nick end labeling and cytoplasmic nucleosome enzyme-linked immunosorbent assay, we demonstrated that 4-hydroxytamoxifen-induced apoptosis was totally lost in PTPL1/FAP-1 antisense transfectants in which enzyme expression was abrogated, revealing the crucial role of this phosphatase in the apoptotic process in human breast cancer cells. hydroxytamoxifen 162-180 protein tyrosine phosphatase non-receptor type 13 Homo sapiens 225-230 12413861-0 2002 Synthesis and estrogen receptor affinity of a 4-hydroxytamoxifen-labeled ligand for diagnostic imaging. hydroxytamoxifen 46-64 estrogen receptor 1 Homo sapiens 14-31 12413861-2 2002 Tamoxifen and its primary metabolite 4-hydroxytamoxifen are common estrogen receptor ligands. hydroxytamoxifen 37-55 estrogen receptor 1 Homo sapiens 67-84 12419790-1 2002 BACKGROUND: Human sulfotransferase 1A1 (SULT1A1) catalyzes the sulfation of a variety of phenolic and estrogenic compounds, including 4-hydroxytamoxifen (4-OH TAM), the active metabolite of tamoxifen. hydroxytamoxifen 134-152 sulfotransferase family 1A member 1 Homo sapiens 18-38 12419790-1 2002 BACKGROUND: Human sulfotransferase 1A1 (SULT1A1) catalyzes the sulfation of a variety of phenolic and estrogenic compounds, including 4-hydroxytamoxifen (4-OH TAM), the active metabolite of tamoxifen. hydroxytamoxifen 134-152 sulfotransferase family 1A member 1 Homo sapiens 40-47 12147685-7 2002 Activation of STAT3 in fetal hepatocytes of transgenic mice expressing the STAT3-estrogen receptor fusion protein by 4-hydroxytamoxifen resulted in the suppression of cyclin D1 and D2 expression. hydroxytamoxifen 117-135 signal transducer and activator of transcription 3 Mus musculus 14-19 12147685-7 2002 Activation of STAT3 in fetal hepatocytes of transgenic mice expressing the STAT3-estrogen receptor fusion protein by 4-hydroxytamoxifen resulted in the suppression of cyclin D1 and D2 expression. hydroxytamoxifen 117-135 signal transducer and activator of transcription 3 Mus musculus 75-80 12147685-7 2002 Activation of STAT3 in fetal hepatocytes of transgenic mice expressing the STAT3-estrogen receptor fusion protein by 4-hydroxytamoxifen resulted in the suppression of cyclin D1 and D2 expression. hydroxytamoxifen 117-135 cyclin D1 Mus musculus 167-176 12373635-3 2002 To study the function and regulation of the transcription factor FKHR in hepatic cells, we constructed a hydroxytamoxifen-inducible version of FKHR by fusing a part of the hormone binding domain of the estrogen receptor (ER) to the C-terminus of FKHR (FKHR-ER). hydroxytamoxifen 105-121 forkhead box O1 Rattus norvegicus 65-69 12373635-3 2002 To study the function and regulation of the transcription factor FKHR in hepatic cells, we constructed a hydroxytamoxifen-inducible version of FKHR by fusing a part of the hormone binding domain of the estrogen receptor (ER) to the C-terminus of FKHR (FKHR-ER). hydroxytamoxifen 105-121 forkhead box O1 Rattus norvegicus 143-147 12373635-3 2002 To study the function and regulation of the transcription factor FKHR in hepatic cells, we constructed a hydroxytamoxifen-inducible version of FKHR by fusing a part of the hormone binding domain of the estrogen receptor (ER) to the C-terminus of FKHR (FKHR-ER). hydroxytamoxifen 105-121 estrogen receptor 1 Rattus norvegicus 202-219 12373635-3 2002 To study the function and regulation of the transcription factor FKHR in hepatic cells, we constructed a hydroxytamoxifen-inducible version of FKHR by fusing a part of the hormone binding domain of the estrogen receptor (ER) to the C-terminus of FKHR (FKHR-ER). hydroxytamoxifen 105-121 estrogen receptor 1 Rattus norvegicus 221-223 12373635-3 2002 To study the function and regulation of the transcription factor FKHR in hepatic cells, we constructed a hydroxytamoxifen-inducible version of FKHR by fusing a part of the hormone binding domain of the estrogen receptor (ER) to the C-terminus of FKHR (FKHR-ER). hydroxytamoxifen 105-121 forkhead box O1 Rattus norvegicus 143-147 12373635-3 2002 To study the function and regulation of the transcription factor FKHR in hepatic cells, we constructed a hydroxytamoxifen-inducible version of FKHR by fusing a part of the hormone binding domain of the estrogen receptor (ER) to the C-terminus of FKHR (FKHR-ER). hydroxytamoxifen 105-121 forkhead box O1 Rattus norvegicus 252-259 12373635-4 2002 In HepG2-cells transiently transfected with plasmids encoding the FKHR-ER fusion protein and a glucose-6-phosphatase reporter construct, hydroxytamoxifen induced a marked induction of glucose-6-phosphatase promoter activity, whereas no effect was observed in control cells. hydroxytamoxifen 137-153 forkhead box O1 Rattus norvegicus 66-73 12373635-4 2002 In HepG2-cells transiently transfected with plasmids encoding the FKHR-ER fusion protein and a glucose-6-phosphatase reporter construct, hydroxytamoxifen induced a marked induction of glucose-6-phosphatase promoter activity, whereas no effect was observed in control cells. hydroxytamoxifen 137-153 glucose-6-phosphatase catalytic subunit 1 Rattus norvegicus 95-116 12373635-4 2002 In HepG2-cells transiently transfected with plasmids encoding the FKHR-ER fusion protein and a glucose-6-phosphatase reporter construct, hydroxytamoxifen induced a marked induction of glucose-6-phosphatase promoter activity, whereas no effect was observed in control cells. hydroxytamoxifen 137-153 glucose-6-phosphatase catalytic subunit 1 Rattus norvegicus 184-205 12124303-1 2002 The cytochrome P450 (P450)-mediated biotransformation of tamoxifen is important in determining both the clearance of the drug and its conversion to the active metabolite, trans-4-hydroxytamoxifen. hydroxytamoxifen 171-195 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 4-19 12124303-10 2002 CYP1B1 was the principal catalyst of 4-hydroxytamoxifen trans-cis isomerization but CYP2B6 and CYP2C19 also contributed. hydroxytamoxifen 37-55 cytochrome P450 family 1 subfamily B member 1 Homo sapiens 0-6 11904289-4 2002 Transfection of tissue culture cells with expression vectors encoding this hybrid protein allows the signal transduction function of beta-catenin to be induced by the synthetic estrogen, 4-hydroxytamoxifen, leading to regulated activation of a beta-catenin-lymphocyte enhancer-binding factor-dependent reporter gene as well as induction of endogenous cyclin D1 expression. hydroxytamoxifen 187-205 catenin beta 1 Homo sapiens 133-145 12161509-6 2002 An ER alpha-mixed agonist/antagonist and ER beta antagonist, 4-hydroxytamoxifen, also down-regulated CRH gene expression. hydroxytamoxifen 61-79 estrogen receptor 1 Homo sapiens 3-11 12161509-6 2002 An ER alpha-mixed agonist/antagonist and ER beta antagonist, 4-hydroxytamoxifen, also down-regulated CRH gene expression. hydroxytamoxifen 61-79 estrogen receptor 2 Homo sapiens 41-48 12161509-6 2002 An ER alpha-mixed agonist/antagonist and ER beta antagonist, 4-hydroxytamoxifen, also down-regulated CRH gene expression. hydroxytamoxifen 61-79 corticotropin releasing hormone Homo sapiens 101-104 12004054-10 2002 The cooperational function of these two pathways was confirmed by experiments with cell lines stably expressing 4-hydroxytamoxifen-inducible oncogenic Raf-1 (DeltaRaf-1:ER[DD]). hydroxytamoxifen 112-130 Raf-1 proto-oncogene, serine/threonine kinase Homo sapiens 151-156 12122114-5 2002 Crucially, addition of the anti-estrogen 4-hydroxytamoxifen caused a differential recruitment in vivo of ERalpha and ERbeta onto the hTERT promoter and inhibited telomerase activity. hydroxytamoxifen 41-59 estrogen receptor 1 Homo sapiens 105-112 12122114-5 2002 Crucially, addition of the anti-estrogen 4-hydroxytamoxifen caused a differential recruitment in vivo of ERalpha and ERbeta onto the hTERT promoter and inhibited telomerase activity. hydroxytamoxifen 41-59 estrogen receptor 2 Homo sapiens 117-123 12122114-5 2002 Crucially, addition of the anti-estrogen 4-hydroxytamoxifen caused a differential recruitment in vivo of ERalpha and ERbeta onto the hTERT promoter and inhibited telomerase activity. hydroxytamoxifen 41-59 telomerase reverse transcriptase Homo sapiens 133-138 12113885-9 2002 Furthermore, we showed that the estrogen-induced increase in the FasL protein and mRNA levels could be abolished by 4-hydroxytamoxifen, which suggests that the observed increase in FasL expression was mediated by estrogen receptor. hydroxytamoxifen 116-134 Fas ligand Homo sapiens 65-69 12113885-9 2002 Furthermore, we showed that the estrogen-induced increase in the FasL protein and mRNA levels could be abolished by 4-hydroxytamoxifen, which suggests that the observed increase in FasL expression was mediated by estrogen receptor. hydroxytamoxifen 116-134 Fas ligand Homo sapiens 181-185 12113885-9 2002 Furthermore, we showed that the estrogen-induced increase in the FasL protein and mRNA levels could be abolished by 4-hydroxytamoxifen, which suggests that the observed increase in FasL expression was mediated by estrogen receptor. hydroxytamoxifen 116-134 estrogen receptor 1 Homo sapiens 213-230 12067725-4 2002 100 nM 17beta-estradiol and 4-hydroxytamoxifen blocked high calcium-induced cytochrome c release from mitochondria but not mitochondrial swelling. hydroxytamoxifen 28-46 cytochrome c, somatic Homo sapiens 76-88 11904289-4 2002 Transfection of tissue culture cells with expression vectors encoding this hybrid protein allows the signal transduction function of beta-catenin to be induced by the synthetic estrogen, 4-hydroxytamoxifen, leading to regulated activation of a beta-catenin-lymphocyte enhancer-binding factor-dependent reporter gene as well as induction of endogenous cyclin D1 expression. hydroxytamoxifen 187-205 catenin beta 1 Homo sapiens 244-256 11981757-4 2002 By placing 2 mutated hormone-binding domains of murine estrogen receptor (Mer) at both termini of the Cre, we show that the fusion protein is active only on administration of the synthetic estrogen antagonist 4-hydroxytamoxifen (4-OHT) without any background in the absence of the inducing agent. hydroxytamoxifen 209-227 estrogen receptor 1 (alpha) Mus musculus 55-72 12082641-2 2002 In Ba/F3 cells, activation of exogenous AML1 (RUNX1)-ER with 4-hydroxytamoxifen prevents inhibition of G1 progression mediated by CBFbeta-SMMHC, a CBF oncoprotein. hydroxytamoxifen 61-79 runt related transcription factor 1 Mus musculus 40-44 12082641-2 2002 In Ba/F3 cells, activation of exogenous AML1 (RUNX1)-ER with 4-hydroxytamoxifen prevents inhibition of G1 progression mediated by CBFbeta-SMMHC, a CBF oncoprotein. hydroxytamoxifen 61-79 runt related transcription factor 1 Mus musculus 46-51 12082641-2 2002 In Ba/F3 cells, activation of exogenous AML1 (RUNX1)-ER with 4-hydroxytamoxifen prevents inhibition of G1 progression mediated by CBFbeta-SMMHC, a CBF oncoprotein. hydroxytamoxifen 61-79 core binding factor beta Mus musculus 130-137 12082641-2 2002 In Ba/F3 cells, activation of exogenous AML1 (RUNX1)-ER with 4-hydroxytamoxifen prevents inhibition of G1 progression mediated by CBFbeta-SMMHC, a CBF oncoprotein. hydroxytamoxifen 61-79 myosin, heavy polypeptide 11, smooth muscle Mus musculus 138-143 12168826-0 2002 NAD(P)H: quinone oxidoreductase enhances proliferation inhibition by 4-hydroxytamoxifen. hydroxytamoxifen 69-87 crystallin zeta Homo sapiens 9-31 11950795-0 2002 Induction of cytochrome P450 3A4 in primary human hepatocytes and activation of the human pregnane X receptor by tamoxifen and 4-hydroxytamoxifen. hydroxytamoxifen 127-145 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 13-32 11950795-0 2002 Induction of cytochrome P450 3A4 in primary human hepatocytes and activation of the human pregnane X receptor by tamoxifen and 4-hydroxytamoxifen. hydroxytamoxifen 127-145 nuclear receptor subfamily 1 group I member 2 Homo sapiens 90-109 11950795-5 2002 Here, we report that tamoxifen and its metabolite 4-hydroxytamoxifen markedly induce cytochrome P450 3A4, a drug-metabolizing enzyme of central importance, in primary cultures of human hepatocytes. hydroxytamoxifen 50-68 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 85-104 11950795-6 2002 Tamoxifen and 4-hydroxytamoxifen (1-10 microM) significantly increased the CYP3A4 expression and activity (measured as the rate of testosterone 6beta-hydroxylation). hydroxytamoxifen 14-32 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 75-81 11950795-8 2002 At this level, tamoxifen and 4-hydroxytamoxifen caused a 1.5- to 3.3-fold (mean, 2.1-fold) and 3.4- to 17-fold (mean, 7.5-fold) increase in the CYP3A4 activity, respectively. hydroxytamoxifen 29-47 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 144-150 11950795-11 2002 Furthermore, tamoxifen and 4-hydroxytamoxifen efficaciously activated the human pregnane X receptor (hPXR; also known as the steroid xenobiotic receptor), a key regulator of CYP3A4 expression. hydroxytamoxifen 27-45 nuclear receptor subfamily 1 group I member 2 Homo sapiens 80-99 11950795-11 2002 Furthermore, tamoxifen and 4-hydroxytamoxifen efficaciously activated the human pregnane X receptor (hPXR; also known as the steroid xenobiotic receptor), a key regulator of CYP3A4 expression. hydroxytamoxifen 27-45 nuclear receptor subfamily 1 group I member 2 Homo sapiens 101-105 11950795-11 2002 Furthermore, tamoxifen and 4-hydroxytamoxifen efficaciously activated the human pregnane X receptor (hPXR; also known as the steroid xenobiotic receptor), a key regulator of CYP3A4 expression. hydroxytamoxifen 27-45 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 174-180 11950795-12 2002 The efficacy of tamoxifen and 4-hydroxytamoxifen relative to rifampicin for hPXR activation was approximately 30 and 60%, respectively. hydroxytamoxifen 30-48 nuclear receptor subfamily 1 group I member 2 Homo sapiens 76-80 11823467-0 2002 Mutations targeted to a predicted helix in the extreme carboxyl-terminal region of the human estrogen receptor-alpha alter its response to estradiol and 4-hydroxytamoxifen. hydroxytamoxifen 153-171 estrogen receptor 1 Homo sapiens 93-116 12481303-9 2002 Human phenol-sulfating sulfotransferase and human estrogen sulfotransferase are the major enzymes for the sulfation of 4-OH-TAM. hydroxytamoxifen 119-127 sulfotransferase family 1E member 1 Homo sapiens 50-75 12007790-3 2002 NIH 3T3 cells expressing a hydroxytamoxifen-inducible oncogenic c-Raf-1-oestrogen receptor fusion protein (c-Raf-1-BxB-ER, N-BxB-ER cells) undergo morphological transformation upon stimulation of the Raf kinase. hydroxytamoxifen 27-43 v-raf-leukemia viral oncogene 1 Mus musculus 64-69 12007790-3 2002 NIH 3T3 cells expressing a hydroxytamoxifen-inducible oncogenic c-Raf-1-oestrogen receptor fusion protein (c-Raf-1-BxB-ER, N-BxB-ER cells) undergo morphological transformation upon stimulation of the Raf kinase. hydroxytamoxifen 27-43 v-raf-leukemia viral oncogene 1 Mus musculus 107-112 12007790-3 2002 NIH 3T3 cells expressing a hydroxytamoxifen-inducible oncogenic c-Raf-1-oestrogen receptor fusion protein (c-Raf-1-BxB-ER, N-BxB-ER cells) undergo morphological transformation upon stimulation of the Raf kinase. hydroxytamoxifen 27-43 zinc fingers and homeoboxes 2 Mus musculus 66-69 11751902-2 2002 4-Hydroxytamoxifen is a full agonist at a transforming growth factor alpha target gene in situ in MDA-MB-231 human breast cancer cells stably transfected with the wild-type ERalpha. hydroxytamoxifen 0-18 tumor necrosis factor Homo sapiens 42-74 11751902-2 2002 4-Hydroxytamoxifen is a full agonist at a transforming growth factor alpha target gene in situ in MDA-MB-231 human breast cancer cells stably transfected with the wild-type ERalpha. hydroxytamoxifen 0-18 estrogen receptor 1 Homo sapiens 173-180 11751902-4 2002 Because D351G ERalpha allosterically silences activation function-1 activity in the 4-hydroxytamoxifen-ERalpha complex with the complete loss of estrogen-like activity, we examined the converse interaction of amino acid 351 and the piperidine ring of the antiestrogen side chain of raloxifene to enhance estrogen-like action. hydroxytamoxifen 84-102 estrogen receptor 1 Homo sapiens 103-110 11861507-3 2002 We report that SHP interacts with 4-hydroxytamoxifen (4-OHT) or E2-occupied ER(alpha) in a temperature-dependent manner in vitro. hydroxytamoxifen 34-52 nuclear receptor subfamily 0 group B member 2 Homo sapiens 15-18 11864604-3 2002 Docking of the previously reported ERR antagonists, diethylstilbestrol and 4-hydroxytamoxifen, requires structural rearrangements enlarging the ligand binding pocket that can only be accommodated with an antagonist LBD conformation. hydroxytamoxifen 75-93 solute carrier family 7 member 1 Homo sapiens 35-38 12017331-7 2002 The in vitro experiments showed that TAM and 4-OH-TAM stimulate established glioma cell lines to increase their secretion of TGF-beta2. hydroxytamoxifen 45-53 transforming growth factor beta 2 Homo sapiens 125-134 12439862-7 2002 The most conspicuous difference between beta-HCH and HRG in MCF-7 foci formation test was their response to 4-hydroxytamoxifen and LY294002, a PI3K inhibitor, i.e., the action of beta-HCH was inhibited by 4-hydroxytamoxifen but stimulated by LY294002, whereas that of heregulin was suppressed by LY294002 but stimulated by 4-hydroxytamoxifen. hydroxytamoxifen 108-126 histidine rich glycoprotein Homo sapiens 53-56 12439862-7 2002 The most conspicuous difference between beta-HCH and HRG in MCF-7 foci formation test was their response to 4-hydroxytamoxifen and LY294002, a PI3K inhibitor, i.e., the action of beta-HCH was inhibited by 4-hydroxytamoxifen but stimulated by LY294002, whereas that of heregulin was suppressed by LY294002 but stimulated by 4-hydroxytamoxifen. hydroxytamoxifen 205-223 histidine rich glycoprotein Homo sapiens 53-56 12439862-7 2002 The most conspicuous difference between beta-HCH and HRG in MCF-7 foci formation test was their response to 4-hydroxytamoxifen and LY294002, a PI3K inhibitor, i.e., the action of beta-HCH was inhibited by 4-hydroxytamoxifen but stimulated by LY294002, whereas that of heregulin was suppressed by LY294002 but stimulated by 4-hydroxytamoxifen. hydroxytamoxifen 205-223 histidine rich glycoprotein Homo sapiens 53-56 11432835-3 2001 The anti-estrogen 4-hydroxytamoxifen blocks Rsk2-mediated activation of ERalpha, by inducing a conformation of ERalpha in which the Rsk2 docking site is masked. hydroxytamoxifen 18-36 ribosomal protein S6 kinase A3 Homo sapiens 44-48 11682626-8 2001 Binding of 4-hydroxytamoxifen (OHT) to the hERalpha C-terminal region induced a functional AF-1 conformation in vitro through this N- and C-terminal interaction. hydroxytamoxifen 11-29 Era like 12S mitochondrial rRNA chaperone 1 Homo sapiens 43-51 11682626-8 2001 Binding of 4-hydroxytamoxifen (OHT) to the hERalpha C-terminal region induced a functional AF-1 conformation in vitro through this N- and C-terminal interaction. hydroxytamoxifen 11-29 interferon gamma receptor 2 Homo sapiens 91-95 11773441-6 2002 PAK6 also bound to the ERalpha, and binding was enhanced by 4-hydroxytamoxifen. hydroxytamoxifen 60-78 p21 (RAC1) activated kinase 6 Homo sapiens 0-4 11773441-6 2002 PAK6 also bound to the ERalpha, and binding was enhanced by 4-hydroxytamoxifen. hydroxytamoxifen 60-78 estrogen receptor 1 Homo sapiens 23-30 11447273-0 2001 4-Hydroxytamoxifen binds to and deactivates the estrogen-related receptor gamma. hydroxytamoxifen 0-18 estrogen related receptor gamma Homo sapiens 48-79 11447273-2 2001 By using a peptide sensor assay, we have identified the stilbenes diethylstilbestrol (DES), tamoxifen (TAM), and 4-hydroxytamoxifen (4-OHT) as high-affinity ligands for ERR gamma. hydroxytamoxifen 113-131 estrogen related receptor gamma Homo sapiens 169-178 11432835-3 2001 The anti-estrogen 4-hydroxytamoxifen blocks Rsk2-mediated activation of ERalpha, by inducing a conformation of ERalpha in which the Rsk2 docking site is masked. hydroxytamoxifen 18-36 estrogen receptor 1 Homo sapiens 72-79 11432835-3 2001 The anti-estrogen 4-hydroxytamoxifen blocks Rsk2-mediated activation of ERalpha, by inducing a conformation of ERalpha in which the Rsk2 docking site is masked. hydroxytamoxifen 18-36 estrogen receptor 1 Homo sapiens 111-118 11432835-3 2001 The anti-estrogen 4-hydroxytamoxifen blocks Rsk2-mediated activation of ERalpha, by inducing a conformation of ERalpha in which the Rsk2 docking site is masked. hydroxytamoxifen 18-36 ribosomal protein S6 kinase A3 Homo sapiens 132-136 11325832-1 2001 4-Hydroxytamoxifen (4-OHT), a selective estrogen receptor modulator, is an agonist at a transforming growth factor-alpha (TGF-alpha) target gene in situ in MDA-MB-231 human breast cancer cells stably transfected with wild-type human ERalpha. hydroxytamoxifen 0-18 tumor necrosis factor Homo sapiens 88-120 11530283-0 2001 Estrogen receptor alpha mediated induction of the transforming growth factor alpha gene by estradiol and 4-hydroxytamoxifen in MDA-MB-231 breast cancer cells. hydroxytamoxifen 105-123 estrogen receptor 1 Homo sapiens 0-23 11530283-0 2001 Estrogen receptor alpha mediated induction of the transforming growth factor alpha gene by estradiol and 4-hydroxytamoxifen in MDA-MB-231 breast cancer cells. hydroxytamoxifen 105-123 tumor necrosis factor Homo sapiens 50-82 11530283-1 2001 The selective estrogen receptor modulator, 4-hydroxytamoxifen (4-OHT) is a full agonist at the transforming growth factor (TGF) alpha gene in ER negative breast cancer cells stably transfected with ER alpha cDNA (Levenson et al., Br. hydroxytamoxifen 43-61 transforming growth factor alpha Homo sapiens 123-133 11530283-1 2001 The selective estrogen receptor modulator, 4-hydroxytamoxifen (4-OHT) is a full agonist at the transforming growth factor (TGF) alpha gene in ER negative breast cancer cells stably transfected with ER alpha cDNA (Levenson et al., Br. hydroxytamoxifen 43-61 estrogen receptor 1 Homo sapiens 198-206 11325832-1 2001 4-Hydroxytamoxifen (4-OHT), a selective estrogen receptor modulator, is an agonist at a transforming growth factor-alpha (TGF-alpha) target gene in situ in MDA-MB-231 human breast cancer cells stably transfected with wild-type human ERalpha. hydroxytamoxifen 0-18 transforming growth factor alpha Homo sapiens 122-131 11325832-1 2001 4-Hydroxytamoxifen (4-OHT), a selective estrogen receptor modulator, is an agonist at a transforming growth factor-alpha (TGF-alpha) target gene in situ in MDA-MB-231 human breast cancer cells stably transfected with wild-type human ERalpha. hydroxytamoxifen 0-18 estrogen receptor 1 Homo sapiens 233-240 11274368-4 2001 We found that activation of a Myc-estrogen receptor fusion protein by 4-hydroxytamoxifen in mouse cells resulted in suppression of endogenous p21 transcription. hydroxytamoxifen 70-88 myelocytomatosis oncogene Mus musculus 30-33 11320145-5 2001 Addition of the specific estradiol-receptor antagonist hydroxytamoxifen suppressed the estradiol-induced formation of micronuclei in MCF-7 cells. hydroxytamoxifen 55-71 estrogen receptor 1 Homo sapiens 25-43 11274368-4 2001 We found that activation of a Myc-estrogen receptor fusion protein by 4-hydroxytamoxifen in mouse cells resulted in suppression of endogenous p21 transcription. hydroxytamoxifen 70-88 cyclin-dependent kinase inhibitor 1A (P21) Mus musculus 142-145 11181531-8 2001 Because it is known that some antiestrogens can also display tissue-specific agonistic properties, 4-hydroxytamoxifen was tested for its capacity in repressing NF-kappa B activity and was found to be active (albeit less efficient than 17 beta-estradiol) and, interestingly, only with ER alpha. hydroxytamoxifen 99-117 nuclear factor kappa B subunit 1 Homo sapiens 160-170 11306549-2 2001 One approach to regulate Cre activity utilizes a mutant estrogen hormone-binding domain (ERT) to keep Cre inactive unless the non-steroidal estrogen analog 4-hydroxytamoxifen (OHT) is present. hydroxytamoxifen 156-174 SH2 domain containing 1B2 Mus musculus 89-92 11306182-5 2001 ERalpha, occupied by estradiol (E2) or 4-hydroxytamoxifen (4-OHT), was incubated with select EREs and digested by chymotrypsin followed by a Western analysis with antibodies to ERalpha. hydroxytamoxifen 39-57 estrogen receptor 1 Homo sapiens 0-7 11181531-8 2001 Because it is known that some antiestrogens can also display tissue-specific agonistic properties, 4-hydroxytamoxifen was tested for its capacity in repressing NF-kappa B activity and was found to be active (albeit less efficient than 17 beta-estradiol) and, interestingly, only with ER alpha. hydroxytamoxifen 99-117 estrogen receptor 1 Homo sapiens 284-292 11134296-6 2001 The Nef-ER is kept in an inactive state due to steric hindrance, and addition of the membrane-permeable drug 4-hydroxytamoxifen (4-HT), which binds to the ER domain, leads to inducible activation of Nef-ER within cells. hydroxytamoxifen 109-127 S100 calcium binding protein B Homo sapiens 4-7 11384868-5 2001 Incubation of cells in E(2)-containing growth medium caused cell proliferation and hyperphosphorylation of pRB; the latter effect was seen maximally between 24-72 h. The E(2)-induced hyperphosphorylation of pRB and increase in the level of p53 were sensitive to the presence of ICI and 4-hydroxy tamoxifen (OHT). hydroxytamoxifen 286-305 RB transcriptional corepressor 1 Homo sapiens 107-110 11384868-5 2001 Incubation of cells in E(2)-containing growth medium caused cell proliferation and hyperphosphorylation of pRB; the latter effect was seen maximally between 24-72 h. The E(2)-induced hyperphosphorylation of pRB and increase in the level of p53 were sensitive to the presence of ICI and 4-hydroxy tamoxifen (OHT). hydroxytamoxifen 286-305 RB transcriptional corepressor 1 Homo sapiens 207-210 11134296-6 2001 The Nef-ER is kept in an inactive state due to steric hindrance, and addition of the membrane-permeable drug 4-hydroxytamoxifen (4-HT), which binds to the ER domain, leads to inducible activation of Nef-ER within cells. hydroxytamoxifen 109-127 S100 calcium binding protein B Homo sapiens 199-202 11162936-5 2000 Antiestrogens such as hydroxytamoxifen, which are mixed agonist/antagonists through ERalpha, are pure antagonists through ERbeta at estrogen response element-containing gene sites. hydroxytamoxifen 22-38 estrogen receptor 1 Homo sapiens 84-91 11113208-7 2001 CIA-ERalpha interactions were found to be independent of AF-2 and enhanced by the antiestrogens EM-652 and ICI 182,780 but not by 4-hydroxytamoxifen and raloxifene. hydroxytamoxifen 130-148 nuclear receptor coactivator 5 Homo sapiens 0-3 11113208-7 2001 CIA-ERalpha interactions were found to be independent of AF-2 and enhanced by the antiestrogens EM-652 and ICI 182,780 but not by 4-hydroxytamoxifen and raloxifene. hydroxytamoxifen 130-148 estrogen receptor 1 Homo sapiens 4-11 11162936-5 2000 Antiestrogens such as hydroxytamoxifen, which are mixed agonist/antagonists through ERalpha, are pure antagonists through ERbeta at estrogen response element-containing gene sites. hydroxytamoxifen 22-38 estrogen receptor 2 Homo sapiens 122-128 10873560-2 2000 4-Hydroxytamoxifen (4-OHTam), a metabolite found in the bloodstream, has much higher affinity for the estrogen receptor than tamoxifen itself. hydroxytamoxifen 0-18 estrogen receptor 1 Homo sapiens 102-119 11063868-4 2000 Proliferation, cell-cycle status, and apoptosis of myeloid progenitor 32D cell lines engineered to permit the conditional induction of the constitutively active intracellular domain of mNotch1 (mN1(IC)) by the 4-hydroxytamoxifen(OHT)-inducible system were analyzed in the presence or absence of OHT. hydroxytamoxifen 210-228 notch 1 Mus musculus 185-192 11059777-3 2000 We validated proper expression, specific DNA binding, corepressor interaction, and nuclear localization for the KRAB-PAX3-HBD protein and showed it to be a 4-hydroxytamoxifen-dependent transcriptional repressor of transiently transfected and integrated PAX3 reporters in ARMS cells. hydroxytamoxifen 158-174 paired box 3 Mus musculus 117-121 10966511-6 2000 An antiestrogen, 4-hydroxytamoxifen, significantly inhibited E2-mediated transactivation and interaction between hER alpha and TIF2 through hER alpha binding (p < 0.05). hydroxytamoxifen 17-35 Era like 12S mitochondrial rRNA chaperone 1 Homo sapiens 113-122 10966511-6 2000 An antiestrogen, 4-hydroxytamoxifen, significantly inhibited E2-mediated transactivation and interaction between hER alpha and TIF2 through hER alpha binding (p < 0.05). hydroxytamoxifen 17-35 nuclear receptor coactivator 2 Homo sapiens 127-131 10966511-6 2000 An antiestrogen, 4-hydroxytamoxifen, significantly inhibited E2-mediated transactivation and interaction between hER alpha and TIF2 through hER alpha binding (p < 0.05). hydroxytamoxifen 17-35 Era like 12S mitochondrial rRNA chaperone 1 Homo sapiens 140-149 11075819-0 2000 MEKK1 activation of human estrogen receptor alpha and stimulation of the agonistic activity of 4-hydroxytamoxifen in endometrial and ovarian cancer cells. hydroxytamoxifen 95-113 mitogen-activated protein kinase kinase kinase 1 Homo sapiens 0-5 11075819-8 2000 More importantly, the expression of the constitutively active MEKK1 increased the agonistic activity of 4-hydroxytamoxifen to a level comparable to that of 17beta-estradiol and fully blocked its antagonistic activity. hydroxytamoxifen 104-122 mitogen-activated protein kinase kinase kinase 1 Homo sapiens 62-67 11059777-3 2000 We validated proper expression, specific DNA binding, corepressor interaction, and nuclear localization for the KRAB-PAX3-HBD protein and showed it to be a 4-hydroxytamoxifen-dependent transcriptional repressor of transiently transfected and integrated PAX3 reporters in ARMS cells. hydroxytamoxifen 158-174 paired box 3 Mus musculus 253-257 11059777-6 2000 SCID mice that were engrafted with the KRAB-PAX3-HBD ARMS cell lines and were implanted with 4-hydroxytamoxifen timed-release pellets exhibited suppression of tumor growth and an altered vascularity that was not observed in the control mice. hydroxytamoxifen 93-111 paired box 3 Mus musculus 44-48 10861205-5 2000 The PKB activity of this recombinant protein was rapidly activated in hepatocytes challenged with 4-hydroxytamoxifen (OHT), as was endogenous PKB in hepatocytes challenged with insulin. hydroxytamoxifen 98-116 protein tyrosine kinase 2 beta Homo sapiens 4-7 10937835-4 2000 This method measures the ability of various estrogenic compounds to compete with a known estrogen-receptor-mediated antihormonal drug, 4-hydroxytamoxifen, using the 1-[4,5-dimethylthiazol-2-yl]-3,5-diphenylformazan (MTT) assay to assess mitochondrial activity. hydroxytamoxifen 135-153 estrogen receptor 1 Homo sapiens 89-106 10937835-5 2000 Because 4-hydroxytamoxifen treatment of cells results in a dramatic decrease in mitochondrial dehydrogenase activity which is directly related to their estrogen-receptor content, inhibition of this effect with estrogenic compounds represents an estrogen-receptor interaction, or estrogenic rescue. hydroxytamoxifen 8-26 estrogen receptor 1 Homo sapiens 152-169 10937835-5 2000 Because 4-hydroxytamoxifen treatment of cells results in a dramatic decrease in mitochondrial dehydrogenase activity which is directly related to their estrogen-receptor content, inhibition of this effect with estrogenic compounds represents an estrogen-receptor interaction, or estrogenic rescue. hydroxytamoxifen 8-26 estrogen receptor 1 Homo sapiens 245-262 10788561-7 2000 From the maximal level, GFP expression plateaued, and then declined when E2 was increased to the highest concentration tested, 10(-7) M. 4-Hydroxytamoxifen (TFN-OH) treatment of cells produced a dose-dependent inhibition of E2-induced GFP expression, indicating the interaction of ER in the regulation of GFP gene expression. hydroxytamoxifen 137-155 estrogen receptor 1 Homo sapiens 281-283 10725863-6 2000 Abrogation of the mifepristone- and 4-hydroxytamoxifen-induced cytotoxicity by TGFbeta(1)-neutralizing antibody and by the addition of mannose-6-phosphate confirmed the correlation between induction of active TGFbeta(1) and subsequent prostate cancer cell death. hydroxytamoxifen 36-54 transforming growth factor beta 1 Homo sapiens 79-89 10770489-5 2000 Addition of E2, 4-hydroxytamoxifen, or ICI 182,780 causes ERalpha to partition with the NM-bound fraction on a similar time course (10-20 min) as the spatial reorganization suggesting that the two events are related. hydroxytamoxifen 16-34 estrogen receptor 1 Homo sapiens 58-65 10725863-6 2000 Abrogation of the mifepristone- and 4-hydroxytamoxifen-induced cytotoxicity by TGFbeta(1)-neutralizing antibody and by the addition of mannose-6-phosphate confirmed the correlation between induction of active TGFbeta(1) and subsequent prostate cancer cell death. hydroxytamoxifen 36-54 transforming growth factor beta 1 Homo sapiens 209-219 10649967-17 2000 However, in the presence of tyrosinase and GSH, 4-hydroxytamoxifen was primarily converted to o-quinone GSH conjugates. hydroxytamoxifen 48-66 tyrosinase Homo sapiens 28-38 10810385-7 2000 The stimulation of NES1 by estradiol can be dramatically blocked by the estrogen antagonists ICI 182,780 and 4-hydroxytamoxifen. hydroxytamoxifen 109-127 kallikrein related peptidase 10 Homo sapiens 19-23 10617642-0 2000 Activation of the p38 mitogen-activated protein kinase pathway by estrogen or by 4-hydroxytamoxifen is coupled to estrogen receptor-induced apoptosis. hydroxytamoxifen 81-99 mitogen-activated protein kinase 14 Homo sapiens 18-21 10617642-0 2000 Activation of the p38 mitogen-activated protein kinase pathway by estrogen or by 4-hydroxytamoxifen is coupled to estrogen receptor-induced apoptosis. hydroxytamoxifen 81-99 estrogen receptor 1 Homo sapiens 114-131 10617642-1 2000 17beta-Estradiol (E(2)) or the antiestrogen, 4-hydroxytamoxifen (OHT), induce apoptosis in stably transfected estrogen receptor (ER)-positive HeLa-ER5 cells. hydroxytamoxifen 45-63 estrogen receptor 1 Homo sapiens 110-127 10617642-1 2000 17beta-Estradiol (E(2)) or the antiestrogen, 4-hydroxytamoxifen (OHT), induce apoptosis in stably transfected estrogen receptor (ER)-positive HeLa-ER5 cells. hydroxytamoxifen 45-63 estrogen receptor 1 Homo sapiens 129-131 10619353-3 1999 COUP-TF binding to half-site estrogen response elements (EREs) was increased by the addition of estradiol (E2) -liganded ER (E2-ER), but not by ER liganded with the antiestrogens 4-hydroxytamoxifen (4-OHT-ER) or tamoxifen aziridine (TAz-ER). hydroxytamoxifen 179-197 estrogen receptor 1 Homo sapiens 57-59 10556809-4 1999 Activation of an inducible PKCtheta AE-estrogen receptor fusion mutant led to a CaN-dependent and rapid FasL reporter activity detected as early as 4 h after addition of 4-hydroxytamoxifen, incidating a direct effect of PKCtheta action on FasL expression. hydroxytamoxifen 170-188 Fas ligand Homo sapiens 104-108 10704907-4 1999 On both cell lines the IGF-I or heregulin- induced proliferation was enhanced further by 4-OH-TAM. hydroxytamoxifen 89-97 insulin like growth factor 1 Homo sapiens 23-28 10559241-8 1999 Caveolin-1-mediated activation of ERalpha was sensitive to a well known ER antagonist, 4-hydroxytamoxifen. hydroxytamoxifen 87-105 caveolin 1 Homo sapiens 0-10 10559241-8 1999 Caveolin-1-mediated activation of ERalpha was sensitive to a well known ER antagonist, 4-hydroxytamoxifen. hydroxytamoxifen 87-105 estrogen receptor 1 Homo sapiens 34-41 10630357-0 1999 Synergistic effect of paclitaxel and 4-hydroxytamoxifen on estrogen receptor-negative colon cancer and lung cancer cell lines. hydroxytamoxifen 37-55 estrogen receptor 1 Homo sapiens 59-76 10630357-4 1999 Here we reported that paclitaxel and 4-hydroxytamoxifen (4-HT) have a synergistic cytotoxic effect on the ER-negative colon cancer cell line HCT15, which is refractory to paclitaxel alone. hydroxytamoxifen 37-55 estrogen receptor 1 Homo sapiens 106-108 10402064-5 1999 To further delineate whether tamoxifen may be of benefit in altering the course of HCC, we documented the effects of 4-hydroxytamoxifen and 17beta-estradiol on TGF-beta1 mRNA and protein levels and cell proliferation in a human HCC cell line. hydroxytamoxifen 117-135 transforming growth factor beta 1 Homo sapiens 160-169 10428964-7 1999 This construction (STAT3ER) induced expression of junB (one of the targets of STAT3) in ES cells in the presence of the synthetic ligand 4-hydroxytamoxifen (4HT), thereby indicating that STAT3ER is a conditionally active form. hydroxytamoxifen 137-155 jun B proto-oncogene Mus musculus 50-54 10428964-7 1999 This construction (STAT3ER) induced expression of junB (one of the targets of STAT3) in ES cells in the presence of the synthetic ligand 4-hydroxytamoxifen (4HT), thereby indicating that STAT3ER is a conditionally active form. hydroxytamoxifen 137-155 signal transducer and activator of transcription 3 Mus musculus 19-24 10428964-7 1999 This construction (STAT3ER) induced expression of junB (one of the targets of STAT3) in ES cells in the presence of the synthetic ligand 4-hydroxytamoxifen (4HT), thereby indicating that STAT3ER is a conditionally active form. hydroxytamoxifen 137-155 signal transducer and activator of transcription 3 Mus musculus 78-83 10400647-2 1999 In order to selectively turn on the Akt kinase cascade, we expressed a hydroxytamoxifen-regulatable form of Akt (myristoylated Akt1 estrogen receptor chimera (MER-Akt1)) in the Hepa1c1c7 cells; we verified that hydroxytamoxifen stimulates MER-Akt1 activity to a similar extent as the activation of endogenous Akt by insulin. hydroxytamoxifen 71-87 thymoma viral proto-oncogene 1 Mus musculus 108-111 10400647-2 1999 In order to selectively turn on the Akt kinase cascade, we expressed a hydroxytamoxifen-regulatable form of Akt (myristoylated Akt1 estrogen receptor chimera (MER-Akt1)) in the Hepa1c1c7 cells; we verified that hydroxytamoxifen stimulates MER-Akt1 activity to a similar extent as the activation of endogenous Akt by insulin. hydroxytamoxifen 71-87 thymoma viral proto-oncogene 1 Mus musculus 127-131 10400647-2 1999 In order to selectively turn on the Akt kinase cascade, we expressed a hydroxytamoxifen-regulatable form of Akt (myristoylated Akt1 estrogen receptor chimera (MER-Akt1)) in the Hepa1c1c7 cells; we verified that hydroxytamoxifen stimulates MER-Akt1 activity to a similar extent as the activation of endogenous Akt by insulin. hydroxytamoxifen 71-87 thymoma viral proto-oncogene 1 Mus musculus 163-167 10400647-2 1999 In order to selectively turn on the Akt kinase cascade, we expressed a hydroxytamoxifen-regulatable form of Akt (myristoylated Akt1 estrogen receptor chimera (MER-Akt1)) in the Hepa1c1c7 cells; we verified that hydroxytamoxifen stimulates MER-Akt1 activity to a similar extent as the activation of endogenous Akt by insulin. hydroxytamoxifen 71-87 thymoma viral proto-oncogene 1 Mus musculus 163-167 10400647-2 1999 In order to selectively turn on the Akt kinase cascade, we expressed a hydroxytamoxifen-regulatable form of Akt (myristoylated Akt1 estrogen receptor chimera (MER-Akt1)) in the Hepa1c1c7 cells; we verified that hydroxytamoxifen stimulates MER-Akt1 activity to a similar extent as the activation of endogenous Akt by insulin. hydroxytamoxifen 71-87 thymoma viral proto-oncogene 1 Mus musculus 108-111 10400647-2 1999 In order to selectively turn on the Akt kinase cascade, we expressed a hydroxytamoxifen-regulatable form of Akt (myristoylated Akt1 estrogen receptor chimera (MER-Akt1)) in the Hepa1c1c7 cells; we verified that hydroxytamoxifen stimulates MER-Akt1 activity to a similar extent as the activation of endogenous Akt by insulin. hydroxytamoxifen 211-227 thymoma viral proto-oncogene 1 Mus musculus 36-39 10400647-2 1999 In order to selectively turn on the Akt kinase cascade, we expressed a hydroxytamoxifen-regulatable form of Akt (myristoylated Akt1 estrogen receptor chimera (MER-Akt1)) in the Hepa1c1c7 cells; we verified that hydroxytamoxifen stimulates MER-Akt1 activity to a similar extent as the activation of endogenous Akt by insulin. hydroxytamoxifen 211-227 thymoma viral proto-oncogene 1 Mus musculus 108-111 10400647-2 1999 In order to selectively turn on the Akt kinase cascade, we expressed a hydroxytamoxifen-regulatable form of Akt (myristoylated Akt1 estrogen receptor chimera (MER-Akt1)) in the Hepa1c1c7 cells; we verified that hydroxytamoxifen stimulates MER-Akt1 activity to a similar extent as the activation of endogenous Akt by insulin. hydroxytamoxifen 211-227 thymoma viral proto-oncogene 1 Mus musculus 108-111 10400647-3 1999 Our studies reveal that stimulation of MER-Akt1 by hydroxytamoxifen induces GLUT1 mRNA and protein accumulation to levels comparable to that induced by insulin; therefore, activation of the Akt cascade suffices to induce GLUT1 gene expression in this cell system. hydroxytamoxifen 51-67 thymoma viral proto-oncogene 1 Mus musculus 43-47 10400647-3 1999 Our studies reveal that stimulation of MER-Akt1 by hydroxytamoxifen induces GLUT1 mRNA and protein accumulation to levels comparable to that induced by insulin; therefore, activation of the Akt cascade suffices to induce GLUT1 gene expression in this cell system. hydroxytamoxifen 51-67 solute carrier family 2 (facilitated glucose transporter), member 1 Mus musculus 76-81 10400647-3 1999 Our studies reveal that stimulation of MER-Akt1 by hydroxytamoxifen induces GLUT1 mRNA and protein accumulation to levels comparable to that induced by insulin; therefore, activation of the Akt cascade suffices to induce GLUT1 gene expression in this cell system. hydroxytamoxifen 51-67 thymoma viral proto-oncogene 1 Mus musculus 43-46 10400647-3 1999 Our studies reveal that stimulation of MER-Akt1 by hydroxytamoxifen induces GLUT1 mRNA and protein accumulation to levels comparable to that induced by insulin; therefore, activation of the Akt cascade suffices to induce GLUT1 gene expression in this cell system. hydroxytamoxifen 51-67 solute carrier family 2 (facilitated glucose transporter), member 1 Mus musculus 221-226 10402064-7 1999 4-Hydroxytamoxifen and 17beta-estradiol decreased TGF-beta1 mRNA and protein levels in a time- and dose-dependent manner. hydroxytamoxifen 0-18 transforming growth factor beta 1 Homo sapiens 50-59 10493022-3 1999 METHODS: Based on the finding that the progression of DNA/RNA polymerases on templates might be blocked by bulky DNA adducts, we successfully developed and used a polymerase stop assay to map the sites of adduct formation in the target lacI gene following its reaction in vitro with alpha-acetoxytamoxifen and horseradish peroxidase/H2O2 (HRP/H2O2) activated 4-hydroxytamoxifen. hydroxytamoxifen 359-377 tissue factor pathway inhibitor Rattus norvegicus 236-240 10493022-4 1999 RESULTS: Using a T4 DNA polymerase stop assay, adduct formation in the lacI gene of the plasmid constructs, after the reaction in vitro with alpha-acetoxytamoxifen and HRP/H2O2 activated 4-hydroxytamoxifen, was found to mainly occur with guanines. hydroxytamoxifen 187-205 tissue factor pathway inhibitor Homo sapiens 71-75 10022879-5 1999 We first demonstrated that the individual activation function 1 (AF-1) domains act in a dominant manner within the ERalpha-ERbeta heterodimer: the mixed agonist-antagonist 4-hydroxytamoxifen acts as an agonist in a promoter- and cell context-dependent manner via the ERalpha AF-1, while activation of the complex by the mitogen-activated protein kinase (MAPK) pathway requires only the ERalpha- or ERbeta-responsive MAPK site. hydroxytamoxifen 172-190 estrogen receptor 1 Homo sapiens 115-122 10402064-8 1999 TGF-beta1 significantly inhibited PLC/PRF/5 cell proliferation, whereas both 4-hydroxytamoxifen and 17beta-estradiol stimulated PLC/PRF/5 cell proliferation. hydroxytamoxifen 77-95 heparan sulfate proteoglycan 2 Homo sapiens 128-131 10402064-9 1999 The stimulatory effects of 4-hydroxytamoxifen on PLC/PRF/5 cell proliferation raise concerns regarding its use in the treatment of HCC in human patients and suggest that 4-hydroxytamoxifen may have no beneficial effects in some patients with HCC. hydroxytamoxifen 27-45 heparan sulfate proteoglycan 2 Homo sapiens 49-52 10066447-5 1999 Maximal stimulation of PCDGF mRNA and protein expression by 17-beta-estradiol was observed at a concentration of 10(-8) M. The stimulation of PCDGF expression by 17-beta-estradiol was completely inhibited by treatment with actinomycin D and with the antiestrogen 4-hydroxytamoxifen. hydroxytamoxifen 263-281 granulin precursor Homo sapiens 23-28 10066447-5 1999 Maximal stimulation of PCDGF mRNA and protein expression by 17-beta-estradiol was observed at a concentration of 10(-8) M. The stimulation of PCDGF expression by 17-beta-estradiol was completely inhibited by treatment with actinomycin D and with the antiestrogen 4-hydroxytamoxifen. hydroxytamoxifen 263-281 granulin precursor Homo sapiens 142-147 10400647-2 1999 In order to selectively turn on the Akt kinase cascade, we expressed a hydroxytamoxifen-regulatable form of Akt (myristoylated Akt1 estrogen receptor chimera (MER-Akt1)) in the Hepa1c1c7 cells; we verified that hydroxytamoxifen stimulates MER-Akt1 activity to a similar extent as the activation of endogenous Akt by insulin. hydroxytamoxifen 71-87 thymoma viral proto-oncogene 1 Mus musculus 36-39 10076999-5 1999 While hERbeta did not confer estrogen responsiveness on this promoter, it did elicit transcriptional activation in the presence of 4-hydroxytamoxifen (4-OH-Tam). hydroxytamoxifen 131-149 estrogen receptor 2 Homo sapiens 6-13 10076999-5 1999 While hERbeta did not confer estrogen responsiveness on this promoter, it did elicit transcriptional activation in the presence of 4-hydroxytamoxifen (4-OH-Tam). hydroxytamoxifen 151-159 estrogen receptor 2 Homo sapiens 6-13 10022879-5 1999 We first demonstrated that the individual activation function 1 (AF-1) domains act in a dominant manner within the ERalpha-ERbeta heterodimer: the mixed agonist-antagonist 4-hydroxytamoxifen acts as an agonist in a promoter- and cell context-dependent manner via the ERalpha AF-1, while activation of the complex by the mitogen-activated protein kinase (MAPK) pathway requires only the ERalpha- or ERbeta-responsive MAPK site. hydroxytamoxifen 172-190 estrogen receptor 2 Homo sapiens 123-129 10022879-5 1999 We first demonstrated that the individual activation function 1 (AF-1) domains act in a dominant manner within the ERalpha-ERbeta heterodimer: the mixed agonist-antagonist 4-hydroxytamoxifen acts as an agonist in a promoter- and cell context-dependent manner via the ERalpha AF-1, while activation of the complex by the mitogen-activated protein kinase (MAPK) pathway requires only the ERalpha- or ERbeta-responsive MAPK site. hydroxytamoxifen 172-190 estrogen receptor 1 Homo sapiens 267-274 10022879-5 1999 We first demonstrated that the individual activation function 1 (AF-1) domains act in a dominant manner within the ERalpha-ERbeta heterodimer: the mixed agonist-antagonist 4-hydroxytamoxifen acts as an agonist in a promoter- and cell context-dependent manner via the ERalpha AF-1, while activation of the complex by the mitogen-activated protein kinase (MAPK) pathway requires only the ERalpha- or ERbeta-responsive MAPK site. hydroxytamoxifen 172-190 estrogen receptor 1 Homo sapiens 267-274 10022879-5 1999 We first demonstrated that the individual activation function 1 (AF-1) domains act in a dominant manner within the ERalpha-ERbeta heterodimer: the mixed agonist-antagonist 4-hydroxytamoxifen acts as an agonist in a promoter- and cell context-dependent manner via the ERalpha AF-1, while activation of the complex by the mitogen-activated protein kinase (MAPK) pathway requires only the ERalpha- or ERbeta-responsive MAPK site. hydroxytamoxifen 172-190 estrogen receptor 2 Homo sapiens 398-404 9990040-2 1999 We explored an inducible system in which Smad4 protein is activated by translocation to the nucleus when cell lines that stably express wild-type or mutant Smad4 proteins fused to a murine estrogen receptor domain are treated with 4-hydroxytamoxifen. hydroxytamoxifen 231-249 SMAD family member 4 Mus musculus 41-46 10076999-10 1999 Through the use of mutant and chimeric receptors, it was shown that the 4-OH-Tam activity via ERbeta from the hRARalpha-1 promoter in Hep G2 cells required the amino-terminal region of ERbeta, a region that was not necessary for estrogen-induced ERbeta activity from an ERE in Hep G2 cells. hydroxytamoxifen 72-80 estrogen receptor 2 Homo sapiens 94-100 10076999-10 1999 Through the use of mutant and chimeric receptors, it was shown that the 4-OH-Tam activity via ERbeta from the hRARalpha-1 promoter in Hep G2 cells required the amino-terminal region of ERbeta, a region that was not necessary for estrogen-induced ERbeta activity from an ERE in Hep G2 cells. hydroxytamoxifen 72-80 estrogen receptor 2 Homo sapiens 185-191 10076999-10 1999 Through the use of mutant and chimeric receptors, it was shown that the 4-OH-Tam activity via ERbeta from the hRARalpha-1 promoter in Hep G2 cells required the amino-terminal region of ERbeta, a region that was not necessary for estrogen-induced ERbeta activity from an ERE in Hep G2 cells. hydroxytamoxifen 72-80 estrogen receptor 2 Homo sapiens 185-191 9990040-2 1999 We explored an inducible system in which Smad4 protein is activated by translocation to the nucleus when cell lines that stably express wild-type or mutant Smad4 proteins fused to a murine estrogen receptor domain are treated with 4-hydroxytamoxifen. hydroxytamoxifen 231-249 SMAD family member 4 Mus musculus 156-161 9920887-5 1999 Estrogen receptor antagonists 4-hydroxytamoxifen and 7alpha-[9-(4,4, 5,5,5-pentafluoro-pentylsulfinyl)nonyl]estra-1,3,5(10)-tr iene3, 17beta-diol restored TCDD-induced CYP1A1 transcription, steady-state mRNA levels, and enzymatic activity in ECC-1 cells. hydroxytamoxifen 30-48 estrogen receptor 1 Homo sapiens 0-17 9875847-3 1998 Here we report the crystal structure of the human estrogen receptor alpha (hER alpha) ligand-binding domain (LBD) bound to both the agonist diethylstilbestrol (DES) and a peptide derived from the NR box II region of the coactivator GRIP1 and the crystal structure of the hER alpha LBD bound to the selective antagonist 4-hydroxytamoxifen (OHT). hydroxytamoxifen 319-337 estrogen receptor 1 Homo sapiens 50-73 9892606-5 1999 In parallel, TGF-beta1 inhibited c-Myc expression in T cell hybridomas, and ectopic expression of a chimeric molecule composed of c-Myc and the steroid binding domain of the estrogen receptor (Myc-ER) blocked both the inhibition of FasL and the decrease of AICD induced by TGF-beta1, providing that 4-hydroxytamoxifen was present. hydroxytamoxifen 299-317 estrogen receptor 1 Homo sapiens 174-191 9914518-7 1999 Moreover, this enhancement of transcriptional activation by COUP-TFI requires specifically the AF-1 transactivation function of ER and can be observed in the presence of E2 or 4-hydroxytamoxifen but not ICI 164384. hydroxytamoxifen 176-194 nuclear receptor subfamily 2 group F member 1 Gallus gallus 60-68 9875216-1 1998 In this study we demonstrate that physiologic concentrations of genistein are sufficient to mediate agonism and to reverse the repressive effects of 4-hydroxytamoxifen on estrogen receptor (ER alpha)-responsive reporter genes. hydroxytamoxifen 149-167 estrogen receptor 1 Homo sapiens 190-198 9833770-3 1998 We confirmed reports of ER disappearance in the presence of estrogens (Es; E2 and DES) and pure anti-estrogens (AEs; RU 58,668 and ICI 164,384) as well as its increase with partial AEs (4-OH-TAM and RU 39,119). hydroxytamoxifen 186-194 estrogen receptor 1 Homo sapiens 24-26 9875216-5 1998 More importantly, coincubation with genistein and 4-hydroxytamoxifen or genistein treatment following preincubation of the ER with 4-hydroxytamoxifen also resulted in a strong physical interaction with SRC-1. hydroxytamoxifen 50-68 nuclear receptor coactivator 1 Homo sapiens 202-207 9875216-5 1998 More importantly, coincubation with genistein and 4-hydroxytamoxifen or genistein treatment following preincubation of the ER with 4-hydroxytamoxifen also resulted in a strong physical interaction with SRC-1. hydroxytamoxifen 131-149 nuclear receptor coactivator 1 Homo sapiens 202-207 9778038-1 1998 Activation of high ectopic levels of c-Myc in serum-deprived Rat1-MycER cells by 4-hydroxytamoxifen induces both proliferation and apoptosis. hydroxytamoxifen 81-99 MYC proto-oncogene, bHLH transcription factor Rattus norvegicus 37-42 9879983-4 1998 The estradiol-induced effect was blocked by 100 nM of the estrogen receptor antagonist 4-hydroxytamoxifen, indicating dephosphorylation of FAK is an estrogen receptor-mediated event. hydroxytamoxifen 87-105 protein tyrosine kinase 2 Homo sapiens 139-142 9790998-3 1998 Therefore, the effect of 17beta-estradiol (E2), tamoxifen, or its more potent metabolite, 4-hydroxytamoxifen (OH-tamoxifen), on PTHrP expression in an estrogen receptor (ER)-positive breast carcinoma cell line (MCF-7) was evaluated. hydroxytamoxifen 90-108 parathyroid hormone like hormone Homo sapiens 128-133 9790998-3 1998 Therefore, the effect of 17beta-estradiol (E2), tamoxifen, or its more potent metabolite, 4-hydroxytamoxifen (OH-tamoxifen), on PTHrP expression in an estrogen receptor (ER)-positive breast carcinoma cell line (MCF-7) was evaluated. hydroxytamoxifen 90-108 estrogen receptor 1 Homo sapiens 151-168 9790998-3 1998 Therefore, the effect of 17beta-estradiol (E2), tamoxifen, or its more potent metabolite, 4-hydroxytamoxifen (OH-tamoxifen), on PTHrP expression in an estrogen receptor (ER)-positive breast carcinoma cell line (MCF-7) was evaluated. hydroxytamoxifen 90-108 estrogen receptor 1 Homo sapiens 170-172 9879777-4 1998 Abrogation of the mifepristone- and/or 4-hydroxytamoxifen-induced cytotoxicity by TGFbeta1 neutralizing antibody confirms the correlation between induction of active TGFbeta1 and subsequent cell death. hydroxytamoxifen 39-57 latent transforming growth factor beta binding protein 1 Homo sapiens 82-90 9879777-4 1998 Abrogation of the mifepristone- and/or 4-hydroxytamoxifen-induced cytotoxicity by TGFbeta1 neutralizing antibody confirms the correlation between induction of active TGFbeta1 and subsequent cell death. hydroxytamoxifen 39-57 latent transforming growth factor beta binding protein 1 Homo sapiens 166-174 9879777-5 1998 The effect of a combination of mifepristone and 4-hydroxytamoxifen on cell growth inhibition, on the increase in DNA fragmentation, bcl2 downregulation, and induction of TGFbeta1 protein was additive and significantly different (P < 0.05) from the effect of monotherapy. hydroxytamoxifen 48-66 BCL2 apoptosis regulator Homo sapiens 132-136 9879777-5 1998 The effect of a combination of mifepristone and 4-hydroxytamoxifen on cell growth inhibition, on the increase in DNA fragmentation, bcl2 downregulation, and induction of TGFbeta1 protein was additive and significantly different (P < 0.05) from the effect of monotherapy. hydroxytamoxifen 48-66 latent transforming growth factor beta binding protein 1 Homo sapiens 170-178 9581811-2 1998 To address this issue, the survival of Rat-1 fibroblasts containing a 4-hydroxytamoxifen-regulated c-Myc allele, c-MycER (T. D. Littlewood et al., Nucleic Acids Res., 23: 1686-1690, 1995), after single and fractionated doses of radiation was investigated. hydroxytamoxifen 70-88 MYC proto-oncogene, bHLH transcription factor Rattus norvegicus 99-104 9667651-0 1998 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. hydroxytamoxifen 29-47 tumor necrosis factor Homo sapiens 64-96 9667651-4 1998 We now report that 4-hydroxytamoxifen (4-OHT) shows oestrogen-like effects on the induction of TGF-alpha gene expression in our transfectants. hydroxytamoxifen 19-37 transforming growth factor alpha Homo sapiens 95-104 9565622-3 1998 In the present study, a conditionally active version of Akt was constructed by fusing the Akt containing the myristoylation sequence to the hormone binding domain of a mutant murine estrogen receptor that selectively binds 4-hydroxytamoxifen. hydroxytamoxifen 223-241 thymoma viral proto-oncogene 1 Mus musculus 56-59 9806352-3 1998 When ER is bound by 4-hydroxytamoxifen (4-OHT), the active metabolite of the widely used therapeutic antiestrogen tamoxifen (TAM), the receptor binds to EREs with high affinity. hydroxytamoxifen 20-38 estrogen receptor 1 Homo sapiens 5-7 9686563-4 1998 Activation of STAT6:ER* by 4-hydroxytamoxifen leads to specific activation of STAT6-regulated gene expression including the activation of a STAT6 reporter construct and induction of CD23 in B cell lines. hydroxytamoxifen 27-45 signal transducer and activator of transcription 6 Homo sapiens 14-19 9686563-4 1998 Activation of STAT6:ER* by 4-hydroxytamoxifen leads to specific activation of STAT6-regulated gene expression including the activation of a STAT6 reporter construct and induction of CD23 in B cell lines. hydroxytamoxifen 27-45 signal transducer and activator of transcription 6 Homo sapiens 78-83 9686563-4 1998 Activation of STAT6:ER* by 4-hydroxytamoxifen leads to specific activation of STAT6-regulated gene expression including the activation of a STAT6 reporter construct and induction of CD23 in B cell lines. hydroxytamoxifen 27-45 signal transducer and activator of transcription 6 Homo sapiens 78-83 9686563-4 1998 Activation of STAT6:ER* by 4-hydroxytamoxifen leads to specific activation of STAT6-regulated gene expression including the activation of a STAT6 reporter construct and induction of CD23 in B cell lines. hydroxytamoxifen 27-45 Fc epsilon receptor II Homo sapiens 182-186 9764805-4 1998 We report that agents which reduced cell attachment to plastic and invasion through fibronectin in vitro (tamoxifen, N-desmethyltamoxifen and 17beta-oestradiol) caused increases in levels of F-actin and vimentin, whereas agents which did not affect attachment or invasion (4-hydroxytamoxifen and dihydrotestosterone) had little or no effect on the cytoskeletal proteins. hydroxytamoxifen 273-291 fibronectin 1 Homo sapiens 84-95 9764805-4 1998 We report that agents which reduced cell attachment to plastic and invasion through fibronectin in vitro (tamoxifen, N-desmethyltamoxifen and 17beta-oestradiol) caused increases in levels of F-actin and vimentin, whereas agents which did not affect attachment or invasion (4-hydroxytamoxifen and dihydrotestosterone) had little or no effect on the cytoskeletal proteins. hydroxytamoxifen 273-291 vimentin Homo sapiens 203-211 9738981-4 1998 The ligand-binding domain of MfasER was replaced with that of a mutant estrogen receptor which is unable to bind estrogen yet retains affinity for a synthetic ligand, 4-hydroxytamoxifen (Tm). hydroxytamoxifen 167-185 estrogen receptor 1 (alpha) Mus musculus 71-88 9636226-11 1998 Activating PKB with 4-hydroxytamoxifen mimicked insulin by decreasing mTOR reactivity with mTAb1 and by increasing the PHAS-I kinase activity of mTOR. hydroxytamoxifen 20-38 insulin Homo sapiens 48-55 9636226-11 1998 Activating PKB with 4-hydroxytamoxifen mimicked insulin by decreasing mTOR reactivity with mTAb1 and by increasing the PHAS-I kinase activity of mTOR. hydroxytamoxifen 20-38 mechanistic target of rapamycin kinase Homo sapiens 70-74 9636226-11 1998 Activating PKB with 4-hydroxytamoxifen mimicked insulin by decreasing mTOR reactivity with mTAb1 and by increasing the PHAS-I kinase activity of mTOR. hydroxytamoxifen 20-38 TGF-beta activated kinase 1/MAP3K7 binding protein 1 Mus musculus 91-96 9636226-11 1998 Activating PKB with 4-hydroxytamoxifen mimicked insulin by decreasing mTOR reactivity with mTAb1 and by increasing the PHAS-I kinase activity of mTOR. hydroxytamoxifen 20-38 eukaryotic translation initiation factor 4E binding protein 1 Homo sapiens 119-125 9636226-11 1998 Activating PKB with 4-hydroxytamoxifen mimicked insulin by decreasing mTOR reactivity with mTAb1 and by increasing the PHAS-I kinase activity of mTOR. hydroxytamoxifen 20-38 mechanistic target of rapamycin kinase Homo sapiens 145-149 9563474-1 1998 The selection of NIH 3T3 cells expressing a hydroxytamoxifen-inducible c-Raf-1-estrogen receptor fusion protein (c-Raf-1-BxB-ER) in the absence or presence of the inducer results in dramatic differences in the expression levels of the fusion protein. hydroxytamoxifen 44-60 v-raf-leukemia viral oncogene 1 Mus musculus 71-76 9563474-1 1998 The selection of NIH 3T3 cells expressing a hydroxytamoxifen-inducible c-Raf-1-estrogen receptor fusion protein (c-Raf-1-BxB-ER) in the absence or presence of the inducer results in dramatic differences in the expression levels of the fusion protein. hydroxytamoxifen 44-60 v-raf-leukemia viral oncogene 1 Mus musculus 113-118 9563474-2 1998 Hydroxytamoxifen-mediated constitutive activation of the Raf signal favors the selection of cells expressing low levels of c-Raf-1-BxB-ER. hydroxytamoxifen 0-16 zinc fingers and homeoboxes 2 Mus musculus 57-60 9563474-2 1998 Hydroxytamoxifen-mediated constitutive activation of the Raf signal favors the selection of cells expressing low levels of c-Raf-1-BxB-ER. hydroxytamoxifen 0-16 v-raf-leukemia viral oncogene 1 Mus musculus 123-128 9563474-3 1998 Cells selected in the absence of hydroxytamoxifen express up to 20 times higher levels of the inducible Raf kinase. hydroxytamoxifen 33-49 zinc fingers and homeoboxes 2 Mus musculus 104-107 9584839-5 1998 4-Hydroxytamoxifen and the pure anti-estrogen ICI 164,384 reduced receptor transcriptional activity in the presence of PKC delta. hydroxytamoxifen 0-18 protein kinase C, delta Mus musculus 119-128 9544987-7 1998 In the presence of unliganded thyroid hormone receptor (TR) or ER complexed with the antiestrogen 4-hydroxytamoxifen, which presumably sequesters a limiting pool of the inhibitory cofactor, RU486-PR-B functions as a transcriptional activator of a progesterone-responsive gene even in the absence of hormone agonist. hydroxytamoxifen 98-116 estrogen receptor 1 Homo sapiens 63-65 9566718-1 1998 We have shown that 4-hydroxytamoxifen (4-OHT) has estrogen-like effects on induction of TGFalpha mRNA in estrogen receptor (ER)-negative MDA-MB-231 human breast cancer cells, transfected with either wildtype (S30 cells) or a codon 351asp-->tyr mutant ER (BC-2 cells). hydroxytamoxifen 19-37 transforming growth factor alpha Homo sapiens 88-96 9566718-1 1998 We have shown that 4-hydroxytamoxifen (4-OHT) has estrogen-like effects on induction of TGFalpha mRNA in estrogen receptor (ER)-negative MDA-MB-231 human breast cancer cells, transfected with either wildtype (S30 cells) or a codon 351asp-->tyr mutant ER (BC-2 cells). hydroxytamoxifen 19-37 estrogen receptor 1 Homo sapiens 105-122 9566718-1 1998 We have shown that 4-hydroxytamoxifen (4-OHT) has estrogen-like effects on induction of TGFalpha mRNA in estrogen receptor (ER)-negative MDA-MB-231 human breast cancer cells, transfected with either wildtype (S30 cells) or a codon 351asp-->tyr mutant ER (BC-2 cells). hydroxytamoxifen 19-37 estrogen receptor 1 Homo sapiens 124-126 9605415-3 1998 As measured by competition studies, the affinity of EM-652, the active metabolite of the prodrug EM-800, for the estrogen receptor is 7-11 times higher than that of 17beta-estradiol (E2), ICI 182780, and hydroxy-tamoxifen (OH-TAM), the active metabolite of Tamoxifen. hydroxytamoxifen 204-221 estrogen receptor 1 Rattus norvegicus 113-130 9271411-2 1997 We show that ectopic expression of cyclin D1 can stimulate the transcriptional activity of the estrogen receptor in the absence of estradiol and that this activity can be inhibited by 4-hydroxytamoxifen and ICI 182,780. hydroxytamoxifen 184-202 cyclin D1 Homo sapiens 35-44 9405735-8 1998 Interestingly, 4-hydroxytamoxifen (10(-7) M), a documented pure antiestrogen in reproductive tissues, also increased IGF-I mRNA to levels similar to those observed in E2-treated cells. hydroxytamoxifen 15-33 insulin like growth factor 1 Homo sapiens 117-122 9395481-8 1997 When ER was liganded by the antiestrogen 4-hydroxytamoxifen (4-OHT), COUP-TF-half-site interaction decreased. hydroxytamoxifen 41-59 estrogen receptor 1 Gallus gallus 5-7 9395481-8 1997 When ER was liganded by the antiestrogen 4-hydroxytamoxifen (4-OHT), COUP-TF-half-site interaction decreased. hydroxytamoxifen 41-59 nuclear receptor subfamily 2 group F member 1 Bos taurus 69-76 9371770-6 1997 Activation of a Myc-estrogen receptor fusion protein by 4-hydroxytamoxifen was sufficient to repress gas1 gene transcription. hydroxytamoxifen 56-74 MYC proto-oncogene, bHLH transcription factor Homo sapiens 16-19 9371770-6 1997 Activation of a Myc-estrogen receptor fusion protein by 4-hydroxytamoxifen was sufficient to repress gas1 gene transcription. hydroxytamoxifen 56-74 growth arrest specific 1 Homo sapiens 101-105 9815609-3 1997 We demonstrate that the antiestrogens 4-hydroxytamoxifen (4-OH tamoxifen) and ICI 182780 (ICI) stimulate MDGI expression in vitro. hydroxytamoxifen 38-56 fatty acid binding protein 3 Homo sapiens 105-109 9815609-3 1997 We demonstrate that the antiestrogens 4-hydroxytamoxifen (4-OH tamoxifen) and ICI 182780 (ICI) stimulate MDGI expression in vitro. hydroxytamoxifen 58-72 fatty acid binding protein 3 Homo sapiens 105-109 9815609-5 1997 Both 4-OH tamoxifen and ICI stabilized MDGI mRNA without affecting the transcription rate of the MDGI gene. hydroxytamoxifen 5-19 fatty acid binding protein 3 Homo sapiens 39-43 9815609-6 1997 Under estrogen-free conditions, the half-life of MDGI mRNA in control explants was approximately 6 h. This half-life was increased to 7.5 h in the presence of 10(-7) M 4-OH tamoxifen and to greater than 12 h in the presence of 10(-7) M ICI. hydroxytamoxifen 168-182 fatty acid binding protein 3 Homo sapiens 49-53 9464539-4 1998 Fusion of the c-Raf-1 kinase domain with the hormone binding domain of the estrogen receptor (c-Raf-1-BxB-ER) provides a 4-hydroxytamoxifen regulated form of the oncogenic c-Raf-1 kinase. hydroxytamoxifen 121-139 v-raf-leukemia viral oncogene 1 Mus musculus 14-19 9464539-4 1998 Fusion of the c-Raf-1 kinase domain with the hormone binding domain of the estrogen receptor (c-Raf-1-BxB-ER) provides a 4-hydroxytamoxifen regulated form of the oncogenic c-Raf-1 kinase. hydroxytamoxifen 121-139 estrogen receptor 1 (alpha) Mus musculus 75-92 9464539-4 1998 Fusion of the c-Raf-1 kinase domain with the hormone binding domain of the estrogen receptor (c-Raf-1-BxB-ER) provides a 4-hydroxytamoxifen regulated form of the oncogenic c-Raf-1 kinase. hydroxytamoxifen 121-139 v-raf-leukemia viral oncogene 1 Mus musculus 94-99 9464539-4 1998 Fusion of the c-Raf-1 kinase domain with the hormone binding domain of the estrogen receptor (c-Raf-1-BxB-ER) provides a 4-hydroxytamoxifen regulated form of the oncogenic c-Raf-1 kinase. hydroxytamoxifen 121-139 v-raf-leukemia viral oncogene 1 Mus musculus 94-99 9464539-6 1998 4-hydroxytamoxifen mediated activation of the fusion protein in serum starved N-BxB-ER induces the expression of the c-myc gene within 2-6 h. Deletion of the c-Raf-1 kinase domain generates a mutant c-Raf-1 protein (c-Raf-1-C4B), which can directly interact with the effector domain of the Ras protein and thereby block Ras mediated signalling. hydroxytamoxifen 0-18 v-raf-leukemia viral oncogene 1 Mus musculus 158-163 9464539-6 1998 4-hydroxytamoxifen mediated activation of the fusion protein in serum starved N-BxB-ER induces the expression of the c-myc gene within 2-6 h. Deletion of the c-Raf-1 kinase domain generates a mutant c-Raf-1 protein (c-Raf-1-C4B), which can directly interact with the effector domain of the Ras protein and thereby block Ras mediated signalling. hydroxytamoxifen 0-18 v-raf-leukemia viral oncogene 1 Mus musculus 199-204 9464539-6 1998 4-hydroxytamoxifen mediated activation of the fusion protein in serum starved N-BxB-ER induces the expression of the c-myc gene within 2-6 h. Deletion of the c-Raf-1 kinase domain generates a mutant c-Raf-1 protein (c-Raf-1-C4B), which can directly interact with the effector domain of the Ras protein and thereby block Ras mediated signalling. hydroxytamoxifen 0-18 v-raf-leukemia viral oncogene 1 Mus musculus 199-204 9366526-6 1997 When compared with controls, both clonal and polyclonal populations of FGF-1 overexpressing cells exhibited increased anchorage-independent growth and decreased population doubling times in estrogen-depleted or 4-hydroxytamoxifen containing medium. hydroxytamoxifen 211-229 fibroblast growth factor 1 Mus musculus 71-76 9010347-5 1996 Interestingly, the binding of ER liganded with the antiestrogen 4-hydroxytamoxifen (4-OHT-ER) was non-cooperative with an apparent stoichiometry of 0.5 4-OHT-ER dimer per ERE, regardless of ER purity or ERE flanking sequence. hydroxytamoxifen 64-82 estrogen receptor 1 Bos taurus 30-32 9205071-11 1997 RXR compounds also potentiated the action of the antiestrogen 4-hydroxytamoxifen to inhibit the growth of T-47D cells. hydroxytamoxifen 62-80 retinoid X receptor alpha Homo sapiens 0-3 9207217-7 1997 4-Hydroxy tamoxifen had anti-estrogenic activity only in yeast lacking the transporter Pdr5. hydroxytamoxifen 0-19 ATP-binding cassette multidrug transporter PDR5 Saccharomyces cerevisiae S288C 87-91 9207217-8 1997 Whole cell binding assays indicated that 4-hydroxy tamoxifen is exported by Pdr5. hydroxytamoxifen 41-60 ATP-binding cassette multidrug transporter PDR5 Saccharomyces cerevisiae S288C 76-80 8982077-4 1996 Co-transfection experiments in NIH 3T3 fibroblasts showed that the resulting chimeric protein, Myb/En/ER, repressed transactivation of a c-Myb-responsive reporter only in the presence of the synthetic steroid, 4-hydroxytamoxifen (OHT). hydroxytamoxifen 210-228 myeloblastosis oncogene Mus musculus 95-98 8982077-4 1996 Co-transfection experiments in NIH 3T3 fibroblasts showed that the resulting chimeric protein, Myb/En/ER, repressed transactivation of a c-Myb-responsive reporter only in the presence of the synthetic steroid, 4-hydroxytamoxifen (OHT). hydroxytamoxifen 210-228 myeloblastosis oncogene Mus musculus 137-142 9178906-8 1997 When a chimeric protein comprised of c-myc and the estrogen binding domain of estrogen receptor was activated by addition of 4-hydroxytamoxifen (OHT), expression of RCC1 mRNA increased twofold. hydroxytamoxifen 125-143 MYC proto-oncogene, bHLH transcription factor Homo sapiens 37-42 9178906-8 1997 When a chimeric protein comprised of c-myc and the estrogen binding domain of estrogen receptor was activated by addition of 4-hydroxytamoxifen (OHT), expression of RCC1 mRNA increased twofold. hydroxytamoxifen 125-143 estrogen receptor 1 Homo sapiens 78-95 9178906-8 1997 When a chimeric protein comprised of c-myc and the estrogen binding domain of estrogen receptor was activated by addition of 4-hydroxytamoxifen (OHT), expression of RCC1 mRNA increased twofold. hydroxytamoxifen 125-143 regulator of chromosome condensation 1 Homo sapiens 165-169 9010347-5 1996 Interestingly, the binding of ER liganded with the antiestrogen 4-hydroxytamoxifen (4-OHT-ER) was non-cooperative with an apparent stoichiometry of 0.5 4-OHT-ER dimer per ERE, regardless of ER purity or ERE flanking sequence. hydroxytamoxifen 64-82 estrogen receptor 1 Bos taurus 90-92 9010347-5 1996 Interestingly, the binding of ER liganded with the antiestrogen 4-hydroxytamoxifen (4-OHT-ER) was non-cooperative with an apparent stoichiometry of 0.5 4-OHT-ER dimer per ERE, regardless of ER purity or ERE flanking sequence. hydroxytamoxifen 64-82 estrogen receptor 1 Bos taurus 90-92 9010347-5 1996 Interestingly, the binding of ER liganded with the antiestrogen 4-hydroxytamoxifen (4-OHT-ER) was non-cooperative with an apparent stoichiometry of 0.5 4-OHT-ER dimer per ERE, regardless of ER purity or ERE flanking sequence. hydroxytamoxifen 64-82 estrogen receptor 1 Bos taurus 90-92 8752163-7 1996 The antiestrogens tamoxifen, 4-OH tamoxifen, and nafoxidine produce similar increases in uterine VEGF mRNA levels within 6 h, with 1 mg/kg tamoxifen producing a maximum response of 15-20-fold. hydroxytamoxifen 29-43 vascular endothelial growth factor A Rattus norvegicus 97-101 8800639-3 1995 Antiestrogens, 4-hydroxytamoxifen and ICI 164,384, prevented the effects of the xenobiotics, indicating that the induction of gene expression is mediated by the ER. hydroxytamoxifen 15-33 estrogen receptor Oncorhynchus mykiss 161-163 22358926-4 1996 We have developed a "switchable" chimaeric c-Myc protein whose activity is dependent on the synthetic ligand, 4-hydroxytamoxifen. hydroxytamoxifen 110-128 MYC proto-oncogene, bHLH transcription factor Homo sapiens 43-48 22358926-5 1996 In cells expressing this switchable c-Myc, proliferation and apoptosis in cultured fibroblasts can be regulated by addition of 4-hydroxytamoxifen. hydroxytamoxifen 127-145 MYC proto-oncogene, bHLH transcription factor Homo sapiens 36-41 8761295-2 1996 The protein product of this gene, p53ERTM, is expressed in cells constitutively but is not functional unless associated with tamoxifen or 4-hydroxytamoxifen. hydroxytamoxifen 138-156 transformation related protein 53, pseudogene Mus musculus 34-37 8761295-4 1996 Activation of p53 in these transformed cells by the addition of tamoxifen or 4-hydroxytamoxifen resulted in apoptosis. hydroxytamoxifen 77-95 transformation related protein 53, pseudogene Mus musculus 14-17 8625307-5 1996 In both these cell lines, the nonsteroidal antiestrogen 4-hydroxytamoxifen has little effect on the mRNA level but causes a net accumulation of the ER protein over time. hydroxytamoxifen 56-74 estrogen receptor 1 Homo sapiens 148-150 8738832-0 1996 Site-directed estrogen receptor antibodies stabilize 4-hydroxytamoxifen ligand, but not estradiol, and indicate ligand-specific differences in the recognition of estrogen response element DNA in vitro. hydroxytamoxifen 53-71 estrogen receptor 1 Homo sapiens 14-31 8738832-3 1996 Although 4-hydroxytamoxifen-liganded-ER (4-OHT-ER) and E2-ER bind a consensus ERE with equal high affinity, the stoichiometry of 4-OHT-ER-ERE binding at saturation is approximately 50% lower than that of E2-ER binding to all ERE sequences tested. hydroxytamoxifen 9-27 estrogen receptor 1 Homo sapiens 37-39 8738832-3 1996 Although 4-hydroxytamoxifen-liganded-ER (4-OHT-ER) and E2-ER bind a consensus ERE with equal high affinity, the stoichiometry of 4-OHT-ER-ERE binding at saturation is approximately 50% lower than that of E2-ER binding to all ERE sequences tested. hydroxytamoxifen 9-27 estrogen receptor 1 Homo sapiens 47-49 8738832-3 1996 Although 4-hydroxytamoxifen-liganded-ER (4-OHT-ER) and E2-ER bind a consensus ERE with equal high affinity, the stoichiometry of 4-OHT-ER-ERE binding at saturation is approximately 50% lower than that of E2-ER binding to all ERE sequences tested. hydroxytamoxifen 9-27 estrogen receptor 1 Homo sapiens 47-49 8809185-2 1996 These assays revealed identical, high affinity ER-ERE binding, Kd of approximately 0.25 nM, for estradiol-liganded ER (E2-ER), 4-hydroxytamoxifen liganded ER (4-OHT-ER), tamoxifen aziridine liganded ER (TAz-ER), and unliganded dimeric ER, for each ERE in constructs containing up to four tandem EREs. hydroxytamoxifen 127-145 estrogen receptor 1 Homo sapiens 47-49 8809185-2 1996 These assays revealed identical, high affinity ER-ERE binding, Kd of approximately 0.25 nM, for estradiol-liganded ER (E2-ER), 4-hydroxytamoxifen liganded ER (4-OHT-ER), tamoxifen aziridine liganded ER (TAz-ER), and unliganded dimeric ER, for each ERE in constructs containing up to four tandem EREs. hydroxytamoxifen 127-145 estrogen receptor 1 Homo sapiens 50-52 8809185-2 1996 These assays revealed identical, high affinity ER-ERE binding, Kd of approximately 0.25 nM, for estradiol-liganded ER (E2-ER), 4-hydroxytamoxifen liganded ER (4-OHT-ER), tamoxifen aziridine liganded ER (TAz-ER), and unliganded dimeric ER, for each ERE in constructs containing up to four tandem EREs. hydroxytamoxifen 127-145 estrogen receptor 1 Homo sapiens 50-52 8809185-2 1996 These assays revealed identical, high affinity ER-ERE binding, Kd of approximately 0.25 nM, for estradiol-liganded ER (E2-ER), 4-hydroxytamoxifen liganded ER (4-OHT-ER), tamoxifen aziridine liganded ER (TAz-ER), and unliganded dimeric ER, for each ERE in constructs containing up to four tandem EREs. hydroxytamoxifen 127-145 estrogen receptor 1 Homo sapiens 50-52 8809185-2 1996 These assays revealed identical, high affinity ER-ERE binding, Kd of approximately 0.25 nM, for estradiol-liganded ER (E2-ER), 4-hydroxytamoxifen liganded ER (4-OHT-ER), tamoxifen aziridine liganded ER (TAz-ER), and unliganded dimeric ER, for each ERE in constructs containing up to four tandem EREs. hydroxytamoxifen 127-145 estrogen receptor 1 Homo sapiens 50-52 8640815-7 1996 Another metabolite of 4-OH-tam, assumed to be 3,4-dihydroxytamoxifen (3,4-di-OH-tam) catechol, was demonstrated by its monomethylation with [3H]S-adenosyl-L-methionine ([3H]SAM) in presence of endogenous catechol-O-methyltransferase. hydroxytamoxifen 22-30 catechol-O-methyltransferase Rattus norvegicus 204-232 8593782-9 1996 MCF-7WT and MCF-7D3Res cells exhibit comparable sensitivity to induction of apoptosis and up-regulation of clusterin in response to the antiestrogen 4-hydroxytamoxifen. hydroxytamoxifen 149-167 clusterin Homo sapiens 107-116 8593782-11 1996 In both sensitive and resistant cell lines, 1,25-(OH)2D3 up-regulates whereas 4-hydroxytamoxifen down-regulates VDR protein expression, indicating appropriate homologous and heterologous VDR regulation in MCF-7D3Ras cells. hydroxytamoxifen 78-96 vitamin D receptor Homo sapiens 112-115 8825558-7 1996 Induction of rPRL and rPRL-Tn5 expression by E2 was reduced by coincubation of cells with the antiestrogen 4-hydroxytamoxifen. hydroxytamoxifen 107-125 prolactin Rattus norvegicus 13-17 8825558-7 1996 Induction of rPRL and rPRL-Tn5 expression by E2 was reduced by coincubation of cells with the antiestrogen 4-hydroxytamoxifen. hydroxytamoxifen 107-125 prolactin Rattus norvegicus 22-26 8524784-6 1995 Binding also occurs with the glucocorticoid receptor complexed with the antiglucocorticoid RU 38486, with the estrogen receptor complexed with the antiestrogen 4-hydroxytamoxifen or ICI 164,384, and even with receptors not complexed with ligand. hydroxytamoxifen 160-178 nuclear receptor subfamily 3 group C member 1 Homo sapiens 29-52 7838527-3 1995 Addition of estrogen or the antagonist hydroxytamoxifen to Jurkat T-cells expressing these constructs led to the trans-activation or responsive promoters and upregulation of cell surface markers CD28, CD69 and CD5 but not CD25 (IL2R-alpha subunit) or B7 (ligand for CD28). hydroxytamoxifen 39-55 CD28 molecule Homo sapiens 195-199 7649107-6 1995 The PKC-modulating drugs, bryostatin and H-7, and antiestrogens (ICI 164,384 and 4-hydroxytamoxifen) interfere with AR induction by TPA and estrogen, respectively. hydroxytamoxifen 81-99 amphiregulin Homo sapiens 116-118 7624356-2 1995 We have established homozygous retinoid X receptor alpha-negative (RXR alpha-/-) F9 embryonal carcinoma cells constitutively expressing Cre-ER and have shown that estradiol or the estrogen agonist/antagonist 4-hydroxytamoxifen efficiently induced the recombinase activity, whereas no activity was detected in the absence of ligand or in the presence of the antiestrogen ICI 164,384. hydroxytamoxifen 208-226 retinoid X receptor alpha Homo sapiens 31-56 7760810-6 1995 We demonstrate that the transcriptional activity of GATA-1 is strongly repressed by the estrogen receptor (ER) in a ligand-dependent manner and that this repression is reversible in the presence of 4-hydroxytamoxifen. hydroxytamoxifen 198-216 GATA binding protein 1 Homo sapiens 52-58 7760810-6 1995 We demonstrate that the transcriptional activity of GATA-1 is strongly repressed by the estrogen receptor (ER) in a ligand-dependent manner and that this repression is reversible in the presence of 4-hydroxytamoxifen. hydroxytamoxifen 198-216 estrogen receptor 1 Homo sapiens 88-105 7760810-6 1995 We demonstrate that the transcriptional activity of GATA-1 is strongly repressed by the estrogen receptor (ER) in a ligand-dependent manner and that this repression is reversible in the presence of 4-hydroxytamoxifen. hydroxytamoxifen 198-216 estrogen receptor 1 Homo sapiens 107-109 7784172-7 1995 When the hormone-binding domain of this mutant oestrogen receptor is fused to the C-terminus of the c-Myc protein, Myc-induced proliferation and apoptosis in fibroblasts becomes dependent on 4-hydroxytamoxifen, but remains refractory to 17 beta-oestradiol. hydroxytamoxifen 191-209 myelocytomatosis oncogene Mus musculus 102-105 7784172-7 1995 When the hormone-binding domain of this mutant oestrogen receptor is fused to the C-terminus of the c-Myc protein, Myc-induced proliferation and apoptosis in fibroblasts becomes dependent on 4-hydroxytamoxifen, but remains refractory to 17 beta-oestradiol. hydroxytamoxifen 191-209 myelocytomatosis oncogene Mus musculus 115-118 7867590-6 1995 This stimulation was mediated by ER, because 1) dose-response curves established with tamoxifen and hydroxytamoxifen were in agreement with their affinity for ER; 2) when present with antiestrogens, estradiol abolished this phenomenon; and 3) this effect was not observed in MDT (ER-negative) cells. hydroxytamoxifen 100-116 estrogen receptor 1 Homo sapiens 33-35 7867590-6 1995 This stimulation was mediated by ER, because 1) dose-response curves established with tamoxifen and hydroxytamoxifen were in agreement with their affinity for ER; 2) when present with antiestrogens, estradiol abolished this phenomenon; and 3) this effect was not observed in MDT (ER-negative) cells. hydroxytamoxifen 100-116 estrogen receptor 1 Homo sapiens 159-161 7867590-6 1995 This stimulation was mediated by ER, because 1) dose-response curves established with tamoxifen and hydroxytamoxifen were in agreement with their affinity for ER; 2) when present with antiestrogens, estradiol abolished this phenomenon; and 3) this effect was not observed in MDT (ER-negative) cells. hydroxytamoxifen 100-116 estrogen receptor 1 Homo sapiens 159-161 7873531-6 1995 Interestingly, when ER was liganded with 4-hydroxytamoxifen (4-OHT), the active metabolite of the widely used therapeutic antiestrogen tamoxifen, the antiestrogen-liganded ER complex (4-OHT-ER) did not bind cooperatively to multiple EREs, regardless of spacing or flanking sequence. hydroxytamoxifen 41-59 estrogen receptor 1 Homo sapiens 20-22 7873531-6 1995 Interestingly, when ER was liganded with 4-hydroxytamoxifen (4-OHT), the active metabolite of the widely used therapeutic antiestrogen tamoxifen, the antiestrogen-liganded ER complex (4-OHT-ER) did not bind cooperatively to multiple EREs, regardless of spacing or flanking sequence. hydroxytamoxifen 41-59 estrogen receptor 1 Homo sapiens 172-174 7625716-6 1995 Alternatively, if a "TAF2 function" is supplied by another factor, 4-OH tamoxifen can manifest ER agonist activity. hydroxytamoxifen 67-81 TATA-box binding protein associated factor 2 Homo sapiens 21-25 8592512-7 1995 Depending on the cell and promoter context and the particular ER form expressed, 4-OH tamoxifen and the related compound, keoxifene, functioned as partial agonists. hydroxytamoxifen 81-95 estrogen receptor 1 Homo sapiens 62-64 7649348-5 1995 Hydroxy-tamoxifen was shown to increase latent TGF-beta 1 secretion in three of the eight tumor tissue-derived fibroblast cultures. hydroxytamoxifen 0-17 transforming growth factor beta 1 Homo sapiens 47-57 7721882-6 1995 Our study also demonstrates that, within the context of the whole human estrogen receptor, the same AF-1 activating domains are "induced" by either estradiol or 4-hydroxytamoxifen. hydroxytamoxifen 161-179 estrogen receptor 1 Homo sapiens 72-89 7721882-6 1995 Our study also demonstrates that, within the context of the whole human estrogen receptor, the same AF-1 activating domains are "induced" by either estradiol or 4-hydroxytamoxifen. hydroxytamoxifen 161-179 interferon gamma receptor 2 Homo sapiens 100-104 7838527-3 1995 Addition of estrogen or the antagonist hydroxytamoxifen to Jurkat T-cells expressing these constructs led to the trans-activation or responsive promoters and upregulation of cell surface markers CD28, CD69 and CD5 but not CD25 (IL2R-alpha subunit) or B7 (ligand for CD28). hydroxytamoxifen 39-55 CD69 molecule Homo sapiens 201-205 7838527-3 1995 Addition of estrogen or the antagonist hydroxytamoxifen to Jurkat T-cells expressing these constructs led to the trans-activation or responsive promoters and upregulation of cell surface markers CD28, CD69 and CD5 but not CD25 (IL2R-alpha subunit) or B7 (ligand for CD28). hydroxytamoxifen 39-55 CD5 molecule Homo sapiens 210-213 7838527-3 1995 Addition of estrogen or the antagonist hydroxytamoxifen to Jurkat T-cells expressing these constructs led to the trans-activation or responsive promoters and upregulation of cell surface markers CD28, CD69 and CD5 but not CD25 (IL2R-alpha subunit) or B7 (ligand for CD28). hydroxytamoxifen 39-55 interleukin 2 receptor subunit alpha Homo sapiens 222-226 7838527-3 1995 Addition of estrogen or the antagonist hydroxytamoxifen to Jurkat T-cells expressing these constructs led to the trans-activation or responsive promoters and upregulation of cell surface markers CD28, CD69 and CD5 but not CD25 (IL2R-alpha subunit) or B7 (ligand for CD28). hydroxytamoxifen 39-55 interleukin 2 receptor subunit alpha Homo sapiens 228-238 7838527-3 1995 Addition of estrogen or the antagonist hydroxytamoxifen to Jurkat T-cells expressing these constructs led to the trans-activation or responsive promoters and upregulation of cell surface markers CD28, CD69 and CD5 but not CD25 (IL2R-alpha subunit) or B7 (ligand for CD28). hydroxytamoxifen 39-55 CD28 molecule Homo sapiens 266-270 7961858-2 1994 We have previously identified an intragenic (+698/+723) estrogen-responsive element present in the progesterone receptor gene, which binds the estradiol receptor and mediates estrogen and 4-OH tamoxifen induction. hydroxytamoxifen 188-202 progesterone receptor Homo sapiens 99-120 8573710-10 1995 Droloxifene and TAT-59 mimic the metabolite 4-hydroxytamoxifen in having a high affinity for the estrogen receptor (Jordan et al, J Endocrinol 75:305, 1977). hydroxytamoxifen 44-62 estrogen receptor 1 Homo sapiens 97-114 8001229-9 1994 Cis-4-hydroxytamoxifen was also converted to trans-4-hydroxytamoxifen (range 22-27%). hydroxytamoxifen 45-69 suppressor of cytokine signaling 6 Homo sapiens 0-5 7961858-3 1994 Progesterone receptor gene expression was equally stimulated by estradiol and 4-OH tamoxifen in the presence of a NH2 terminally deleted estrogen receptor mutant lacking activation function 1, suggesting that activation function 2 was the predominant activation domain. hydroxytamoxifen 78-92 progesterone receptor Homo sapiens 0-21 8274405-0 1993 Differential impact of flanking sequences on estradiol- vs 4-hydroxytamoxifen-liganded estrogen receptor binding to estrogen responsive element DNA. hydroxytamoxifen 59-77 estrogen receptor 1 Homo sapiens 87-104 7914405-5 1994 Antiestrogens such as tamoxifen, metabolites of tamoxifen (4-hydroxytamoxifen and N-desmethyltamoxifen), droloxifen, and toremifene stimulated the Pgp ATPase activity, and the maximum stimulation obtained with these agents equalled the maximal stimulation obtained by the best known MDR chemosensitizer, verapamil. hydroxytamoxifen 59-77 ATP binding cassette subfamily B member 1 Homo sapiens 147-150 7913604-2 1994 Tamoxifen and its metabolites, N-desmethyltamoxifen and 4-hydroxytamoxifen, were potent inhibitors of [3H]tamoxifen aziridine binding to P-glycoprotein with 4-hydroxytamoxifen > tamoxifen > N-desmethyltamoxifen. hydroxytamoxifen 56-74 ATP binding cassette subfamily B member 1 Homo sapiens 137-151 8205532-12 1994 The findings reported here raise the possibility that exposure of women undergoing tamoxifen therapy to agents that induce human CYP1A2 or CYPB1/2 analogues may produce increased levels of 4-hydroxytamoxifen and that this may affect the therapeutic potency of tamoxifen. hydroxytamoxifen 189-207 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 129-135 8293548-10 1994 The major metabolite detected by HPLC was N-desmethyltamoxifen, and 4-hydroxytamoxifen was also detected in cells with cytochrome P450 2E1 and 2D6. hydroxytamoxifen 68-86 cytochrome P450 family 2 subfamily E member 1 Homo sapiens 119-146 7873531-6 1995 Interestingly, when ER was liganded with 4-hydroxytamoxifen (4-OHT), the active metabolite of the widely used therapeutic antiestrogen tamoxifen, the antiestrogen-liganded ER complex (4-OHT-ER) did not bind cooperatively to multiple EREs, regardless of spacing or flanking sequence. hydroxytamoxifen 41-59 estrogen receptor 1 Homo sapiens 172-174 8137248-3 1994 All-trans-retinoic acid (RA) and 1,25-dihydroxyvitamin D3 (Vit D3) inhibited estrogen-induced growth of MCF-7 cells and their effect was potentiated by the classical antiestrogen, hydroxytamoxifen. hydroxytamoxifen 180-196 vitrin Homo sapiens 59-62 8143893-2 1993 We have evaluated the regulation of TGF beta 1, TGF beta 2, and TGF beta 3 mRNAs by 17 beta-estradiol (E2) and 4-hydroxytamoxifen (MOH) in estrogen receptor-positive (ER(+)) MCF-7 and estrogen receptor-negative (ER(-)) MDA-MB-231 human breast cancer cells. hydroxytamoxifen 111-129 transforming growth factor beta 1 Homo sapiens 36-46 8143893-2 1993 We have evaluated the regulation of TGF beta 1, TGF beta 2, and TGF beta 3 mRNAs by 17 beta-estradiol (E2) and 4-hydroxytamoxifen (MOH) in estrogen receptor-positive (ER(+)) MCF-7 and estrogen receptor-negative (ER(-)) MDA-MB-231 human breast cancer cells. hydroxytamoxifen 111-129 transforming growth factor beta 2 Homo sapiens 48-58 8143893-2 1993 We have evaluated the regulation of TGF beta 1, TGF beta 2, and TGF beta 3 mRNAs by 17 beta-estradiol (E2) and 4-hydroxytamoxifen (MOH) in estrogen receptor-positive (ER(+)) MCF-7 and estrogen receptor-negative (ER(-)) MDA-MB-231 human breast cancer cells. hydroxytamoxifen 111-129 transforming growth factor beta 3 Homo sapiens 64-74 8344199-7 1993 By contrast, 4-hydroxytamoxifen had an agonist effect on cathepsin-D and an additive effect on IGF-I-induced mRNA. hydroxytamoxifen 13-31 cathepsin D Homo sapiens 57-68 8402691-7 1993 However, treatment with the antiestrogen hydroxytamoxifen caused growth inhibition, implying that hydroxytamoxifen acts as an agonist of estrogen action in ER-transfected cells. hydroxytamoxifen 41-57 estrogen receptor 1 Homo sapiens 156-158 8402691-7 1993 However, treatment with the antiestrogen hydroxytamoxifen caused growth inhibition, implying that hydroxytamoxifen acts as an agonist of estrogen action in ER-transfected cells. hydroxytamoxifen 98-114 estrogen receptor 1 Homo sapiens 156-158 8344199-7 1993 By contrast, 4-hydroxytamoxifen had an agonist effect on cathepsin-D and an additive effect on IGF-I-induced mRNA. hydroxytamoxifen 13-31 insulin like growth factor 1 Homo sapiens 95-100 8324732-3 1993 A stepwise in vitro selection of the hormone-independent human breast cancer variant MCF-7/LCC1 against 4-hydroxytamoxifen produced a stable resistant population designated MCF7/LCC2. hydroxytamoxifen 104-122 C-C motif chemokine ligand 16 Homo sapiens 91-95 8357855-1 1993 A highly sensitive and specific assay was developed for the quantitative measurement of 4-hydroxy tamoxifen (4-OH Tam) at the femtomole level in human plasma and mammary tumours. hydroxytamoxifen 88-107 Myeloproliferative syndrome, transient (transient abnormal myelopoiesis) Homo sapiens 114-117 8388710-7 1993 ICI 164384 and the tamoxifen metabolite 4-hydroxytamoxifen also blocked 17 beta-hydroxysteroid dehydrogenase at concentrations of 470 and 275 microM, respectively. hydroxytamoxifen 40-58 hydroxysteroid 17-beta dehydrogenase 7 Homo sapiens 72-108 8388710-8 1993 In human breast tumors, 4-hydroxytamoxifen and desmethyltamoxifen blocked estrone sulfatase and 17 beta-hydroxysteroid dehydrogenase but at higher concentrations than in the rat (i.e. IC50s of 1000-2000 microM). hydroxytamoxifen 24-42 hydroxysteroid 17-beta dehydrogenase 7 Homo sapiens 96-132 1419885-7 1992 However, the elution profile of the DP-TAT-59-ER complex from a DEAE-Sephadex column was different for both estradiol-and 4-OH-TAM-ER complexes. hydroxytamoxifen 122-130 estrogen receptor 1 Rattus norvegicus 46-48 8502228-7 1993 The nonsteroidal antiestrogens nafoxidine, Cl-628, and 4-hydroxytamoxifen also induce c-fos expression. hydroxytamoxifen 55-73 Fos proto-oncogene, AP-1 transcription factor subunit Rattus norvegicus 86-91 8219251-2 1993 Previous studies have demonstrated that a point mutation in the estrogen receptor (ER) resulted in an alteration of the pharmacology of 4-hydroxytamoxifen, the active metabolite of tamoxifen (Jiang et al, Mol Endocrinol 6:2167-2174, 1992). hydroxytamoxifen 136-154 estrogen receptor 1 Homo sapiens 64-81 8219251-2 1993 Previous studies have demonstrated that a point mutation in the estrogen receptor (ER) resulted in an alteration of the pharmacology of 4-hydroxytamoxifen, the active metabolite of tamoxifen (Jiang et al, Mol Endocrinol 6:2167-2174, 1992). hydroxytamoxifen 136-154 estrogen receptor 1 Homo sapiens 83-85 1491696-3 1992 We have studied the effect of a point mutation that leads to the substitution of Val for Gly at codon 400 in the ligand-binding domain of the estrogen receptor (ER) on estrogenic and antiestrogenic activities of 4-hydroxytamoxifen (4-OHT) and its derivatives. hydroxytamoxifen 212-230 estrogen receptor 1 Homo sapiens 142-159 1491696-3 1992 We have studied the effect of a point mutation that leads to the substitution of Val for Gly at codon 400 in the ligand-binding domain of the estrogen receptor (ER) on estrogenic and antiestrogenic activities of 4-hydroxytamoxifen (4-OHT) and its derivatives. hydroxytamoxifen 212-230 estrogen receptor 1 Homo sapiens 161-163 8368130-12 1993 4-Hydroxytamoxifen had no effect on the steady-state level of receptor mRNA and effectively blocked the suppression of ER mRNA by estradiol. hydroxytamoxifen 0-18 estrogen receptor 1 Homo sapiens 119-121 1419885-8 1992 These results suggest that ER forms different complexes with DP-TAT-59 than estradiol or 4-OH-TAM, while the ER binding affinity of these compounds are similar to each other. hydroxytamoxifen 89-97 estrogen receptor 1 Rattus norvegicus 27-29 1537281-8 1992 While 4-OH-tam frequently decreased the amount of c-erbA beta transcripts, ICI 164 384 did not alter the distribution of alpha and beta cDNA transcripts. hydroxytamoxifen 6-14 thyroid hormone receptor beta Homo sapiens 50-61 1632645-3 1992 2, 307-312) were used to find the standard free energy changes that describe the binding of estradiol and 4-hydroxytamoxifen to the estrogen receptor. hydroxytamoxifen 106-124 estrogen receptor 1 Homo sapiens 132-149 1632645-4 1992 For the binding of estradiol or 4-hydroxytamoxifen to the estrogen receptor the data do not deviate systematically from the best fit to the model. hydroxytamoxifen 32-50 estrogen receptor 1 Homo sapiens 58-75 1632645-5 1992 The standard free energy change for binding of one molecule of estradiol at one site and one molecule of 4-hydroxytamoxifen at the second site of estrogen receptor indicates that 4-hydroxytamoxifen antagonizes the binding of estradiol to the estrogen receptor. hydroxytamoxifen 105-123 estrogen receptor 1 Homo sapiens 146-163 1632645-5 1992 The standard free energy change for binding of one molecule of estradiol at one site and one molecule of 4-hydroxytamoxifen at the second site of estrogen receptor indicates that 4-hydroxytamoxifen antagonizes the binding of estradiol to the estrogen receptor. hydroxytamoxifen 105-123 estrogen receptor 1 Homo sapiens 242-259 1632645-5 1992 The standard free energy change for binding of one molecule of estradiol at one site and one molecule of 4-hydroxytamoxifen at the second site of estrogen receptor indicates that 4-hydroxytamoxifen antagonizes the binding of estradiol to the estrogen receptor. hydroxytamoxifen 179-197 estrogen receptor 1 Homo sapiens 146-163 1632645-5 1992 The standard free energy change for binding of one molecule of estradiol at one site and one molecule of 4-hydroxytamoxifen at the second site of estrogen receptor indicates that 4-hydroxytamoxifen antagonizes the binding of estradiol to the estrogen receptor. hydroxytamoxifen 179-197 estrogen receptor 1 Homo sapiens 242-259 1614867-4 1992 We also confirm that the agonistic activity of 4-hydroxytamoxifen (OHT) can be ascribed to the activity of TAF-1. hydroxytamoxifen 47-65 histone acetyltransferase Saccharomyces cerevisiae S288C 107-112 1532902-1 1992 We have examined the effects of medroxyprogesterone acetate (MPA) and 4-hydroxytamoxifen (OH-TAM) on the cell proliferation and the expression of TGF-alpha and TGF-beta genes in Ishikawa cells and HEC-50 human endometrial adenocarcinoma cells. hydroxytamoxifen 70-88 transforming growth factor alpha Homo sapiens 146-155 1532902-1 1992 We have examined the effects of medroxyprogesterone acetate (MPA) and 4-hydroxytamoxifen (OH-TAM) on the cell proliferation and the expression of TGF-alpha and TGF-beta genes in Ishikawa cells and HEC-50 human endometrial adenocarcinoma cells. hydroxytamoxifen 70-88 transforming growth factor beta 1 Homo sapiens 160-168 1661135-8 1991 The antiestrogens tamoxifen and 4-hydroxytamoxifen were found to enhance the growth stimulation resulting from Zn2+ induced IGF-II production in MI7 cells. hydroxytamoxifen 32-50 insulin like growth factor 2 Homo sapiens 124-130 1776859-8 1991 In the same way, the antiestrogen 4-hydroxytamoxifen equally decreased c-myc expression but the reversal effect of E2 after long-term antiestrogen treatment was more pronounced than after short-term treatment. hydroxytamoxifen 34-52 MYC proto-oncogene, bHLH transcription factor Homo sapiens 71-76 1930624-3 1991 Production of GCDFP-15 was increased by oestradiol-17 beta, tamoxifen and 4-OH tamoxifen. hydroxytamoxifen 74-88 prolactin induced protein Homo sapiens 14-22 1930624-5 1991 Moreover, oestradiol-17 beta and 4-OH tamoxifen acted synergystically in enhancing GCDFP-15 release. hydroxytamoxifen 33-47 prolactin induced protein Homo sapiens 83-91 1562525-0 1992 Accumulation of a non-binding form of estrogen receptor in MCF-7 cells under hydroxytamoxifen treatment. hydroxytamoxifen 77-93 estrogen receptor 1 Homo sapiens 38-55 18755852-4 2008 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. hydroxytamoxifen 92-110 estrogen receptor 1 Homo sapiens 38-55 1834933-8 1991 The inhibitory effect of norethindrone on TGF beta 2 and TGF beta 3 mRNA levels could be blocked by the addition of 10(-7) M 4-hydroxytamoxifen. hydroxytamoxifen 125-143 transforming growth factor beta 3 Homo sapiens 57-67 1883484-4 1991 PR was significantly increased following treatment with 4-OH tamoxifen, this response being antagonized in the presence of ICI 164,384. hydroxytamoxifen 56-70 progesterone receptor Homo sapiens 0-2 2005879-3 1991 This compound, 4-hydroxytamoxifen, is a metabolite of tamoxifen and has a very high binding affinity for ER [J. Endocrinol. hydroxytamoxifen 15-33 estrogen receptor 1 Homo sapiens 105-107 1826824-0 1991 Distinct effects of gonadotropin-releasing hormone analogs and 4-hydroxytamoxifen on pS2 mRNA expression with respect to cell proliferation in MCF-7 breast cancer cells. hydroxytamoxifen 63-81 taste 2 receptor member 64 pseudogene Homo sapiens 85-88 1965340-4 1990 We have found that: 1) cellular proliferation and estrogen or progesterone receptor concentration were mutually dependent, the greatest estradiol binding capacity was obtained in cells in which mitotic activity had been slowed down (G0/G1) by the antiestrogenic action of hydroxytamoxifen added to the culture; 2) the presence of estradiol in the culture medium induced marked changes in the synthesis and catabolism of estrogen and progesterone receptors; and 3) both receptors acted as functional proteins whose intracellular concentrations varied depending on the phases of the mitotic cycle. hydroxytamoxifen 272-288 progesterone receptor Homo sapiens 62-83 2144749-6 1990 Secretion of insulin-like growth factor 1 (IGF-1) was not affected by DFMO-induced polyamine depletion but 4-hydroxytamoxifen increased IGF-1, which suggests an estradiol-like effect. hydroxytamoxifen 107-125 insulin like growth factor 1 Homo sapiens 136-141 1868844-1 1991 The action of diethylpyrocarbonate on lamb uterine estrogen receptor produced an homogeneous population of the receptor (approximately 55%) which still bound triarylethylene antiestrogens such as 4-hydroxytamoxifen with a high affinity but bound classical potent estrogens such as estradiol or diethylstilbestrol with a very low affinity. hydroxytamoxifen 196-214 estrogen receptor 1 Homo sapiens 51-68 1834933-8 1991 The inhibitory effect of norethindrone on TGF beta 2 and TGF beta 3 mRNA levels could be blocked by the addition of 10(-7) M 4-hydroxytamoxifen. hydroxytamoxifen 125-143 transforming growth factor beta 2 Homo sapiens 42-52 2257239-4 1990 Another interesting aspect is the response of the antiestrogen 4-hydroxytamoxifen which in isolated cells of very close tissues such as the uterus and vagina is an antagonist for the former and agonist for the latter concerning the progesterone receptor. hydroxytamoxifen 63-81 LOW QUALITY PROTEIN: progesterone receptor Cavia porcellus 232-253 2280188-8 1990 Finally, studies using the anti-estrogen drug, hydroxytamoxifen, resulted in blockage of the estrogen-related induction of RBP mRNA in the kidney, suggesting that the induction of RBP mRNA in the kidney by estrogen may be mediated by the nuclear estrogen receptor. hydroxytamoxifen 47-63 retinol binding protein 4 Rattus norvegicus 123-126 2280188-8 1990 Finally, studies using the anti-estrogen drug, hydroxytamoxifen, resulted in blockage of the estrogen-related induction of RBP mRNA in the kidney, suggesting that the induction of RBP mRNA in the kidney by estrogen may be mediated by the nuclear estrogen receptor. hydroxytamoxifen 47-63 retinol binding protein 4 Rattus norvegicus 180-183 18755852-4 2008 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. hydroxytamoxifen 92-110 estrogen receptor 1 Homo sapiens 57-59 34261921-2 2021 Previously, we found that RPS14 was significantly downregulated in estrogen receptor-positive (ER+) breast cancer cells following treatment with 4-hydroxytamoxifen (4-OH-TAM). hydroxytamoxifen 165-173 ribosomal protein S14 Homo sapiens 26-31 34261921-2 2021 Previously, we found that RPS14 was significantly downregulated in estrogen receptor-positive (ER+) breast cancer cells following treatment with 4-hydroxytamoxifen (4-OH-TAM). hydroxytamoxifen 165-173 estrogen receptor 1 Homo sapiens 67-84 34261921-2 2021 Previously, we found that RPS14 was significantly downregulated in estrogen receptor-positive (ER+) breast cancer cells following treatment with 4-hydroxytamoxifen (4-OH-TAM). hydroxytamoxifen 165-173 epiregulin Homo sapiens 95-97 2608058-4 1989 4-Hydroxytamoxifen had no effect on the steady-state level of receptor mRNA and effectively blocked the suppression of ER mRNA by estradiol. hydroxytamoxifen 0-18 estrogen receptor 1 Homo sapiens 119-121 2790797-4 1989 In order to gain insight into the molecular mechanism of action of antiestrogens in human breast cancer, we studied the effect of tamoxifen and 4-hydroxytamoxifen on the concentration of ODC mRNA, ODC activity, and the polyamine levels in a hormone-responsive breast cancer cell line, MCF-7. hydroxytamoxifen 144-162 ornithine decarboxylase 1 Homo sapiens 187-190 2790797-5 1989 ODC mRNA concentration was reduced to 40% of the controls after 6 h of treatment of the cells with 100 nM 4-hydroxytamoxifen, but tamoxifen had no significant effect on ODC mRNA after treating with even 1 microM concentration for 36 h. ODC activity was, however, reduced to 40 and 75% of the controls after 24 h of treatment with 4-hydroxytamoxifen and tamoxifen, respectively. hydroxytamoxifen 106-124 ornithine decarboxylase 1 Homo sapiens 0-3 2790797-5 1989 ODC mRNA concentration was reduced to 40% of the controls after 6 h of treatment of the cells with 100 nM 4-hydroxytamoxifen, but tamoxifen had no significant effect on ODC mRNA after treating with even 1 microM concentration for 36 h. ODC activity was, however, reduced to 40 and 75% of the controls after 24 h of treatment with 4-hydroxytamoxifen and tamoxifen, respectively. hydroxytamoxifen 330-348 ornithine decarboxylase 1 Homo sapiens 0-3 2783569-3 1989 This response to EGF was dose dependent; a half-maximal effect was obtained at 10(-10) M. The antiestrogens tamoxifen and 4-hydroxytamoxifen were able to antagonize the stimulatory effect of EGF on progesterone receptor concentrations, but they did not affect its mitogenic effect. hydroxytamoxifen 122-140 epidermal growth factor Homo sapiens 17-20 2775256-3 1989 The secretion of Tf by the hormone-responsive cell-line MCF-7 is stimulated by 17 beta-estradiol and reduced by the antiestrogen 4-hydroxy tamoxifen. hydroxytamoxifen 129-148 transferrin Homo sapiens 17-19 2720565-3 1989 Addition of the active metabolite of the estrogen-receptor blocker/partial-agonist 4-hydroxytamoxifen had a stimulating effect on the growth rate of the gastric cell lines. hydroxytamoxifen 83-101 estrogen receptor 1 Homo sapiens 41-58 2736207-4 1989 N-Desmethyltamoxifen and 4-hydroxytamoxifen behaved like tamoxifen except that N-desmethyltamoxifen did not induce the pNR-2 RNA and was only a partial oestrogen for the induction of cathepsin D RNA, and 4-hydroxytamoxifen did not induce the pNR-2 or pNR-25 RNAs. hydroxytamoxifen 25-43 cathepsin D Homo sapiens 183-194 2631032-3 1989 Epidermal growth factor (EGF) stimulates both cell proliferation and the progesterone receptor 4-Hydroxytamoxifen, a tamoxifen metabolite and potent anti-oestrogen, completely inhibits the stimulatory effect of EGF on the progesterone receptor but has no effect on the EGF-induced cell growth. hydroxytamoxifen 95-113 pro-epidermal growth factor Cavia porcellus 0-23 2631032-3 1989 Epidermal growth factor (EGF) stimulates both cell proliferation and the progesterone receptor 4-Hydroxytamoxifen, a tamoxifen metabolite and potent anti-oestrogen, completely inhibits the stimulatory effect of EGF on the progesterone receptor but has no effect on the EGF-induced cell growth. hydroxytamoxifen 95-113 pro-epidermal growth factor Cavia porcellus 25-28 2631032-3 1989 Epidermal growth factor (EGF) stimulates both cell proliferation and the progesterone receptor 4-Hydroxytamoxifen, a tamoxifen metabolite and potent anti-oestrogen, completely inhibits the stimulatory effect of EGF on the progesterone receptor but has no effect on the EGF-induced cell growth. hydroxytamoxifen 95-113 LOW QUALITY PROTEIN: progesterone receptor Cavia porcellus 73-94 2631032-3 1989 Epidermal growth factor (EGF) stimulates both cell proliferation and the progesterone receptor 4-Hydroxytamoxifen, a tamoxifen metabolite and potent anti-oestrogen, completely inhibits the stimulatory effect of EGF on the progesterone receptor but has no effect on the EGF-induced cell growth. hydroxytamoxifen 95-113 pro-epidermal growth factor Cavia porcellus 211-214 2631032-3 1989 Epidermal growth factor (EGF) stimulates both cell proliferation and the progesterone receptor 4-Hydroxytamoxifen, a tamoxifen metabolite and potent anti-oestrogen, completely inhibits the stimulatory effect of EGF on the progesterone receptor but has no effect on the EGF-induced cell growth. hydroxytamoxifen 95-113 LOW QUALITY PROTEIN: progesterone receptor Cavia porcellus 222-243 2631032-3 1989 Epidermal growth factor (EGF) stimulates both cell proliferation and the progesterone receptor 4-Hydroxytamoxifen, a tamoxifen metabolite and potent anti-oestrogen, completely inhibits the stimulatory effect of EGF on the progesterone receptor but has no effect on the EGF-induced cell growth. hydroxytamoxifen 95-113 pro-epidermal growth factor Cavia porcellus 211-214 2784313-4 1989 In contrast, when cells are treated with the antiestrogen hydroxytamoxifen, a dose-dependent decrease in EGF-R level occurs. hydroxytamoxifen 58-74 epidermal growth factor receptor Homo sapiens 105-110 2783569-3 1989 This response to EGF was dose dependent; a half-maximal effect was obtained at 10(-10) M. The antiestrogens tamoxifen and 4-hydroxytamoxifen were able to antagonize the stimulatory effect of EGF on progesterone receptor concentrations, but they did not affect its mitogenic effect. hydroxytamoxifen 122-140 epidermal growth factor Homo sapiens 191-194 2783569-3 1989 This response to EGF was dose dependent; a half-maximal effect was obtained at 10(-10) M. The antiestrogens tamoxifen and 4-hydroxytamoxifen were able to antagonize the stimulatory effect of EGF on progesterone receptor concentrations, but they did not affect its mitogenic effect. hydroxytamoxifen 122-140 progesterone receptor Homo sapiens 198-219 2783569-4 1989 The inhibitory effect of 4-hydroxytamoxifen depended on concentration; half-maximal inhibition was observed between 0.5-1 X 10(-9) M. 4-Hydroxytamoxifen could completely inhibit the progesterone receptor increase due to EGF even when added to cells already exposed to the growth factor for 6 days. hydroxytamoxifen 25-43 progesterone receptor Homo sapiens 182-203 2783569-4 1989 The inhibitory effect of 4-hydroxytamoxifen depended on concentration; half-maximal inhibition was observed between 0.5-1 X 10(-9) M. 4-Hydroxytamoxifen could completely inhibit the progesterone receptor increase due to EGF even when added to cells already exposed to the growth factor for 6 days. hydroxytamoxifen 25-43 epidermal growth factor Homo sapiens 220-223 2783569-4 1989 The inhibitory effect of 4-hydroxytamoxifen depended on concentration; half-maximal inhibition was observed between 0.5-1 X 10(-9) M. 4-Hydroxytamoxifen could completely inhibit the progesterone receptor increase due to EGF even when added to cells already exposed to the growth factor for 6 days. hydroxytamoxifen 134-152 progesterone receptor Homo sapiens 182-203 2783569-4 1989 The inhibitory effect of 4-hydroxytamoxifen depended on concentration; half-maximal inhibition was observed between 0.5-1 X 10(-9) M. 4-Hydroxytamoxifen could completely inhibit the progesterone receptor increase due to EGF even when added to cells already exposed to the growth factor for 6 days. hydroxytamoxifen 134-152 epidermal growth factor Homo sapiens 220-223 3275538-5 1988 The increase in progesterone receptor depended on the dose of estradiol, with a half-maximal response at about 5 X 10(-11) M. Progesterone receptor concentrations were inhibited to below basal levels by progesterone and R5020 and the nonsteroidal antiestrogens, tamoxifen, and 4-hydroxytamoxifen. hydroxytamoxifen 277-295 LOW QUALITY PROTEIN: progesterone receptor Cavia porcellus 16-37 2784101-2 1989 Epidermal growth factor (EGF)-stimulated growth (10(-8) M EGF) was assayed in the MCF-7 breast cancer cell line in the presence of various concentrations (10(-10) to 10(-6) M) of three antiestrogens, 4-hydroxytamoxifen (OH TAM), TAM and ICI 164384. hydroxytamoxifen 200-218 epidermal growth factor Homo sapiens 25-28 3050278-4 1988 Both ligands prevented the inactivation of the estrogen receptor by diethylpyrocarbonate, estradiol being more efficient than 4-hydroxytamoxifen. hydroxytamoxifen 126-144 estrogen receptor 1 Homo sapiens 47-64 3378206-4 1988 This shows that the binding of PKC to immobilized N-didesmethyltamoxifen was not merely due to hydrophobic interactions, since N-didesmethyltamoxifen and 4-hydroxytamoxifen have nearly identical hydrophobicities. hydroxytamoxifen 154-172 proline rich transmembrane protein 2 Homo sapiens 31-34 2451827-1 1988 Treatment of human breast cancer cytosol with tamoxifen (Tam) or 4-monohydroxytamoxifen (MHT) enhances the immunoreactivity of the estrogen receptor toward monoclonal antibody H222 but not monoclonal antibodies D547 or D75. hydroxytamoxifen 65-87 estrogen receptor 1 Homo sapiens 131-148 3343247-7 1988 Administration of hydroxytamoxifen abolishes persistent induction of RBP mRNA, suggesting that residual hormone receptor complex plays a role in the persistent induction of RBP gene transcription. hydroxytamoxifen 18-34 SURP and G-patch domain containing 1 L homeolog Xenopus laevis 69-72 3343247-7 1988 Administration of hydroxytamoxifen abolishes persistent induction of RBP mRNA, suggesting that residual hormone receptor complex plays a role in the persistent induction of RBP gene transcription. hydroxytamoxifen 18-34 SURP and G-patch domain containing 1 L homeolog Xenopus laevis 173-176 3167974-2 1988 Estradiol (E2) or the antiestrogen hydroxytamoxifen is required for ER binding as assayed by gel retardation. hydroxytamoxifen 35-51 estrogen receptor 1 Homo sapiens 68-70 3275538-5 1988 The increase in progesterone receptor depended on the dose of estradiol, with a half-maximal response at about 5 X 10(-11) M. Progesterone receptor concentrations were inhibited to below basal levels by progesterone and R5020 and the nonsteroidal antiestrogens, tamoxifen, and 4-hydroxytamoxifen. hydroxytamoxifen 277-295 LOW QUALITY PROTEIN: progesterone receptor Cavia porcellus 126-147 2824472-0 1987 Effects of tamoxifen and 4-hydroxytamoxifen on the pNR-1 and pNR-2 estrogen-regulated RNAs in human breast cancer cells. hydroxytamoxifen 25-43 trefoil factor 1 Homo sapiens 61-66 2824472-1 1987 The estrogenic and antiestrogenic activities of tamoxifen and 4-hydroxytamoxifen have been measured on the expression of two estrogen-regulated RNAs (pNR-1 and pNR-2) in the MCF7 human breast cancer cell line cultured in phenol red-free medium. hydroxytamoxifen 62-80 trefoil factor 1 Homo sapiens 160-165 2824472-3 1987 In contrast, the pNR-2 mRNA was only increased to about 10% of the estradiol-induced level, and its induction by estradiol was antagonized by both tamoxifen and 4-hydroxytamoxifen. hydroxytamoxifen 161-179 trefoil factor 1 Homo sapiens 17-22 2824472-5 1987 4-Hydroxytamoxifen and estradiol have similar affinities for the estrogen receptor; however, the induction of both RNAs by 4-hydroxytamoxifen required a 10-fold higher concentration than estradiol for maximum agonist activity, and a 500-fold molar excess was required to antagonize the induction by estradiol. hydroxytamoxifen 0-18 estrogen receptor 1 Homo sapiens 65-82 2824472-5 1987 4-Hydroxytamoxifen and estradiol have similar affinities for the estrogen receptor; however, the induction of both RNAs by 4-hydroxytamoxifen required a 10-fold higher concentration than estradiol for maximum agonist activity, and a 500-fold molar excess was required to antagonize the induction by estradiol. hydroxytamoxifen 123-141 estrogen receptor 1 Homo sapiens 65-82 3996316-7 1985 Using the 3-day uterine assay in vivo, 4-hydroxytamoxifen partially stimulated progesterone receptor induction in the immature rat, whereas it fully stimulated the same end point in the mature ovariectomized mouse. hydroxytamoxifen 39-57 progesterone receptor Rattus norvegicus 79-100 3343247-2 1988 Estrogen induction of RBP mRNA is completely blocked by the anti-estrogen, hydroxytamoxifen. hydroxytamoxifen 75-91 SURP and G-patch domain containing 1 L homeolog Xenopus laevis 22-25 3454873-3 1987 Administration of 4-hydroxytamoxifen 24 h before estradiol completely blocked both the suppression of albumin mRNA and the transcriptional activation of the vitellogenin genes. hydroxytamoxifen 18-36 Albumin A Xenopus laevis 102-109 3454873-3 1987 Administration of 4-hydroxytamoxifen 24 h before estradiol completely blocked both the suppression of albumin mRNA and the transcriptional activation of the vitellogenin genes. hydroxytamoxifen 18-36 a1-a Xenopus laevis 157-169 3743888-4 1986 In similar conditions hydroxytamoxifen-ER complexes apparently do not undergo such a modification. hydroxytamoxifen 22-38 estrogen receptor 1 Rattus norvegicus 39-41 3743888-7 1986 These data demonstrate that, in vitro, nuclear ER is cleaved into a smaller molecular form and that the receptor fragments can be held together by the triphenylethylene antiestrogen hydroxytamoxifen. hydroxytamoxifen 182-198 estrogen receptor 1 Rattus norvegicus 47-49 3736040-5 1986 Pre-injection with tamoxifen or 4-hydroxytamoxifen suppressed the estrogen-dependent induction of vitellogenin in serum. hydroxytamoxifen 32-50 a1-a Xenopus laevis 98-110 3736040-6 1986 4-Hydroxytamoxifen also inhibited the induction of intracellular vitellogenin and its mRNA by estrogen suggesting that this metabolite of tamoxifen is able to inhibit estrogen-induced transcription of the vitellogenin genes. hydroxytamoxifen 0-18 a1-a Xenopus laevis 65-77 3736040-6 1986 4-Hydroxytamoxifen also inhibited the induction of intracellular vitellogenin and its mRNA by estrogen suggesting that this metabolite of tamoxifen is able to inhibit estrogen-induced transcription of the vitellogenin genes. hydroxytamoxifen 0-18 a1-a Xenopus laevis 205-217 2820746-7 1987 Tamoxifen (TMX) and its metabolites dihydroxy (di-OH-TMX) and 4-hydroxytamoxifen (4-OH-TMX) inhibited PRL in a dose-dependent manner. hydroxytamoxifen 62-80 prolactin Rattus norvegicus 102-105 3497634-4 1987 Furthermore, EGF partially reversed the growth inhibitory effects of several other antiestrogens including tamoxifen, 4-hydroxytamoxifen, and LY 117018. hydroxytamoxifen 118-136 epidermal growth factor Homo sapiens 13-16 3579987-4 1987 Its binding affinity for the estrogen receptor was greater than that of tamoxifen but less than that of 4-hydroxytamoxifen, and it possessed a corresponding degree of antitumour activity against the MCF-7 breast cancer cell line. hydroxytamoxifen 104-122 estrogen receptor 1 Homo sapiens 29-46 3620717-3 1987 The antiestrogen 4-hydroxytamoxifen blocked progesterone receptor induction both by estradiol and by phenolphthalein. hydroxytamoxifen 17-35 progesterone receptor Homo sapiens 44-65 3320566-3 1987 Tamoxifen is readily metabolized by liver to 4-hydroxytamoxifen, which binds the liver nuclear estrogen receptor with a Ki of 0.1 nM. hydroxytamoxifen 45-63 estrogen receptor 1 Gallus gallus 95-112 3320567-5 1987 (3) In the uterus and vagina of newborn guinea-pigs, tamoxifen and its derivatives: 4-hydroxytamoxifen and N-desmethyltamoxifen act as real agonists concerning the uterotrophic and vaginotrophic effects, and also stimulate the amount of DNA per organ, but concerning the progesterone receptor in the uterus, in the short treatment anti-estrogens act as partial agonists but they have no effect in the long treatment. hydroxytamoxifen 84-102 LOW QUALITY PROTEIN: progesterone receptor Cavia porcellus 271-292 4066684-15 1985 They also confirm that the conformations of the estrogen receptor differ when bound to estradiol or to 4-hydroxytamoxifen. hydroxytamoxifen 103-121 estrogen receptor 1 Bos taurus 48-65 6704959-0 1984 Estrogen receptor-mediated and cytotoxic effects of the antiestrogens tamoxifen and 4-hydroxytamoxifen. hydroxytamoxifen 84-102 estrogen receptor 1 Homo sapiens 0-17 3987619-4 1985 Within 1-2 h of a sc injection of high affinity ligands (E2, E2B, and 4-OH-TAM), there was decrease in cytosol ER. hydroxytamoxifen 70-78 estrogen receptor 1 Rattus norvegicus 111-113 4010284-2 1985 Attempts to similarly characterize the isomers of hydroxytamoxifen (which differ greatly in their affinity for the estrogen receptor) are shown to be complicated by their facile isomerization. hydroxytamoxifen 50-66 estrogen receptor 1 Homo sapiens 115-132 7060530-7 1982 These results confirm that ER directly binds androstanediol, tamoxifen, and hydroxytamoxifen. hydroxytamoxifen 76-92 estrogen receptor 1 Bos taurus 27-29 6848368-1 1983 As the polynucleotide domain of the estrogen receptor (Re) is a possible site for the modulation of Re activity, the interaction of antiestrogen (4-hydroxytamoxifen and tamoxifen)-receptor complexes (4-OH-Tam-Re and Tam-Re) with polynucleotides (oligodeoxynucleotide-cellulose, DNA-cellulose, and polyribonucleotide-agarose) was investigated and compared with that of the 17 beta-estradiol-receptor complex (E2-Re). hydroxytamoxifen 146-164 estrogen receptor 1 Homo sapiens 36-53 6371570-5 1984 Tamoxifen and hydroxytamoxifen, estrogen antagonists, were ineffective by themselves, but reversed the E2 facilitation of K+-evoked LH-RH release. hydroxytamoxifen 14-30 gonadotropin releasing hormone 1 Rattus norvegicus 132-137 6537799-2 1984 Studies were undertaken to examine the biological character (estrogenic-antiestrogenic properties) and estrogen receptor (ER) interaction of the cis- and trans-isomers of tamoxifen and hydroxytamoxifen in MCF-7 human breast cancer cells. hydroxytamoxifen 185-201 estrogen receptor 1 Homo sapiens 103-120 6537799-4 1984 The relative binding affinities of the compounds cis-tamoxifen, trans-tamoxifen, cis-hydroxytamoxifen, and trans-hydroxytamoxifen for cytosol ER were 0.3, 2.5, 1.8, and 310%, respectively, in which the affinity of estradiol is considered 100%. hydroxytamoxifen 107-129 estrogen receptor 1 Homo sapiens 142-144 6537799-8 1984 trans-Hydroxytamoxifen had a 100-fold increased affinity for ER and was approximately 100-times more potent than was trans-tamoxifen in suppressing cell growth and plasminogen activator activity. hydroxytamoxifen 0-22 estrogen receptor 1 Homo sapiens 61-63 6537799-10 1984 This apparently paradoxical behavior of cis-hydroxytamoxifen was shown to be due to the fact that the cis- and trans-hydroxytamoxifens readily undergo isomeric interconversion upon exposure to our cell culture conditions, resulting in substantial accumulation of the higher-affinity trans-hydroxytamoxifen in the nuclear ER fraction of cells. hydroxytamoxifen 117-134 estrogen receptor 1 Homo sapiens 321-323 6537799-10 1984 This apparently paradoxical behavior of cis-hydroxytamoxifen was shown to be due to the fact that the cis- and trans-hydroxytamoxifens readily undergo isomeric interconversion upon exposure to our cell culture conditions, resulting in substantial accumulation of the higher-affinity trans-hydroxytamoxifen in the nuclear ER fraction of cells. hydroxytamoxifen 111-133 estrogen receptor 1 Homo sapiens 321-323 6708516-9 1984 ER concentration, estimated by the binding of 4-hydroxytamoxifen (OH-tam) and of estradiol was lower in LB cells than in original tam-sensitive L-929 cells. hydroxytamoxifen 46-64 estrogen receptor 1 (alpha) Mus musculus 0-2 6883346-3 1983 Under conditions where autoradiographic controls indicate that most of the estrogen receptor of MCF-7 human breast cancer cells is in the nucleus, we could demonstrate nuclear fluorescence using 10(-9) M concentrations of coumestrol, 12-oxoestradiol, and 4-hydroxytamoxifen. hydroxytamoxifen 255-273 estrogen receptor 1 Homo sapiens 75-92 6575210-5 1983 In the absence of 17 beta-estradiol, 3-hydroxytamoxifen gave rise to a moderate increase in the progesterone receptor levels, which demonstrates the partially estrogenic character of hydroxytamoxifen. hydroxytamoxifen 39-55 progesterone receptor Homo sapiens 96-117 29557271-3 2019 Rigid Docking analysis of DAH at the ligand binding domain (LBD) of ER alpha showed hydrogen bond interactions with Arg394 and Glu353 at the active site, similar to the positive controls 4-Hydroxy Tamoxifen (4-OHT) and Fulvestrant (FUL). hydroxytamoxifen 187-206 estrogen receptor 1 Homo sapiens 68-76 32085898-4 2020 In MDCK cells expressing a modified Src that can be activated by hydroxytamoxifen, activated Src was transported to late endosomes/lysosomes and secreted via sEVs. hydroxytamoxifen 65-81 SRC proto-oncogene, non-receptor tyrosine kinase Canis lupus familiaris 36-39 32085898-4 2020 In MDCK cells expressing a modified Src that can be activated by hydroxytamoxifen, activated Src was transported to late endosomes/lysosomes and secreted via sEVs. hydroxytamoxifen 65-81 SRC proto-oncogene, non-receptor tyrosine kinase Canis lupus familiaris 93-96 31826231-2 2019 Methods: Intraperitoneal administration of tamoxifen and (Z)-4-hydroxytamoxifen eyedrops were used to trace the lineage of Myh11-expressing cells with the Myh11-Cre-ERT2-flox-tdTomato mouse model. hydroxytamoxifen 57-79 myosin, heavy polypeptide 11, smooth muscle Mus musculus 123-128 31826231-2 2019 Methods: Intraperitoneal administration of tamoxifen and (Z)-4-hydroxytamoxifen eyedrops were used to trace the lineage of Myh11-expressing cells with the Myh11-Cre-ERT2-flox-tdTomato mouse model. hydroxytamoxifen 57-79 myosin, heavy polypeptide 11, smooth muscle Mus musculus 155-160 31826231-2 2019 Methods: Intraperitoneal administration of tamoxifen and (Z)-4-hydroxytamoxifen eyedrops were used to trace the lineage of Myh11-expressing cells with the Myh11-Cre-ERT2-flox-tdTomato mouse model. hydroxytamoxifen 57-79 mitogen-activated protein kinase 3 Mus musculus 165-169 31241994-5 2019 4-hydroxytamoxifen was injected into Sod2lox/lox, SM-CreERT2(ki)Cre/+ mice to activate CreERT2-mediated deletion of Sod2. hydroxytamoxifen 0-18 lysyl oxidase Mus musculus 41-44 31241994-5 2019 4-hydroxytamoxifen was injected into Sod2lox/lox, SM-CreERT2(ki)Cre/+ mice to activate CreERT2-mediated deletion of Sod2. hydroxytamoxifen 0-18 superoxide dismutase 2, mitochondrial Mus musculus 37-41 30987380-5 2019 Our transcriptomics analysis showed that 4-Hydroxytamoxifen (4-OHT), SEL alone or their combination induced differential Akt signaling- and metabolism-associated gene expression profiles. hydroxytamoxifen 41-59 AKT serine/threonine kinase 1 Homo sapiens 121-124 7317574-2 1981 4-Hydroxytamoxifen binds to the estrogen receptor with affinity equal to estradiol, and with 25-50 times higher affinity than does tamoxifen. hydroxytamoxifen 0-18 estrogen receptor 1 Homo sapiens 32-49 7451477-2 1981 4-Hydroxytamoxifen and M2, another hydroxylated metabolite of tamoxifen, were the major tritiated compounds of the cytosol and the KCl-nuclear extract of target tissues and appeared to occupy the estrogen receptor sites since their accumulation in these fractions was saturable, resistant to charcoal, and prevented by estradiol. hydroxytamoxifen 0-18 estrogen receptor 1 Rattus norvegicus 196-213 7451477-7 1981 4-Hydroxytamoxifen formed in vitro was able to bind selectively to estrogen receptor with a high affinity and with a low dissociation rate similar to estradiol. hydroxytamoxifen 0-18 estrogen receptor 1 Rattus norvegicus 67-84 7451477-8 1981 These results demonstrate that 4-hydroxytamoxifen is formed in vivo and retained on estrogen receptor in target tissues, due to its high affinity. hydroxytamoxifen 31-49 estrogen receptor 1 Rattus norvegicus 84-101 31916635-2 2020 TAM is activated by endogenous CYP450 enzymes to the more biologically active metabolites 4-hydroxytamoxifen and endoxifen mainly via CYP2D6 and CYP3A4/5. hydroxytamoxifen 90-108 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 134-140 31916635-2 2020 TAM is activated by endogenous CYP450 enzymes to the more biologically active metabolites 4-hydroxytamoxifen and endoxifen mainly via CYP2D6 and CYP3A4/5. hydroxytamoxifen 90-108 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 145-151 31141164-5 2019 Inhibition of NAMPT by FK866 inhibited cell viability and aggravated apoptosis in cancer cells treated with 4-hydroxytamoxifen. hydroxytamoxifen 108-126 nicotinamide phosphoribosyltransferase Mus musculus 14-19 31398422-0 2019 Corrigendum to "Plasma endoxifen and 4-hydroxytamoxifen levels in CYP2D6(C100T) carrying breast cancer patients and association with serum cholesterol" [Toxicology and Applied Pharmacology, 378 (2019) 114619]. hydroxytamoxifen 37-55 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 66-71 31263129-9 2019 Transient overexpression of HNRNPA2/B1 reduced MCF-7 sensitivity to 4-hydroxytamoxifen and fulvestrant, suggesting a role for HNRNPA2/B1 in endocrine-resistance. hydroxytamoxifen 68-86 heterogeneous nuclear ribonucleoprotein A2/B1 Homo sapiens 28-38 30937657-14 2019 4-OH-TAM sensitized ERalpha-positive breast cancer cells to docetaxel in a ZNF423 SNP-dependent manner. hydroxytamoxifen 0-8 estrogen receptor 1 Homo sapiens 20-27 30937657-14 2019 4-OH-TAM sensitized ERalpha-positive breast cancer cells to docetaxel in a ZNF423 SNP-dependent manner. hydroxytamoxifen 0-8 zinc finger protein 423 Homo sapiens 75-81 30901604-5 2019 In the present study, the effects of c-Myc activation in UW228-MycER MB cell line were investigated using 4-hydroxytamoxifen (4-OHT) induction system. hydroxytamoxifen 106-124 MYC proto-oncogene, bHLH transcription factor Homo sapiens 37-42 30707122-2 2019 WHAT THIS ARTICLE TELLS US THAT IS NEW: In a tamoxifen-activated astrocyte-specific Ndufs4(KO) mouse, the induction EC50s for tail clamp in both isoflurane and halothane were similar between the control and astrocyte-specific Ndufs4(KO) mice at 3 weeks after 4-hydroxy tamoxifen injection. hydroxytamoxifen 259-278 NADH:ubiquinone oxidoreductase core subunit S4 Mus musculus 84-90 30423024-7 2019 An in vitro model of CDH1 mutated ER-positive breast cancer demonstrates that NF1 knockdown confers a growth advantage in the presence of 4-hydroxy tamoxifen. hydroxytamoxifen 138-157 cadherin 1 Homo sapiens 21-25 30782165-12 2019 Importantly, MTA1 knockout sensitized hormone receptor negative cells to 4-hydroxy tamoxifen treatment, which could be reversed by the addition of MTA1-exosomes. hydroxytamoxifen 73-92 metastasis associated 1 Homo sapiens 13-17 30782165-12 2019 Importantly, MTA1 knockout sensitized hormone receptor negative cells to 4-hydroxy tamoxifen treatment, which could be reversed by the addition of MTA1-exosomes. hydroxytamoxifen 73-92 metastasis associated 1 Homo sapiens 147-151 30416150-8 2019 An in vitro spermatogonia culture model (germline stem cells) revealed that hydroxytamoxifen-induced deletion of PTBP1 from germline stem cells caused severe proliferation arrest accompanied by an increase of apoptotic cell death. hydroxytamoxifen 76-92 polypyrimidine tract binding protein 1 Mus musculus 113-118 30180270-9 2019 Nlrp3L351P CreT HSCs also showed elevated mRNA and protein expression of fibrotic markers 24 hours after inflammasome activation induced with 4-hydroxytamoxifen (4OHT). hydroxytamoxifen 142-160 NLR family, pyrin domain containing 3 Mus musculus 0-5 30180270-9 2019 Nlrp3L351P CreT HSCs also showed elevated mRNA and protein expression of fibrotic markers 24 hours after inflammasome activation induced with 4-hydroxytamoxifen (4OHT). hydroxytamoxifen 142-160 ret proto-oncogene Mus musculus 11-15 30423024-7 2019 An in vitro model of CDH1 mutated ER-positive breast cancer demonstrates that NF1 knockdown confers a growth advantage in the presence of 4-hydroxy tamoxifen. hydroxytamoxifen 138-157 neurofibromin 1 Homo sapiens 78-81 30312845-3 2018 Here, we engrafted the CRISPR/Cas9 system with a mutated human estrogen receptor (ERT2), which renders it 4-hydroxytamoxifen (4-OHT) inducible for the access of genome, and a nuclear export signal (NES), which lowers the background activity. hydroxytamoxifen 106-124 mitogen-activated protein kinase 3 Homo sapiens 82-86 29899353-4 2018 Using the qPLEX-RIME method, we delineate the temporal changes of the Estrogen Receptor alpha (ERalpha) interactome in breast cancer cells treated with 4-hydroxytamoxifen. hydroxytamoxifen 152-170 estrogen receptor 1 Homo sapiens 70-93 30208932-6 2018 METHODS: Tamoxifen-resistant ERalpha-positive MCF-7 and T47D breast cancer cell lines were established by culturing with gradually increased concentration of 4-hydroxytamoxifen (4-OHT). hydroxytamoxifen 158-176 estrogen receptor 1 Homo sapiens 29-36 29964089-4 2018 Here, we treated pregnant Abcg2 Cre/Cre RosaLSL-YFP mice with a single injection of 4-hydroxytamoxifen at embryonic day 7.5. hydroxytamoxifen 84-102 ATP binding cassette subfamily G member 2 (Junior blood group) Mus musculus 26-31 29890199-11 2018 These effects of glyphosate and E2 were abolished by the ER antagonist, 4-hydroxytamoxifen and U0126, a MEK inhibitor. hydroxytamoxifen 72-90 mitogen-activated protein kinase kinase 7 Homo sapiens 104-107 29899353-4 2018 Using the qPLEX-RIME method, we delineate the temporal changes of the Estrogen Receptor alpha (ERalpha) interactome in breast cancer cells treated with 4-hydroxytamoxifen. hydroxytamoxifen 152-170 estrogen receptor 1 Homo sapiens 95-102 29632071-9 2018 4-Hydroxytamoxifen (4OHT)-mediated transcriptional activity of mouse-human F domain-swapped ERalphas was the inverse of the WT ERalpha activities but not estradiol-mediated transcriptional activities. hydroxytamoxifen 0-18 estrogen receptor 1 Homo sapiens 92-99 29718959-9 2018 Treatment in vitro of CD4+ splenocytes from GIMAP6fl/flERT2Cre mice with 4-hydroxytamoxifen resulted in the disappearance of GIMAP6 within five days. hydroxytamoxifen 73-91 CD4 antigen Mus musculus 22-25 29545311-4 2018 SNIPER(ER)-87 consists of an inhibitor of apoptosis protein (IAP) ligand LCL161 derivative that is conjugated to the estrogen receptor alpha (ERalpha) ligand 4-hydroxytamoxifen by a PEG linker, and we have previously reported that this SNIPER efficiently degrades the ERalpha protein. hydroxytamoxifen 158-176 magnesium transporter 1 Homo sapiens 29-59 29545311-4 2018 SNIPER(ER)-87 consists of an inhibitor of apoptosis protein (IAP) ligand LCL161 derivative that is conjugated to the estrogen receptor alpha (ERalpha) ligand 4-hydroxytamoxifen by a PEG linker, and we have previously reported that this SNIPER efficiently degrades the ERalpha protein. hydroxytamoxifen 158-176 magnesium transporter 1 Homo sapiens 61-64 29545311-4 2018 SNIPER(ER)-87 consists of an inhibitor of apoptosis protein (IAP) ligand LCL161 derivative that is conjugated to the estrogen receptor alpha (ERalpha) ligand 4-hydroxytamoxifen by a PEG linker, and we have previously reported that this SNIPER efficiently degrades the ERalpha protein. hydroxytamoxifen 158-176 estrogen receptor 1 Homo sapiens 117-140 29545311-4 2018 SNIPER(ER)-87 consists of an inhibitor of apoptosis protein (IAP) ligand LCL161 derivative that is conjugated to the estrogen receptor alpha (ERalpha) ligand 4-hydroxytamoxifen by a PEG linker, and we have previously reported that this SNIPER efficiently degrades the ERalpha protein. hydroxytamoxifen 158-176 estrogen receptor 1 Homo sapiens 142-149 29545311-4 2018 SNIPER(ER)-87 consists of an inhibitor of apoptosis protein (IAP) ligand LCL161 derivative that is conjugated to the estrogen receptor alpha (ERalpha) ligand 4-hydroxytamoxifen by a PEG linker, and we have previously reported that this SNIPER efficiently degrades the ERalpha protein. hydroxytamoxifen 158-176 estrogen receptor 1 Homo sapiens 268-275 29718959-9 2018 Treatment in vitro of CD4+ splenocytes from GIMAP6fl/flERT2Cre mice with 4-hydroxytamoxifen resulted in the disappearance of GIMAP6 within five days. hydroxytamoxifen 73-91 GTPase, IMAP family member 6 Mus musculus 44-50 29385237-1 2018 Tamoxifen is biotransformed by CYP2D6 to 4-hydroxytamoxifen and 4-hydroxy N-desmethyl tamoxifen (endoxifen), both with greater antiestrogenic potency than the parent drug. hydroxytamoxifen 41-59 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 31-37 29718959-9 2018 Treatment in vitro of CD4+ splenocytes from GIMAP6fl/flERT2Cre mice with 4-hydroxytamoxifen resulted in the disappearance of GIMAP6 within five days. hydroxytamoxifen 73-91 GTPase, IMAP family member 6 Mus musculus 125-131 29176980-7 2017 In this system, the RAG1 protein is constitutively expressed and functional, while the RAG2 protein, coupled to the estrogen receptor, becomes functionally active upon 4-hydroxytamoxifen (TAM) administration. hydroxytamoxifen 168-186 recombination activating gene 2 Mus musculus 87-91 29237052-3 2018 Here, we designed and vigorously optimized a series of Hybrid drug Inducible CRISPR/Cas9 Technologies (HIT) for transcriptional activation by grafting a mutated human estrogen receptor (ERT2) to multiple CRISPR/Cas9 systems, which renders them 4-hydroxytamoxifen (4-OHT) inducible for the access of genome. hydroxytamoxifen 244-262 estrogen receptor 1 Homo sapiens 167-184 29237052-3 2018 Here, we designed and vigorously optimized a series of Hybrid drug Inducible CRISPR/Cas9 Technologies (HIT) for transcriptional activation by grafting a mutated human estrogen receptor (ERT2) to multiple CRISPR/Cas9 systems, which renders them 4-hydroxytamoxifen (4-OHT) inducible for the access of genome. hydroxytamoxifen 244-262 mitogen-activated protein kinase 3 Homo sapiens 186-190 29285606-9 2018 Regarding phase II metabolism, UGT2B7, 1A8 and 1A3 showed highest activity in glucuronidation of tamoxifen bisphenol and metabolite E. Anti-estrogenic metabolites (Z)-4-hydroxytamoxifen, (Z)-endoxifen and (Z)-norendoxifen inhibited the activity of CYP2C enzymes while tamoxifen bisphenol consistently induced CYPs similar to rifampicin and phenobarbital. hydroxytamoxifen 163-185 UDP glucuronosyltransferase family 2 member B7 Homo sapiens 31-37 29285606-10 2018 On the transcript level, highest induction up to 5.6-fold was observed for CYP3A4 by tamoxifen, (Z)-4-hydroxytamoxifen, tamoxifen bisphenol and (E)-metabolite E. Estrogen-like tamoxifen metabolites are formed in CYP-dependent reactions and are further metabolized by glucuronidation. hydroxytamoxifen 96-118 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 75-81 29436156-4 2018 Only the CYP2D6 variation was significantly associated with concentrations of endoxifen (P = 0.0008) and 4-hydroxytamoxifen (P = 0.0074), tamoxifen"s principal active metabolites, as well as key metabolic ratios. hydroxytamoxifen 105-123 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 9-15 29140506-7 2018 Six days of exposure to 17beta-estradiol or the selective ER modulator 4-hydroxytamoxifen respectively increased or decreased MCF7 organoid CSA (p < .01), consistent with the role of estrogen signaling in ER-positive mammary epithelial cell proliferation. hydroxytamoxifen 71-89 estrogen receptor 1 Homo sapiens 58-60 29140506-7 2018 Six days of exposure to 17beta-estradiol or the selective ER modulator 4-hydroxytamoxifen respectively increased or decreased MCF7 organoid CSA (p < .01), consistent with the role of estrogen signaling in ER-positive mammary epithelial cell proliferation. hydroxytamoxifen 71-89 estrogen receptor 1 Homo sapiens 208-210 29389973-7 2018 In addition, leptin, IL-6 and TNFalpha, at concentrations reflecting plasma concentrations in obese patients, decreased the anti-proliferative efficacy of 4-hydroxytamoxifen (a major active metabolite of Tx). hydroxytamoxifen 155-173 leptin Homo sapiens 13-19 29389973-7 2018 In addition, leptin, IL-6 and TNFalpha, at concentrations reflecting plasma concentrations in obese patients, decreased the anti-proliferative efficacy of 4-hydroxytamoxifen (a major active metabolite of Tx). hydroxytamoxifen 155-173 interleukin 6 Homo sapiens 21-25 29389973-7 2018 In addition, leptin, IL-6 and TNFalpha, at concentrations reflecting plasma concentrations in obese patients, decreased the anti-proliferative efficacy of 4-hydroxytamoxifen (a major active metabolite of Tx). hydroxytamoxifen 155-173 tumor necrosis factor Homo sapiens 30-38 27890927-8 2017 Moreover, 4-hydroxytamoxifen-induced activation of a JunB-ER fusion protein protected dexamethasone-sensitive MM cells against dexamethasone- and bortezomib-induced cytotoxicity. hydroxytamoxifen 10-28 jun B proto-oncogene Mus musculus 53-57 29416786-3 2018 MCF-7 cell growth was inhibited by 4-OH-TAM dose-dependently with IC50 of 29 muM. hydroxytamoxifen 35-43 latexin Homo sapiens 77-80 29416786-8 2018 These genes, except PGR and CCND1 which were down-regulated, were also up-regulated in ER+ MCF-7 cells by 4-OH-TAM. hydroxytamoxifen 106-114 progesterone receptor Homo sapiens 20-23 29416786-8 2018 These genes, except PGR and CCND1 which were down-regulated, were also up-regulated in ER+ MCF-7 cells by 4-OH-TAM. hydroxytamoxifen 106-114 cyclin D1 Homo sapiens 28-33 28892037-6 2017 At postnatal day 1 (P1), we used 4-hydroxytamoxifen (4HT) to activate Cre recombinase activity from the Cdh5-CreErt2 transgene to cleave the floxed allele of Ccm2. hydroxytamoxifen 33-51 cadherin 5 Mus musculus 104-108 28892037-6 2017 At postnatal day 1 (P1), we used 4-hydroxytamoxifen (4HT) to activate Cre recombinase activity from the Cdh5-CreErt2 transgene to cleave the floxed allele of Ccm2. hydroxytamoxifen 33-51 cerebral cavernous malformation 2 Mus musculus 158-162 29245979-8 2017 CYP2D6 AS was the only variable that showed associations with both metabolite concentration and ratio: endoxifen (P < 0.001), NDM (P < 0.001), endoxifen/NDM (P < 0.001), NDM/tamoxifen (P < 0.001), and 4-OH tamoxifen/tamoxifen (P = 0.005). hydroxytamoxifen 213-227 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 0-6 28459113-4 2017 There is also evidence that some AhR-active pharmaceuticals, including tranilast, flutamide, hydroxytamoxifen and omeprazole or their derivatives, may be effective AhR-dependent anticancer agents for single or combination cancer chemotherapies for treatment of breast and pancreatic cancers. hydroxytamoxifen 93-109 aryl hydrocarbon receptor Homo sapiens 33-36 28276606-9 2017 Furthermore, 4-hydroxytamoxifen-mediated deletion of Smarca5 in the ex vivo cultures confirmed its requirement for erythroid cell proliferation. hydroxytamoxifen 13-31 SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 5 Homo sapiens 53-60 27991921-1 2017 To study ROCK2 activation in carcinogenesis, mice expressing 4-hydroxytamoxifen (4HT)-activated ROCK2 (K14.ROCKer) were crossed with mice expressing epidermal-activated rasHa (HK1.ras1205). hydroxytamoxifen 61-79 Rho-associated coiled-coil containing protein kinase 2 Mus musculus 96-101 28075498-2 2017 In this work we demonstrate for the first time that the commonly prescribed breast cancer therapeutic tamoxifen and its major metabolites, 4-hydroxytamoxifen and endoxifen, inhibit DAT function. hydroxytamoxifen 139-157 solute carrier family 6 member 3 Homo sapiens 181-184 28656802-4 2017 Western blot results also showed that 4-hydroxytamoxifen induced the activity of pro-apoptotic protein Caspase-3 in MCF-7 and SKBR3 cells, as evidenced by the cleavage of mammalian sterile 20-like kinase 1 substrate in a dose-dependent manner. hydroxytamoxifen 38-56 caspase 3 Homo sapiens 103-112 28137615-3 2017 We observed that 4-hydroxytamoxifen (4-OHT) increased pri-miR-29b-1 and pri-miR-29a transcription in CHO-K1 cells by activating endogenous estrogen receptor alpha (ERalpha). hydroxytamoxifen 17-35 microRNA 29b Cricetulus griseus 58-65 28137615-3 2017 We observed that 4-hydroxytamoxifen (4-OHT) increased pri-miR-29b-1 and pri-miR-29a transcription in CHO-K1 cells by activating endogenous estrogen receptor alpha (ERalpha). hydroxytamoxifen 17-35 microRNA 29a Cricetulus griseus 76-83 28137615-3 2017 We observed that 4-hydroxytamoxifen (4-OHT) increased pri-miR-29b-1 and pri-miR-29a transcription in CHO-K1 cells by activating endogenous estrogen receptor alpha (ERalpha). hydroxytamoxifen 17-35 estrogen receptor Cricetulus griseus 139-162 28166815-6 2017 ESR2-dependent regulation of SMR3A was supported by induced expression after stimulation with estradiol (E2), which was impaired by co-treatment with 4-Hydroxytamoxifen (TAM) or Fulvestrant, respectively. hydroxytamoxifen 150-168 estrogen receptor 2 Homo sapiens 0-4 28166815-6 2017 ESR2-dependent regulation of SMR3A was supported by induced expression after stimulation with estradiol (E2), which was impaired by co-treatment with 4-Hydroxytamoxifen (TAM) or Fulvestrant, respectively. hydroxytamoxifen 150-168 submaxillary gland androgen regulated protein 3A Homo sapiens 29-34 28459113-4 2017 There is also evidence that some AhR-active pharmaceuticals, including tranilast, flutamide, hydroxytamoxifen and omeprazole or their derivatives, may be effective AhR-dependent anticancer agents for single or combination cancer chemotherapies for treatment of breast and pancreatic cancers. hydroxytamoxifen 93-109 aryl hydrocarbon receptor Homo sapiens 164-167 27805390-0 2016 Insights of a Lead Optimization Study and Biological Evaluation of Novel 4-Hydroxytamoxifen Analogs as Estrogen-Related Receptor gamma (ERRgamma) Inverse Agonists. hydroxytamoxifen 73-91 estrogen related receptor gamma Homo sapiens 103-134 29599800-5 2017 Estrogen receptor- (ER-) positive T47D breast cancer cells are less sensitive to 4-hydroxytamoxifen (4-HT) treatment when cultured on the 3D porous scaffolds than in 2D cultures. hydroxytamoxifen 81-99 estrogen receptor 1 Homo sapiens 0-17 28849994-3 2017 The aim of the present study was to characterize single and combined antiestrogenic effects of the aryl hydrocarbon receptor (AhR)-agonist beta-naphthoflavone (BNF) and ER-antagonist 4-hydroxytamoxifen (OHT) on vitellogenin (Vtg) protein using primary rainbow trout (Oncorhynchus mykiss) hepatocytes. hydroxytamoxifen 183-201 estrogen receptor Oncorhynchus mykiss 169-171 28849994-3 2017 The aim of the present study was to characterize single and combined antiestrogenic effects of the aryl hydrocarbon receptor (AhR)-agonist beta-naphthoflavone (BNF) and ER-antagonist 4-hydroxytamoxifen (OHT) on vitellogenin (Vtg) protein using primary rainbow trout (Oncorhynchus mykiss) hepatocytes. hydroxytamoxifen 183-201 LOC100136735 Oncorhynchus mykiss 211-223 27924574-5 2017 These cells are then seeded in the absence or presence of 4-Hydroxytamoxifen (4-OHT), which activates the resident CreERT2 alleles resulting in elimination of the conditional K-Ras alleles and ultimately generating Rasless cells. hydroxytamoxifen 58-76 Kirsten rat sarcoma viral oncogene homolog Mus musculus 175-180 27882656-0 2016 Targeting Cancer with PCPA-Drug Conjugates: LSD1 Inhibition-Triggered Release of 4-Hydroxytamoxifen. hydroxytamoxifen 81-99 lysine demethylase 1A Homo sapiens 44-48 27519631-5 2016 In vitro 4-hydroxytamoxifen (OHT) induced cell proliferation and cell cycle promotion in type I and type II endometrial cancer cell lines, and this proliferation was blocked by GPER silencing. hydroxytamoxifen 9-27 G protein-coupled estrogen receptor 1 Homo sapiens 177-181 27264933-10 2017 4-OH tamoxifen also induced ERalpha homodimers but the subcellular localization of these ERalpha homodimers was predominant in cytoplasm instead of the nuclei induced by E2 treatment. hydroxytamoxifen 0-14 estrogen receptor 1 Homo sapiens 28-35 27264933-10 2017 4-OH tamoxifen also induced ERalpha homodimers but the subcellular localization of these ERalpha homodimers was predominant in cytoplasm instead of the nuclei induced by E2 treatment. hydroxytamoxifen 0-14 estrogen receptor 1 Homo sapiens 89-96 27157612-1 2016 Using a 4-hydroxytamoxifen (4OHT)-inducible, conditional Sos1-null mutation, we analyzed wild-type (WT), single Sos1-KO, Sos2-KO and double Sos1/2 KO primary mouse embryonic fibroblasts (MEF) with an aim at evaluating the functional specificity or redundancy of the Sos1 and Sos2 alleles at the cellular level. hydroxytamoxifen 8-26 SOS Ras/Rac guanine nucleotide exchange factor 1 Mus musculus 57-61 27775859-4 2016 This two-stage system of regulation allows for tissue-selective expression of the ROCK2:ER fusion protein, which then requires administration of estrogen analogues such as tamoxifen or 4-hydroxytamoxifen to elicit kinase activity. hydroxytamoxifen 185-203 Rho-associated coiled-coil containing protein kinase 2 Mus musculus 82-87 27198207-1 2016 Tamoxifen is metabolically activated to 4-hydroxytamoxifen and endoxifen by cytochrome P450 (CYP). hydroxytamoxifen 40-58 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 93-96 27198207-9 2016 Lower concentrations of endoxifen and endoxifen/4-hydroxytamoxifen ratios were seen with impaired CYP2C9 (P = .05 and P = .03, respectively) if patients had the same CYP2D6 phenotype and were not taking a CYP2D6 or CYP2C19 inhibitor. hydroxytamoxifen 48-66 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 98-104 27198207-9 2016 Lower concentrations of endoxifen and endoxifen/4-hydroxytamoxifen ratios were seen with impaired CYP2C9 (P = .05 and P = .03, respectively) if patients had the same CYP2D6 phenotype and were not taking a CYP2D6 or CYP2C19 inhibitor. hydroxytamoxifen 48-66 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 166-172 27198207-9 2016 Lower concentrations of endoxifen and endoxifen/4-hydroxytamoxifen ratios were seen with impaired CYP2C9 (P = .05 and P = .03, respectively) if patients had the same CYP2D6 phenotype and were not taking a CYP2D6 or CYP2C19 inhibitor. hydroxytamoxifen 48-66 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 205-211 27198207-9 2016 Lower concentrations of endoxifen and endoxifen/4-hydroxytamoxifen ratios were seen with impaired CYP2C9 (P = .05 and P = .03, respectively) if patients had the same CYP2D6 phenotype and were not taking a CYP2D6 or CYP2C19 inhibitor. hydroxytamoxifen 48-66 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 215-222 27198207-10 2016 Lower concentrations of 4-hydroxytamoxifen were seen for impaired CYP2C19 when ABCB1 SNP3435 was nonvariant (P = .04). hydroxytamoxifen 24-42 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 66-73 27198207-10 2016 Lower concentrations of 4-hydroxytamoxifen were seen for impaired CYP2C19 when ABCB1 SNP3435 was nonvariant (P = .04). hydroxytamoxifen 24-42 ATP binding cassette subfamily B member 1 Homo sapiens 79-84 27805390-0 2016 Insights of a Lead Optimization Study and Biological Evaluation of Novel 4-Hydroxytamoxifen Analogs as Estrogen-Related Receptor gamma (ERRgamma) Inverse Agonists. hydroxytamoxifen 73-91 estrogen related receptor gamma Homo sapiens 136-144 27618190-3 2016 Here we report the development of a Cas9 variant whose activity can be switched on and off in human cells with 4-hydroxytamoxifen (4-HT) by fusing the Cas9 enzyme with the hormone-binding domain of the estrogen receptor (ERT2). hydroxytamoxifen 111-129 estrogen receptor 1 Homo sapiens 202-219 27618190-3 2016 Here we report the development of a Cas9 variant whose activity can be switched on and off in human cells with 4-hydroxytamoxifen (4-HT) by fusing the Cas9 enzyme with the hormone-binding domain of the estrogen receptor (ERT2). hydroxytamoxifen 111-129 mitogen-activated protein kinase 3 Homo sapiens 221-225 26896706-2 2016 TAM is metabolized to the more active 4-hydroxytamoxifen (4-OH-TAM) and endoxifen by cytochrome P450 (CYP) mainly CYP2D6 and CYP3A4 enzymes. hydroxytamoxifen 38-56 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 85-100 27580485-1 2016 Molecular dynamics (MD) simulations have been used to model dynamic fluctuations in the structure of estrogen receptor-alpha (ER-alpha) upon binding to the natural agonist 17beta-estradiol (E2) and to the active metabolite of the breast cancer drug and antagonist, 4-hydroxytamoxifen (OHT). hydroxytamoxifen 265-283 estrogen receptor 1 Homo sapiens 101-124 27580485-1 2016 Molecular dynamics (MD) simulations have been used to model dynamic fluctuations in the structure of estrogen receptor-alpha (ER-alpha) upon binding to the natural agonist 17beta-estradiol (E2) and to the active metabolite of the breast cancer drug and antagonist, 4-hydroxytamoxifen (OHT). hydroxytamoxifen 265-283 estrogen receptor 1 Homo sapiens 126-134 27236015-0 2016 Synthesis and biological evaluation of novel 4-hydroxytamoxifen analogs as estrogen-related receptor gamma inverse agonists. hydroxytamoxifen 45-63 estrogen related receptor gamma Homo sapiens 75-106 27484880-7 2016 The IGF-I decrease correlated with endoxifen (P = 0.002) and 4-hydroxytamoxifen levels, demonstrating steeper decreases at higher metabolite levels (P = 0.001). hydroxytamoxifen 61-79 insulin like growth factor 1 Homo sapiens 4-9 26645832-8 2016 Treatment with either 4-Hydroxytamoxifen (OHT) or fulvestrant reduced hPYGO2 mRNA 10-fold and protein 5-10-fold within 4 h. Promoter analysis indicated an ER/SP1 binding site at nt -225 to -531 of hPYGO2. hydroxytamoxifen 22-40 pygopus family PHD finger 2 Homo sapiens 70-76 26645832-8 2016 Treatment with either 4-Hydroxytamoxifen (OHT) or fulvestrant reduced hPYGO2 mRNA 10-fold and protein 5-10-fold within 4 h. Promoter analysis indicated an ER/SP1 binding site at nt -225 to -531 of hPYGO2. hydroxytamoxifen 22-40 pygopus family PHD finger 2 Homo sapiens 197-203 27159275-9 2016 Moreover, reactivation of ERalpha expression by resveratrol combined with pterostilbene was found to sensitize ERalpha-dependent response to 17beta-estradiol (E2)-mediated cellular proliferation and antagonist 4-hydroxytamoxifen (4-OHT)-mediated inhibition of cellular proliferation in ERalpha-negative breast cancer cells. hydroxytamoxifen 210-228 estrogen receptor 1 Homo sapiens 26-33 27159275-9 2016 Moreover, reactivation of ERalpha expression by resveratrol combined with pterostilbene was found to sensitize ERalpha-dependent response to 17beta-estradiol (E2)-mediated cellular proliferation and antagonist 4-hydroxytamoxifen (4-OHT)-mediated inhibition of cellular proliferation in ERalpha-negative breast cancer cells. hydroxytamoxifen 210-228 estrogen receptor 1 Homo sapiens 111-118 27159275-9 2016 Moreover, reactivation of ERalpha expression by resveratrol combined with pterostilbene was found to sensitize ERalpha-dependent response to 17beta-estradiol (E2)-mediated cellular proliferation and antagonist 4-hydroxytamoxifen (4-OHT)-mediated inhibition of cellular proliferation in ERalpha-negative breast cancer cells. hydroxytamoxifen 210-228 estrogen receptor 1 Homo sapiens 111-118 27012210-0 2016 Curcumin suppresses 4-hydroxytamoxifen resistance in breast cancer cells by targeting SLUG/Hexokinase 2 pathway. hydroxytamoxifen 20-38 snail family transcriptional repressor 2 Homo sapiens 86-90 27012210-0 2016 Curcumin suppresses 4-hydroxytamoxifen resistance in breast cancer cells by targeting SLUG/Hexokinase 2 pathway. hydroxytamoxifen 20-38 hexokinase 2 Homo sapiens 91-103 27012210-3 2016 4-hydroxytamoxifen (4-OHT) promoted SLUG expression, which was blocked by curcumin. hydroxytamoxifen 0-18 snail family transcriptional repressor 2 Homo sapiens 36-40 26896706-2 2016 TAM is metabolized to the more active 4-hydroxytamoxifen (4-OH-TAM) and endoxifen by cytochrome P450 (CYP) mainly CYP2D6 and CYP3A4 enzymes. hydroxytamoxifen 38-56 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 102-105 26896706-2 2016 TAM is metabolized to the more active 4-hydroxytamoxifen (4-OH-TAM) and endoxifen by cytochrome P450 (CYP) mainly CYP2D6 and CYP3A4 enzymes. hydroxytamoxifen 38-56 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 114-120 26896706-2 2016 TAM is metabolized to the more active 4-hydroxytamoxifen (4-OH-TAM) and endoxifen by cytochrome P450 (CYP) mainly CYP2D6 and CYP3A4 enzymes. hydroxytamoxifen 38-56 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 125-131 26896706-2 2016 TAM is metabolized to the more active 4-hydroxytamoxifen (4-OH-TAM) and endoxifen by cytochrome P450 (CYP) mainly CYP2D6 and CYP3A4 enzymes. hydroxytamoxifen 58-66 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 125-131 27053216-4 2016 The QKI proteins were also required for adult myelin maintenance, because their ablation using PLP-CreERT resulted in hindlimb paralysis with immobility at ~30 d after 4-hydroxytamoxifen injection. hydroxytamoxifen 168-186 quaking, KH domain containing RNA binding Mus musculus 4-7 26692764-8 2015 ERalpha36, a splice variant from the ER1 locus, governs nongenomic membrane signaling pathways triggered by estrogen and confers 4-hydroxytamoxifen resistance in BC therapy. hydroxytamoxifen 129-147 MIER1 transcriptional regulator Homo sapiens 37-40 26898104-1 2016 BACKGROUND: Tamoxifen (TAM) is metabolized to the more active 4-hydroxytamoxifen by CYP2D6 enzyme. hydroxytamoxifen 62-80 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 84-90 27443928-6 2016 We will then outline in detail practical experimental steps for efficient transgenesis toward the creation of single-insertion transgenes and will introduce protocols for 4-hydroxytamoxifen-mediated CreERT2 induction to perform spatiotemporal lox transgene regulation experiments in zebrafish embryos. hydroxytamoxifen 171-189 lysyl oxidase a Danio rerio 243-246 26014809-0 2016 Sensitization of estrogen receptor-positive breast cancer cell lines to 4-hydroxytamoxifen by isothiocyanates present in cruciferous plants. hydroxytamoxifen 72-90 estrogen receptor 1 Homo sapiens 17-34 26418898-9 2016 Additionally, miR-146b overexpression inhibited cell proliferation and reversed chemoresistance to 4-hydroxytamoxifen in TAMR-MCF-7 cells. hydroxytamoxifen 99-117 microRNA 146b Homo sapiens 14-22 26708273-7 2016 Interestingly, 4-hydroxytamoxifen-resistant cells had significantly increased FOXA1 gene expression levels. hydroxytamoxifen 15-33 forkhead box A1 Homo sapiens 78-83 26446141-10 2016 The ratio of endoxifen to N-desmethyltamoxifen and the ratio of 4-hydroxytamoxifen to tamoxifen increased by 3.3- and ~1.5-fold, reflecting increased CYP2D6 activity. hydroxytamoxifen 64-82 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 150-156 27468577-10 2016 Further study showed that overexpres- sion of miR-124-3p could partially reverse 4-hydroxytamoxifen (4-OHT)-induced autophagy in breast cancer cells. hydroxytamoxifen 81-99 microRNA 124-3 Homo sapiens 46-56 26712520-6 2016 Furthermore, treatment with 4-hydroxytamoxifen (4-OHT) resulted in a dose-dependent decrease in PRP4K protein expression in MCF7 cells. hydroxytamoxifen 28-46 pre-mRNA processing factor 4B Homo sapiens 96-101 26304202-5 2015 Mouse embryonic fibroblasts (MEFs) were isolated from RAB6A(loxP/loxP) Rosa26-CreERT2 and incubated with 4-hydroxy tamoxifen, resulting in the efficient depletion of Rab6A and Rab6A". hydroxytamoxifen 105-124 RAB6A, member RAS oncogene family Mus musculus 54-59 26304202-5 2015 Mouse embryonic fibroblasts (MEFs) were isolated from RAB6A(loxP/loxP) Rosa26-CreERT2 and incubated with 4-hydroxy tamoxifen, resulting in the efficient depletion of Rab6A and Rab6A". hydroxytamoxifen 105-124 gene trap ROSA 26, Philippe Soriano Mus musculus 71-77 26304202-5 2015 Mouse embryonic fibroblasts (MEFs) were isolated from RAB6A(loxP/loxP) Rosa26-CreERT2 and incubated with 4-hydroxy tamoxifen, resulting in the efficient depletion of Rab6A and Rab6A". hydroxytamoxifen 105-124 RAB6A, member RAS oncogene family Mus musculus 166-171 26304202-5 2015 Mouse embryonic fibroblasts (MEFs) were isolated from RAB6A(loxP/loxP) Rosa26-CreERT2 and incubated with 4-hydroxy tamoxifen, resulting in the efficient depletion of Rab6A and Rab6A". hydroxytamoxifen 105-124 RAB6A, member RAS oncogene family Mus musculus 176-182 26299756-7 2015 Our studies also show that the gammaSyn protected conformation of ERalpha36 can effectively bind with both estradiol (E2) and 4-hydroxy tamoxifen (4-OHT). hydroxytamoxifen 126-145 synuclein gamma Homo sapiens 31-39 26071758-1 2015 As a prodrug, tamoxifen is activated by the P450 enzyme CYP2D6 that is responsible for converting it to the active metabolites, 4-hydroxytamoxifen and endoxifen. hydroxytamoxifen 128-146 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 56-62 25896350-5 2015 Organoids grown ex vivo from intestinal crypts of Vil-Scap(-) mice are readily killed when Scap is deleted by 4-hydroxytamoxifen. hydroxytamoxifen 110-128 villin 1 Mus musculus 50-53 25896350-5 2015 Organoids grown ex vivo from intestinal crypts of Vil-Scap(-) mice are readily killed when Scap is deleted by 4-hydroxytamoxifen. hydroxytamoxifen 110-128 SREBF chaperone Mus musculus 54-58 26238412-4 2015 To investigate HER4 expression and localization in response to estradiol (E2) and 4-hydroxytamoxifen (4-OHT) exposure, we also performed in vitro studies. hydroxytamoxifen 82-100 erb-b2 receptor tyrosine kinase 4 Homo sapiens 15-19 25819444-4 2015 Our results indicated that endoxifen, N-desmethyltamoxifen (N-desTAM), 4-hydroxytamoxifen (4-OHTAM), and tamoxifen-N-oxide were weak inhibitors of hSULT1E1 with Ki values ranging from 10 muM to 38 muM (i.e., over 1000 times higher than the 8.1 nM Km value for estradiol as substrate for the enzyme). hydroxytamoxifen 71-89 sulfotransferase family 1E member 1 Homo sapiens 147-155 25795461-0 2015 Induction of UDP-glucuronosyltransferase 2B15 gene expression by the major active metabolites of tamoxifen, 4-hydroxytamoxifen and endoxifen, in breast cancer cells. hydroxytamoxifen 108-126 UDP glucuronosyltransferase family 2 member B15 Homo sapiens 13-45 25819444-4 2015 Our results indicated that endoxifen, N-desmethyltamoxifen (N-desTAM), 4-hydroxytamoxifen (4-OHTAM), and tamoxifen-N-oxide were weak inhibitors of hSULT1E1 with Ki values ranging from 10 muM to 38 muM (i.e., over 1000 times higher than the 8.1 nM Km value for estradiol as substrate for the enzyme). hydroxytamoxifen 71-89 latexin Homo sapiens 187-190 25819444-4 2015 Our results indicated that endoxifen, N-desmethyltamoxifen (N-desTAM), 4-hydroxytamoxifen (4-OHTAM), and tamoxifen-N-oxide were weak inhibitors of hSULT1E1 with Ki values ranging from 10 muM to 38 muM (i.e., over 1000 times higher than the 8.1 nM Km value for estradiol as substrate for the enzyme). hydroxytamoxifen 71-89 latexin Homo sapiens 197-200 26022099-12 2015 Treatment of MCF-7 cells with 4-OH tamoxifen or siRNA silencing of estrogen receptor-alpha largely prevented 17beta-estradiol-induced SCD-1 expression. hydroxytamoxifen 30-44 stearoyl-CoA desaturase Homo sapiens 134-139 25900183-4 2015 TFF3 was induced by oestrogen, and its induction was inhibited by antioestrogens, tamoxifen, 4-hydroxytamoxifen and fulvestrant in oestrogen-responsive breast cancer cells. hydroxytamoxifen 93-111 trefoil factor 3 Homo sapiens 0-4 25499232-7 2015 We transduced these lines with an E47/estrogen receptor fusion construct that could be forced to homodimerize with 4-hydroxytamoxifen. hydroxytamoxifen 115-133 transcription factor 3 Homo sapiens 34-37 25091503-4 2015 CYP2C19 and CYP2C9 correlated with norendoxifen and (Z)-4-hydroxytamoxifen concentrations, respectively (P<0.001). hydroxytamoxifen 52-74 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 0-7 25091503-4 2015 CYP2C19 and CYP2C9 correlated with norendoxifen and (Z)-4-hydroxytamoxifen concentrations, respectively (P<0.001). hydroxytamoxifen 52-74 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 12-18 25734062-6 2015 Compared to the wild-type HBD, ER(TAM) has 1000-fold lower affinity for estrogen, yet remains responsive to activation by the synthetic steroid 4-hydroxytamoxifen (4-OHT). hydroxytamoxifen 144-162 estrogen receptor 1 (alpha) Mus musculus 31-33 25279503-2 2015 The goal of the present study was to determine how oestradiol (E2) and 4-hydroxytamoxifen (4-OHT) affect cellular bioenergetic function in MCF-7 and T47D ERalpha+ breast cancer cells in serum-replete compared with dextran-coated charcoal (DCC)-stripped foetal bovine serum (FBS)-containing medium ("serum-starved"). hydroxytamoxifen 71-89 estrogen receptor 1 Homo sapiens 154-161 25893704-0 2015 CYP3A4*22 is related to increased plasma levels of 4-hydroxytamoxifen and partially compensates for reduced CYP2D6 activation of tamoxifen. hydroxytamoxifen 51-69 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 25893704-1 2015 AIM: To evaluate the impact of CYP3A4*22 in the formation of endoxifen (EDF) and hydroxytamoxifen (HTF), under different CYP2D6 genotypic backgrounds. hydroxytamoxifen 81-97 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 31-37 25893704-1 2015 AIM: To evaluate the impact of CYP3A4*22 in the formation of endoxifen (EDF) and hydroxytamoxifen (HTF), under different CYP2D6 genotypic backgrounds. hydroxytamoxifen 99-102 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 31-37 25893704-5 2015 HTF and TAM levels were respectively 47 and 53% higher in CYP3A4*22 carriers compared with *1/*1 patients in the whole group. hydroxytamoxifen 0-3 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 58-64 25073551-1 2014 BACKGROUND AND PURPOSE: Tamoxifen is a prodrug that is metabolically activated by 4-hydroxylation to the potent primary metabolite 4-hydroxytamoxifen (4OHT) or via another primary metabolite N-desmethyltamoxifen (NDMTAM) to a biologically active secondary metabolite endoxifen through a cytochrome P450 2D6 variant system (CYP2D6). hydroxytamoxifen 131-149 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 287-306 25073551-1 2014 BACKGROUND AND PURPOSE: Tamoxifen is a prodrug that is metabolically activated by 4-hydroxylation to the potent primary metabolite 4-hydroxytamoxifen (4OHT) or via another primary metabolite N-desmethyltamoxifen (NDMTAM) to a biologically active secondary metabolite endoxifen through a cytochrome P450 2D6 variant system (CYP2D6). hydroxytamoxifen 131-149 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 323-329 25100862-4 2014 Notable in this regard is the observation here and in other studies that expression of anterior gradient homology 2 (AGR2), a known proto-oncogene and disulfide isomerase, was induced by both estrogen (17beta-estradiol, E2) and 4-hydroxytamoxifen (4OHT) in breast cancer cells. hydroxytamoxifen 228-246 anterior gradient 2, protein disulphide isomerase family member Homo sapiens 87-115 25100862-4 2014 Notable in this regard is the observation here and in other studies that expression of anterior gradient homology 2 (AGR2), a known proto-oncogene and disulfide isomerase, was induced by both estrogen (17beta-estradiol, E2) and 4-hydroxytamoxifen (4OHT) in breast cancer cells. hydroxytamoxifen 228-246 anterior gradient 2, protein disulphide isomerase family member Homo sapiens 117-121 25157097-7 2014 In the hSULT2A1-catalyzed sulfation of PREG, 4-hydroxytamoxifen (4-OHTAM) and N-desmethyltamoxifen (N-desTAM) exhibited Ki values of 12.7 and 9.8 muM, respectively, whereas corresponding Ki values of 19.4 and 17.2 muM were observed with DHEA as substrate. hydroxytamoxifen 45-63 sulfotransferase family 2A member 1 Homo sapiens 7-15 25157097-7 2014 In the hSULT2A1-catalyzed sulfation of PREG, 4-hydroxytamoxifen (4-OHTAM) and N-desmethyltamoxifen (N-desTAM) exhibited Ki values of 12.7 and 9.8 muM, respectively, whereas corresponding Ki values of 19.4 and 17.2 muM were observed with DHEA as substrate. hydroxytamoxifen 45-63 latexin Homo sapiens 146-149 25157097-7 2014 In the hSULT2A1-catalyzed sulfation of PREG, 4-hydroxytamoxifen (4-OHTAM) and N-desmethyltamoxifen (N-desTAM) exhibited Ki values of 12.7 and 9.8 muM, respectively, whereas corresponding Ki values of 19.4 and 17.2 muM were observed with DHEA as substrate. hydroxytamoxifen 45-63 latexin Homo sapiens 214-217 25258390-1 2014 BACKGROUND: Tamoxifen is metabolically activated via a CYP2D6 enzyme system to the more potent hydroxylated derivatives 4-hydroxytamoxifen and endoxifen. hydroxytamoxifen 120-138 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 55-61 25135431-6 2014 4-Hydroxytamoxifen (4-OHT) was given to label Lgr5-positive cells with RFP, for comparison to GFP-positive Lgr5-negative cells. hydroxytamoxifen 0-18 leucine rich repeat containing G protein-coupled receptor 5 Homo sapiens 46-50 25135431-6 2014 4-Hydroxytamoxifen (4-OHT) was given to label Lgr5-positive cells with RFP, for comparison to GFP-positive Lgr5-negative cells. hydroxytamoxifen 0-18 tripartite motif containing 27 Homo sapiens 71-74 24881593-5 2014 The steady-state plasma concentrations of TAM and its active metabolites EDX and 4-hydroxytamoxifen (OHTAM) in patients taking TAM are highly variable, reflecting genetic variants of CYP2D6 involved in TAM metabolism. hydroxytamoxifen 81-99 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 183-189 24482362-3 2014 In comparison with known bis-arylidene drugs, these compounds are at least three orders of magnitude more toxic than tamoxifen and 1.5-4-fold more toxic than 4-hydroxytamoxifen in ER+ MCF-7 cancer cells. hydroxytamoxifen 158-176 estrogen receptor 1 Homo sapiens 180-182 24590896-6 2014 Moreover, hydroxytamoxifen activation of an Akt-estrogen receptor construct blocked an increase in Mirk mRNA and protein. hydroxytamoxifen 10-26 AKT serine/threonine kinase 1 Homo sapiens 44-47 24590896-6 2014 Moreover, hydroxytamoxifen activation of an Akt-estrogen receptor construct blocked an increase in Mirk mRNA and protein. hydroxytamoxifen 10-26 dual specificity tyrosine phosphorylation regulated kinase 1B Homo sapiens 99-103 24066662-9 2014 However, application of 4-hydroxytamoxifen results in translocation of the fusion protein to the nucleus, where it binds to the Atoh1 enhancer, upregulates transcription and translation of endogenous ATOH1 and activates downstream Atoh1 signaling such as upregulation of the hair cell protein MYOSIN 7A. hydroxytamoxifen 24-42 atonal bHLH transcription factor 1 Homo sapiens 128-133 24701358-9 2014 4-Hydroxytamoxifen, alone or associated with triiodothyronine, modulated gene expression of TNFRSF9, BMP-6, and THRA, similar to triiodothyronine treatment. hydroxytamoxifen 0-18 TNF receptor superfamily member 9 Homo sapiens 92-99 24701358-9 2014 4-Hydroxytamoxifen, alone or associated with triiodothyronine, modulated gene expression of TNFRSF9, BMP-6, and THRA, similar to triiodothyronine treatment. hydroxytamoxifen 0-18 bone morphogenetic protein 6 Homo sapiens 101-106 24701358-9 2014 4-Hydroxytamoxifen, alone or associated with triiodothyronine, modulated gene expression of TNFRSF9, BMP-6, and THRA, similar to triiodothyronine treatment. hydroxytamoxifen 0-18 thyroid hormone receptor alpha Homo sapiens 112-116 24066662-9 2014 However, application of 4-hydroxytamoxifen results in translocation of the fusion protein to the nucleus, where it binds to the Atoh1 enhancer, upregulates transcription and translation of endogenous ATOH1 and activates downstream Atoh1 signaling such as upregulation of the hair cell protein MYOSIN 7A. hydroxytamoxifen 24-42 atonal bHLH transcription factor 1 Homo sapiens 200-205 24066662-9 2014 However, application of 4-hydroxytamoxifen results in translocation of the fusion protein to the nucleus, where it binds to the Atoh1 enhancer, upregulates transcription and translation of endogenous ATOH1 and activates downstream Atoh1 signaling such as upregulation of the hair cell protein MYOSIN 7A. hydroxytamoxifen 24-42 atonal bHLH transcription factor 1 Homo sapiens 231-236 24434530-2 2014 Tamoxifen is a mainly inactive prodrug, necessitating metabolism by the cytochrome P450 (CYP450) pathway, predominantly the Cytochrome P450 2D6 (CYP2D6), into the active metabolites 4-hydroxytamoxifen and, in particular, endoxifen to achieve its therapeutic effect. hydroxytamoxifen 182-200 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 124-143 24434530-2 2014 Tamoxifen is a mainly inactive prodrug, necessitating metabolism by the cytochrome P450 (CYP450) pathway, predominantly the Cytochrome P450 2D6 (CYP2D6), into the active metabolites 4-hydroxytamoxifen and, in particular, endoxifen to achieve its therapeutic effect. hydroxytamoxifen 182-200 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 145-151 23790951-5 2013 These results showed that the level of CCNE2 protein expression was specifically inhibited in luteolin-treated (5muM) TAM-R cells, either in the presence or absence of 4-OH-TAM (100nM). hydroxytamoxifen 168-176 cyclin E2 Homo sapiens 39-44 23881388-6 2013 Additionally, the effects of fulvestrant, 4-hydroxytamoxifen, or estrogen on estrogen receptor expression were not associated with TIMP1 levels. hydroxytamoxifen 42-60 estrogen receptor 1 Homo sapiens 77-94 23892277-2 2013 We reported that estradiol (E2) and 4-hydroxytamoxifen (4-OHT) stimulate NRF-1 transcription in an estrogen receptor alpha (ERalpha)- and ERbeta-dependent manner in human breast cancer cells. hydroxytamoxifen 36-54 estrogen receptor 2 Homo sapiens 138-144 23870655-5 2013 METHODS: K14-Raf:ER transgenic mice, in which the 4-hydroxytamoxifen (4OHT)-responsive mutant estrogen receptor ligand binding domain-Raf fusion gene is expressed under control of the keratin 14 promoter, were mated with epidermis-specific Stat3 null mice (K5-Cre.Stat3(flox/flox)). hydroxytamoxifen 50-68 zinc fingers and homeoboxes 2 Mus musculus 13-16 23870655-5 2013 METHODS: K14-Raf:ER transgenic mice, in which the 4-hydroxytamoxifen (4OHT)-responsive mutant estrogen receptor ligand binding domain-Raf fusion gene is expressed under control of the keratin 14 promoter, were mated with epidermis-specific Stat3 null mice (K5-Cre.Stat3(flox/flox)). hydroxytamoxifen 50-68 zinc fingers and homeoboxes 2 Mus musculus 134-137 23805908-4 2013 We initially observed that tamoxifen inhibited macrophage/foam cell formation, but the inhibition was attenuated when FABP4 expression was selectively inhibited by siRNA.We then observed that tamoxifen and 4-hydroxytamoxifen inhibited FABP4 protein expression in primary macrophages isolated from both the male and female wild-type mice, suggesting that the inhibition is sex-independent. hydroxytamoxifen 206-224 fatty acid binding protein 4, adipocyte Mus musculus 118-123 23805908-4 2013 We initially observed that tamoxifen inhibited macrophage/foam cell formation, but the inhibition was attenuated when FABP4 expression was selectively inhibited by siRNA.We then observed that tamoxifen and 4-hydroxytamoxifen inhibited FABP4 protein expression in primary macrophages isolated from both the male and female wild-type mice, suggesting that the inhibition is sex-independent. hydroxytamoxifen 206-224 fatty acid binding protein 4, adipocyte Mus musculus 235-240 23805908-5 2013 Tamoxifen and 4-hydroxytamoxifen inhibited macrophage FABP4 protein expression induced either by activation of GR (glucocorticoid receptor) or PPARgamma (peroxisome-proliferator-activated receptor gamma). hydroxytamoxifen 14-32 fatty acid binding protein 4, adipocyte Mus musculus 54-59 23805908-5 2013 Tamoxifen and 4-hydroxytamoxifen inhibited macrophage FABP4 protein expression induced either by activation of GR (glucocorticoid receptor) or PPARgamma (peroxisome-proliferator-activated receptor gamma). hydroxytamoxifen 14-32 nuclear receptor subfamily 3, group C, member 1 Mus musculus 111-113 23805908-5 2013 Tamoxifen and 4-hydroxytamoxifen inhibited macrophage FABP4 protein expression induced either by activation of GR (glucocorticoid receptor) or PPARgamma (peroxisome-proliferator-activated receptor gamma). hydroxytamoxifen 14-32 nuclear receptor subfamily 3, group C, member 1 Mus musculus 115-138 23805908-5 2013 Tamoxifen and 4-hydroxytamoxifen inhibited macrophage FABP4 protein expression induced either by activation of GR (glucocorticoid receptor) or PPARgamma (peroxisome-proliferator-activated receptor gamma). hydroxytamoxifen 14-32 peroxisome proliferator activated receptor gamma Mus musculus 143-152 23805908-5 2013 Tamoxifen and 4-hydroxytamoxifen inhibited macrophage FABP4 protein expression induced either by activation of GR (glucocorticoid receptor) or PPARgamma (peroxisome-proliferator-activated receptor gamma). hydroxytamoxifen 14-32 peroxisome proliferator activated receptor gamma Mus musculus 154-202 23805908-6 2013 Associated with the decreased protein expression, Fabp4 mRNA expression and promoter activity were also inhibited by tamoxifen and 4-hydroxytamoxifen, indicating transcriptional regulation. hydroxytamoxifen 131-149 fatty acid binding protein 4, adipocyte Mus musculus 50-55 23805908-7 2013 Analysis of promoter activity and EMSA/ChIP assays indicated that tamoxifen and 4-hydroxytamoxifen activated the nGRE (negative glucocorticoid regulatory element), but inhibited the PPRE (PPARgamma regulatory element) in the Fabp4 gene. hydroxytamoxifen 80-98 peroxisome proliferator activated receptor gamma Mus musculus 188-197 23805908-7 2013 Analysis of promoter activity and EMSA/ChIP assays indicated that tamoxifen and 4-hydroxytamoxifen activated the nGRE (negative glucocorticoid regulatory element), but inhibited the PPRE (PPARgamma regulatory element) in the Fabp4 gene. hydroxytamoxifen 80-98 fatty acid binding protein 4, adipocyte Mus musculus 225-230 23892277-2 2013 We reported that estradiol (E2) and 4-hydroxytamoxifen (4-OHT) stimulate NRF-1 transcription in an estrogen receptor alpha (ERalpha)- and ERbeta-dependent manner in human breast cancer cells. hydroxytamoxifen 36-54 nuclear respiratory factor 1 Homo sapiens 73-78 23892277-2 2013 We reported that estradiol (E2) and 4-hydroxytamoxifen (4-OHT) stimulate NRF-1 transcription in an estrogen receptor alpha (ERalpha)- and ERbeta-dependent manner in human breast cancer cells. hydroxytamoxifen 36-54 estrogen receptor 1 Homo sapiens 99-122 23892277-2 2013 We reported that estradiol (E2) and 4-hydroxytamoxifen (4-OHT) stimulate NRF-1 transcription in an estrogen receptor alpha (ERalpha)- and ERbeta-dependent manner in human breast cancer cells. hydroxytamoxifen 36-54 estrogen receptor 1 Homo sapiens 124-131 23991038-9 2013 Furthermore, 4-hydroxytamoxifen had different modes of action in breast cancer cell lines with high or low ZNF703 expression. hydroxytamoxifen 13-31 zinc finger protein 703 Homo sapiens 107-113 23874882-5 2013 Notch1 was conditionally deleted in adult Notch1(flox/flox), K14-Cre-ERT(+/-) mice using hydroxy-tamoxifen. hydroxytamoxifen 89-106 notch 1 Mus musculus 0-6 23811274-6 2013 Correspondingly, cells overexpressing CITED2 demonstrated reduced sensitivity to the growth inhibitory effects of the selective estrogen receptor modulator, 4-hydroxytamoxifen. hydroxytamoxifen 157-175 Cbp/p300 interacting transactivator with Glu/Asp rich carboxy-terminal domain 2 Homo sapiens 38-44 23811274-6 2013 Correspondingly, cells overexpressing CITED2 demonstrated reduced sensitivity to the growth inhibitory effects of the selective estrogen receptor modulator, 4-hydroxytamoxifen. hydroxytamoxifen 157-175 estrogen receptor 1 Homo sapiens 128-145 23770613-8 2013 Therefore, mice were fed a vitamin E-depleted diet for 6 weeks before endothelial deletion of Gpx4 was induced by 4-hydroxytamoxifen. hydroxytamoxifen 114-132 glutathione peroxidase 4 Mus musculus 94-98 23722551-0 2013 4-Hydroxytamoxifen induces autophagic death through K-Ras degradation. hydroxytamoxifen 0-18 KRAS proto-oncogene, GTPase Homo sapiens 52-57 23624423-0 2013 4-Hydroxytamoxifen-stimulated processing of cyclin E is mediated via G protein-coupled receptor 30 (GPR30) and accompanied by enhanced migration in MCF-7 breast cancer cells. hydroxytamoxifen 0-18 G protein-coupled estrogen receptor 1 Homo sapiens 69-98 23704208-5 2013 E2 elevated phosphorylation of c-Src, which was blocked by 4-hydroxytamoxifen (4-OHT), suggesting that E2 activated c-Src through the ER. hydroxytamoxifen 59-77 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 31-36 23704208-5 2013 E2 elevated phosphorylation of c-Src, which was blocked by 4-hydroxytamoxifen (4-OHT), suggesting that E2 activated c-Src through the ER. hydroxytamoxifen 59-77 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 116-121 23704208-5 2013 E2 elevated phosphorylation of c-Src, which was blocked by 4-hydroxytamoxifen (4-OHT), suggesting that E2 activated c-Src through the ER. hydroxytamoxifen 59-77 estrogen receptor 1 Homo sapiens 134-136 23624423-0 2013 4-Hydroxytamoxifen-stimulated processing of cyclin E is mediated via G protein-coupled receptor 30 (GPR30) and accompanied by enhanced migration in MCF-7 breast cancer cells. hydroxytamoxifen 0-18 G protein-coupled estrogen receptor 1 Homo sapiens 100-105 23760924-11 2013 Here, the ablation of Cx43 was achieved by the injection of 4-hydroxytamoxifen (4-OHT; Cx43(Cre-ER(T)/fl) + 4-OHT). hydroxytamoxifen 60-78 gap junction protein, alpha 1 Mus musculus 22-26 23760924-11 2013 Here, the ablation of Cx43 was achieved by the injection of 4-hydroxytamoxifen (4-OHT; Cx43(Cre-ER(T)/fl) + 4-OHT). hydroxytamoxifen 60-78 gap junction protein, alpha 1 Mus musculus 87-91 23781139-9 2013 CONCLUSION: CYP2D6*4/*4 genotype was inversely associated with 4-hydroxy tamoxifen and endoxifen levels. hydroxytamoxifen 63-82 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 12-18 23478097-6 2013 A pulmonary endothelial cell line in which the Bmpr2 gene deletion can be induced by 4-hydroxy tamoxifen was established. hydroxytamoxifen 85-104 bone morphogenetic protein receptor, type II (serine/threonine kinase) Mus musculus 47-52 23595215-3 2013 To answer this question we used Cx43(Cre-ER(T)/fl) mice, in which Cx43 expression is abolished after 4-hydroxytamoxifen (4-OHT) administration. hydroxytamoxifen 101-119 gap junction protein, alpha 1 Mus musculus 32-36 22658320-9 2012 However, blocking c-Src recovered ER expression and down-regulated HER2 which made Sk-Br-3 cells regain responsiveness to 4-hydroxytamoxifen. hydroxytamoxifen 122-140 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 18-23 23384448-7 2013 However, MPT was prevented by ANT ligands ATP, ADP, tamoxifen and 4-hydroxytamoxifen, implying that the MPT induction by acitretin is mediated by the ANT. hydroxytamoxifen 66-84 solute carrier family 25 member 6 Homo sapiens 150-153 23593342-2 2013 In contrast to the Selective Estrogen Receptor Modulators (SERMs) such as 4-hydroxytamoxifen that bind to estrogen receptor alpha (ERalpha) as antagonists or partial agonists, fulvestrant causes proteasomal degradation of ERalpha protein, shutting down the estrogen signaling to induce proliferation arrest and apoptosis of estrogen-dependent breast cancer cells. hydroxytamoxifen 74-92 estrogen receptor 1 Homo sapiens 106-129 23593342-2 2013 In contrast to the Selective Estrogen Receptor Modulators (SERMs) such as 4-hydroxytamoxifen that bind to estrogen receptor alpha (ERalpha) as antagonists or partial agonists, fulvestrant causes proteasomal degradation of ERalpha protein, shutting down the estrogen signaling to induce proliferation arrest and apoptosis of estrogen-dependent breast cancer cells. hydroxytamoxifen 74-92 estrogen receptor 1 Homo sapiens 131-138 23299318-6 2013 When mDPCET cells were treated with 4-hydroxytamoxifen, (ERT2)Cre(ERT2) translocated from the cytoplasm to the nucleus and caused the excision of SV40Tag-TK, which led to the reversion of mDPCETs. hydroxytamoxifen 36-54 mitogen-activated protein kinase 3 Mus musculus 57-61 23299318-6 2013 When mDPCET cells were treated with 4-hydroxytamoxifen, (ERT2)Cre(ERT2) translocated from the cytoplasm to the nucleus and caused the excision of SV40Tag-TK, which led to the reversion of mDPCETs. hydroxytamoxifen 36-54 mitogen-activated protein kinase 3 Mus musculus 66-70 22658320-9 2012 However, blocking c-Src recovered ER expression and down-regulated HER2 which made Sk-Br-3 cells regain responsiveness to 4-hydroxytamoxifen. hydroxytamoxifen 122-140 erb-b2 receptor tyrosine kinase 2 Homo sapiens 67-71 23074235-11 2012 The estrogen antagonist, hydroxytamoxifen, the active metabolite of tamoxifen, reduced IGF1R protein levels and both E2- and IGF-II-induced cell proliferation. hydroxytamoxifen 25-41 insulin like growth factor 1 receptor Homo sapiens 87-92 23074235-11 2012 The estrogen antagonist, hydroxytamoxifen, the active metabolite of tamoxifen, reduced IGF1R protein levels and both E2- and IGF-II-induced cell proliferation. hydroxytamoxifen 25-41 cystatin 12, pseudogene Homo sapiens 117-131 22476979-4 2012 The estrogen-induced FOXA1 upregulation was repressed by 4-hydroxytamoxifen treatment. hydroxytamoxifen 57-75 forkhead box A1 Homo sapiens 21-26 23024189-9 2012 In cultured cells, significantly increased numbers of genes with modified expression were detected after 48 h, compared to 24-h treatments with DPN or 4-hydroxytamoxifen, including the parathyroid-related genes CASR, VDR, JUN, CALR, and ORAI2. hydroxytamoxifen 151-169 calcium sensing receptor Homo sapiens 211-215 23024189-9 2012 In cultured cells, significantly increased numbers of genes with modified expression were detected after 48 h, compared to 24-h treatments with DPN or 4-hydroxytamoxifen, including the parathyroid-related genes CASR, VDR, JUN, CALR, and ORAI2. hydroxytamoxifen 151-169 vitamin D receptor Homo sapiens 217-220 23024189-9 2012 In cultured cells, significantly increased numbers of genes with modified expression were detected after 48 h, compared to 24-h treatments with DPN or 4-hydroxytamoxifen, including the parathyroid-related genes CASR, VDR, JUN, CALR, and ORAI2. hydroxytamoxifen 151-169 calreticulin Homo sapiens 227-231 23024189-9 2012 In cultured cells, significantly increased numbers of genes with modified expression were detected after 48 h, compared to 24-h treatments with DPN or 4-hydroxytamoxifen, including the parathyroid-related genes CASR, VDR, JUN, CALR, and ORAI2. hydroxytamoxifen 151-169 ORAI calcium release-activated calcium modulator 2 Homo sapiens 237-242 22158035-9 2012 Importantly, 4-OH tamoxifen (4-OHT), when used in combination with overexpressed CDK10 or Raf-1 inhibitor, increased cleaved PARP and DNA fragmentation to inhibit cologenic growth of MCF7 cells and Tamoxifen-resistant MCF7 cells, respectively. hydroxytamoxifen 13-27 cyclin dependent kinase 10 Homo sapiens 81-86 22158035-9 2012 Importantly, 4-OH tamoxifen (4-OHT), when used in combination with overexpressed CDK10 or Raf-1 inhibitor, increased cleaved PARP and DNA fragmentation to inhibit cologenic growth of MCF7 cells and Tamoxifen-resistant MCF7 cells, respectively. hydroxytamoxifen 13-27 Raf-1 proto-oncogene, serine/threonine kinase Homo sapiens 90-95 22158035-9 2012 Importantly, 4-OH tamoxifen (4-OHT), when used in combination with overexpressed CDK10 or Raf-1 inhibitor, increased cleaved PARP and DNA fragmentation to inhibit cologenic growth of MCF7 cells and Tamoxifen-resistant MCF7 cells, respectively. hydroxytamoxifen 13-27 collagen type XI alpha 2 chain Homo sapiens 125-129 22158035-9 2012 Importantly, 4-OH tamoxifen (4-OHT), when used in combination with overexpressed CDK10 or Raf-1 inhibitor, increased cleaved PARP and DNA fragmentation to inhibit cologenic growth of MCF7 cells and Tamoxifen-resistant MCF7 cells, respectively. hydroxytamoxifen 29-34 cyclin dependent kinase 10 Homo sapiens 81-86 22158035-9 2012 Importantly, 4-OH tamoxifen (4-OHT), when used in combination with overexpressed CDK10 or Raf-1 inhibitor, increased cleaved PARP and DNA fragmentation to inhibit cologenic growth of MCF7 cells and Tamoxifen-resistant MCF7 cells, respectively. hydroxytamoxifen 29-34 Raf-1 proto-oncogene, serine/threonine kinase Homo sapiens 90-95 22158035-9 2012 Importantly, 4-OH tamoxifen (4-OHT), when used in combination with overexpressed CDK10 or Raf-1 inhibitor, increased cleaved PARP and DNA fragmentation to inhibit cologenic growth of MCF7 cells and Tamoxifen-resistant MCF7 cells, respectively. hydroxytamoxifen 29-34 collagen type XI alpha 2 chain Homo sapiens 125-129 22879383-1 2012 Leflunomide, flutamide, nimodipine, mexiletine, sulindac, tranilast, 4-hydroxytamoxifen, and omeprazole are pharmaceuticals previously characterized as aryl hydrocarbon receptor (AHR) agonists in various cell lines and animal models. hydroxytamoxifen 69-87 aryl hydrocarbon receptor Homo sapiens 152-177 22879383-1 2012 Leflunomide, flutamide, nimodipine, mexiletine, sulindac, tranilast, 4-hydroxytamoxifen, and omeprazole are pharmaceuticals previously characterized as aryl hydrocarbon receptor (AHR) agonists in various cell lines and animal models. hydroxytamoxifen 69-87 aryl hydrocarbon receptor Homo sapiens 179-182 22332638-4 2012 This study reports a destabilizing domain system based on the ligand binding domain of the estrogen receptor that can be regulated by one of two synthetic ligands, CMP8 or 4-hydroxytamoxifen. hydroxytamoxifen 172-190 estrogen receptor 1 Homo sapiens 91-108 22281313-6 2012 Hydroxytamoxifen, an antagonist of both estrogen-related receptor gamma (ERRgamma) and estrogen receptors (ERalpha/ERbeta), blocked the BPA-induced enhancement of the spine density. hydroxytamoxifen 0-16 estrogen receptor 1 Rattus norvegicus 107-114 22281313-6 2012 Hydroxytamoxifen, an antagonist of both estrogen-related receptor gamma (ERRgamma) and estrogen receptors (ERalpha/ERbeta), blocked the BPA-induced enhancement of the spine density. hydroxytamoxifen 0-16 estrogen receptor 2 Rattus norvegicus 115-121 22290080-16 2012 Transactivation of the EGF-receptor was similarly increased in both cell lines by 17beta-estradiol and 4-hydroxytamoxifen. hydroxytamoxifen 103-121 epidermal growth factor receptor Homo sapiens 23-35 22708928-1 2012 BACKGROUND: Sulfotransferase 1A1 (SULT1A1) participates in the elimination of 4-hydroxy-tamoxifen (4-OH-TAM), which is one of the major active metabolites of tamoxifen (TAM). hydroxytamoxifen 99-107 sulfotransferase family 1A member 1 Homo sapiens 12-32 22708928-1 2012 BACKGROUND: Sulfotransferase 1A1 (SULT1A1) participates in the elimination of 4-hydroxy-tamoxifen (4-OH-TAM), which is one of the major active metabolites of tamoxifen (TAM). hydroxytamoxifen 99-107 sulfotransferase family 1A member 1 Homo sapiens 34-41 22425989-0 2012 The G protein-coupled receptor GPR30 mediates the proliferative and invasive effects induced by hydroxytamoxifen in endometrial cancer cells. hydroxytamoxifen 96-112 G protein-coupled estrogen receptor 1 Homo sapiens 31-36 22105178-4 2012 We report that 17beta-estradiol (E(2)), 4-hydroxytamoxifen (4-OHT), and raloxifene increased NRF-1 transcription in HUVECs in an ER-dependent manner. hydroxytamoxifen 40-58 nuclear respiratory factor 1 Homo sapiens 93-98 22429491-6 2012 RESULTS: IGF-1, at physiologically relevant levels, blocked the cytotoxic action(s) of the antiestrogens 4-hydroxytamoxifen (4-OHT) and tamoxifen (TAM) when used as single agents or in combination with the antiprogestin MIF. hydroxytamoxifen 105-123 insulin like growth factor 1 Homo sapiens 9-14 22059479-3 2012 Upon 4-hydroxytamoxifen treatment, the ER(T2) fusion proteins with IL-1 receptor-associated kinase (IRAK)1 and IRAK4 elicited specific activation of a reporter gene for the post-transcriptional regulation of IkappaB-zeta. hydroxytamoxifen 5-23 interleukin 1 receptor associated kinase 1 Homo sapiens 67-106 22611478-6 2012 MCF-7 breast cancer cells treated with UpHT showed decreased proliferation upon co-incubation with RNase 1, consistent with the release of the active drug-4-hydroxytamoxifen. hydroxytamoxifen 155-173 ribonuclease A family member 1, pancreatic Homo sapiens 99-106 21947681-1 2012 CYP2D6 is a key enzyme responsible for the metabolism of tamoxifen to active metabolites, endoxifen, and 4-hydroxytamoxifen. hydroxytamoxifen 105-123 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 0-6 21947681-2 2012 The breast cancer patients who are heterozygous and homozygous for decreased-function and null alleles of CYP2D6 showed lower plasma concentrations of endoxifen and 4-hydroxytamoxifen compared to patients with homozygous-wild-type allele, resulting in worse clinical outcome in tamoxifen therapy. hydroxytamoxifen 165-183 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 106-112 21947681-9 2012 Plasma 4-hydroxytamoxifen concentrations in the patients with CYP2D6*1/*10 and CYP2D6*10/*10 were also significantly increased to the similar levels of the CYP2D6*1/*1 patients according to the increasing tamoxifen dosages (P < 0.001). hydroxytamoxifen 7-25 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 62-68 21947681-9 2012 Plasma 4-hydroxytamoxifen concentrations in the patients with CYP2D6*1/*10 and CYP2D6*10/*10 were also significantly increased to the similar levels of the CYP2D6*1/*1 patients according to the increasing tamoxifen dosages (P < 0.001). hydroxytamoxifen 7-25 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 79-85 21947681-9 2012 Plasma 4-hydroxytamoxifen concentrations in the patients with CYP2D6*1/*10 and CYP2D6*10/*10 were also significantly increased to the similar levels of the CYP2D6*1/*1 patients according to the increasing tamoxifen dosages (P < 0.001). hydroxytamoxifen 7-25 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 79-85 22041137-2 2012 Tamoxifen requires metabolic activation by cytochrome P450 (CYP) enzymes for formation of active metabolites, 4-hydroxytamoxifen and endoxifen, which have 30- to 100-fold greater affinity to the estrogen receptor and the potency to suppress estrogen-dependent breast cancer cell proliferation. hydroxytamoxifen 110-128 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 43-58 22041137-2 2012 Tamoxifen requires metabolic activation by cytochrome P450 (CYP) enzymes for formation of active metabolites, 4-hydroxytamoxifen and endoxifen, which have 30- to 100-fold greater affinity to the estrogen receptor and the potency to suppress estrogen-dependent breast cancer cell proliferation. hydroxytamoxifen 110-128 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 60-63 22059479-3 2012 Upon 4-hydroxytamoxifen treatment, the ER(T2) fusion proteins with IL-1 receptor-associated kinase (IRAK)1 and IRAK4 elicited specific activation of a reporter gene for the post-transcriptional regulation of IkappaB-zeta. hydroxytamoxifen 5-23 interleukin 1 receptor associated kinase 4 Homo sapiens 111-116 22059479-3 2012 Upon 4-hydroxytamoxifen treatment, the ER(T2) fusion proteins with IL-1 receptor-associated kinase (IRAK)1 and IRAK4 elicited specific activation of a reporter gene for the post-transcriptional regulation of IkappaB-zeta. hydroxytamoxifen 5-23 NFKB inhibitor zeta Homo sapiens 208-220 23056320-3 2012 To explore the mechanisms underpinning KLF1 action at the gene loci regulating the first 3 steps in this process, we have exploited the K1-ERp erythroid cell line, in which KLF1 translocates rapidly to the nucleus in response to treatment with 4-OH-Tamoxifen (4-OHT). hydroxytamoxifen 260-265 Kruppel like factor 1 Homo sapiens 39-43 23251571-2 2012 In these cells, the ER-E2F1 fusion protein is expressed in the cytosol; the addition of 4-hydroxytamoxifen (OHT) induces its translocation to the nucleus and activation of E2F1target genes. hydroxytamoxifen 88-106 E2F transcription factor 1 Homo sapiens 23-27 21777996-0 2011 Locating the binding sites of anticancer tamoxifen and its metabolites 4-hydroxytamoxifen and endoxifen on bovine serum albumin. hydroxytamoxifen 71-89 albumin Homo sapiens 114-127 22295107-5 2012 The treatment with estradiol (E2), anti-estrogenic agents 4-hydroxytamoxifen and ICI 182780, ERbeta specific ligand DPN and GPR30 agonist G1 led to a rapid activation of p-ERK1/2, suggesting the involvement of ERalpha36, ERbeta and GPR30 in the non-genomic signaling pathway in these cells. hydroxytamoxifen 58-76 mitogen-activated protein kinase 3 Homo sapiens 172-178 22295107-5 2012 The treatment with estradiol (E2), anti-estrogenic agents 4-hydroxytamoxifen and ICI 182780, ERbeta specific ligand DPN and GPR30 agonist G1 led to a rapid activation of p-ERK1/2, suggesting the involvement of ERalpha36, ERbeta and GPR30 in the non-genomic signaling pathway in these cells. hydroxytamoxifen 58-76 estrogen receptor 2 Homo sapiens 221-227 22295107-5 2012 The treatment with estradiol (E2), anti-estrogenic agents 4-hydroxytamoxifen and ICI 182780, ERbeta specific ligand DPN and GPR30 agonist G1 led to a rapid activation of p-ERK1/2, suggesting the involvement of ERalpha36, ERbeta and GPR30 in the non-genomic signaling pathway in these cells. hydroxytamoxifen 58-76 G protein-coupled estrogen receptor 1 Homo sapiens 232-237 21840388-6 2011 RESULTS: In ERalpha-positive MCF-7 cells, annonacin (half-effective dose ED(50) = 0.31 muM) and 4-hydroxytamoxifen (ED(50) = 1.13 muM) decreased cell survival whereas annonacin (0.5-1 muM) increased cell death at 48 h. Annonacin and 4-hydroxytamoxifen were additive in inhibiting cell survival. hydroxytamoxifen 96-114 latexin Homo sapiens 130-133 21840388-6 2011 RESULTS: In ERalpha-positive MCF-7 cells, annonacin (half-effective dose ED(50) = 0.31 muM) and 4-hydroxytamoxifen (ED(50) = 1.13 muM) decreased cell survival whereas annonacin (0.5-1 muM) increased cell death at 48 h. Annonacin and 4-hydroxytamoxifen were additive in inhibiting cell survival. hydroxytamoxifen 96-114 latexin Homo sapiens 130-133 21820658-0 2011 Induction of macrophage scavenger receptor type BI expression by tamoxifen and 4-hydroxytamoxifen. hydroxytamoxifen 79-97 scavenger receptor class B, member 1 Mus musculus 24-50 21820658-5 2011 METHODS AND RESULTS: In this study, we investigated the effect of tamoxifen and 4-hydroxytamoxifen on macrophage SR-BI expression. hydroxytamoxifen 80-98 scavenger receptor class B, member 1 Mus musculus 113-118 21820658-6 2011 Macrophage cell lines and peritoneal macrophages isolated from wild-type mice were used to determine changes in SR-BI mRNA and protein expression in response to tamoxifen and 4-hydroxytamoxifen. hydroxytamoxifen 175-193 scavenger receptor class B, member 1 Mus musculus 112-117 21820658-7 2011 We observed that tamoxifen and 4-hydroxytamoxifen increased SR-BI protein expression in a macrophage cell line derived from female mice (J774 cells) but not in a line derived from male mice (RAW cells). hydroxytamoxifen 31-49 scavenger receptor class B, member 1 Mus musculus 60-65 21820658-9 2011 Thus, the induction of macrophage SR-BI expression by tamoxifen and 4-hydroxytamoxifen is sex-dependent. hydroxytamoxifen 68-86 scavenger receptor class B, member 1 Mus musculus 34-39 21820658-14 2011 CONCLUSION: Our study demonstrates that tamoxifen and 4-hydroxytamoxifen induce macrophage SR-BI protein expression via a post-transcriptional mechanism. hydroxytamoxifen 54-72 scavenger receptor class B, member 1 Mus musculus 91-96 21900890-1 2011 Tamoxifen (Tam), the major drug for estrogen receptor (ER)-positive breast cancer, is converted to its active metabolites, Z- and Z"-endoxifen and 4-OH-Tam isomers, primarily by cytochrome P450 CYP2D6. hydroxytamoxifen 147-155 estrogen receptor 1 Homo sapiens 36-53 21900890-1 2011 Tamoxifen (Tam), the major drug for estrogen receptor (ER)-positive breast cancer, is converted to its active metabolites, Z- and Z"-endoxifen and 4-OH-Tam isomers, primarily by cytochrome P450 CYP2D6. hydroxytamoxifen 147-155 estrogen receptor 1 Homo sapiens 55-57 21898684-6 2011 Based on this rationale, we screened only 17 small molecules in reprogramming assays and discovered that the nonsteroidal anti-inflammatory drug Nabumetone and the anticancer drug 4-hydroxytamoxifen can generate iPSCs without Sox2. hydroxytamoxifen 180-198 SRY (sex determining region Y)-box 2 Mus musculus 226-230 21870861-0 2011 A mechanistic hypothesis for the cytochrome P450-catalyzed cis-trans isomerization of 4-hydroxytamoxifen: an unusual redox reaction. hydroxytamoxifen 86-104 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 33-48 21870861-1 2011 We provide a detailed description of the cis-trans isomerization of 4-hydroxytamoxifen/endoxifen catalyzed by several isoforms from the cytochrome P450 (CYP) superfamily, including CYP1B1, CYP2B6, and CYP2C19. hydroxytamoxifen 68-86 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 136-151 21870861-1 2011 We provide a detailed description of the cis-trans isomerization of 4-hydroxytamoxifen/endoxifen catalyzed by several isoforms from the cytochrome P450 (CYP) superfamily, including CYP1B1, CYP2B6, and CYP2C19. hydroxytamoxifen 68-86 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 153-156 21870861-1 2011 We provide a detailed description of the cis-trans isomerization of 4-hydroxytamoxifen/endoxifen catalyzed by several isoforms from the cytochrome P450 (CYP) superfamily, including CYP1B1, CYP2B6, and CYP2C19. hydroxytamoxifen 68-86 cytochrome P450 family 1 subfamily B member 1 Homo sapiens 181-187 21870861-1 2011 We provide a detailed description of the cis-trans isomerization of 4-hydroxytamoxifen/endoxifen catalyzed by several isoforms from the cytochrome P450 (CYP) superfamily, including CYP1B1, CYP2B6, and CYP2C19. hydroxytamoxifen 68-86 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 189-195 21870861-1 2011 We provide a detailed description of the cis-trans isomerization of 4-hydroxytamoxifen/endoxifen catalyzed by several isoforms from the cytochrome P450 (CYP) superfamily, including CYP1B1, CYP2B6, and CYP2C19. hydroxytamoxifen 68-86 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 201-208 21789304-3 2011 These 2-phenylquinoline hybrids effectively and selectively photo-degraded the target transcription factor, ER-alpha, which has a high affinity for estradiol and 4-hydroxytamoxifen. hydroxytamoxifen 162-180 estrogen receptor 1 Homo sapiens 108-116 21789304-6 2011 In contrast, 2-phenylquinoline-4-hydroxytamoxifen hybrid 3 inhibited growth of MCF-7 cells in the absence of photo-irradiation due to the antagonist effect of the 4-hydroxytamoxifen moiety against ER-alpha, and upon photo-irradiation significantly inhibited cell growth due to the dual antagonist effect of the 4-hydroxytamoxifen moiety and photo-degradation of ER-alpha. hydroxytamoxifen 31-49 estrogen receptor 1 Homo sapiens 197-205 21789304-6 2011 In contrast, 2-phenylquinoline-4-hydroxytamoxifen hybrid 3 inhibited growth of MCF-7 cells in the absence of photo-irradiation due to the antagonist effect of the 4-hydroxytamoxifen moiety against ER-alpha, and upon photo-irradiation significantly inhibited cell growth due to the dual antagonist effect of the 4-hydroxytamoxifen moiety and photo-degradation of ER-alpha. hydroxytamoxifen 31-49 estrogen receptor 1 Homo sapiens 362-370 21789304-6 2011 In contrast, 2-phenylquinoline-4-hydroxytamoxifen hybrid 3 inhibited growth of MCF-7 cells in the absence of photo-irradiation due to the antagonist effect of the 4-hydroxytamoxifen moiety against ER-alpha, and upon photo-irradiation significantly inhibited cell growth due to the dual antagonist effect of the 4-hydroxytamoxifen moiety and photo-degradation of ER-alpha. hydroxytamoxifen 163-181 estrogen receptor 1 Homo sapiens 197-205 21789304-6 2011 In contrast, 2-phenylquinoline-4-hydroxytamoxifen hybrid 3 inhibited growth of MCF-7 cells in the absence of photo-irradiation due to the antagonist effect of the 4-hydroxytamoxifen moiety against ER-alpha, and upon photo-irradiation significantly inhibited cell growth due to the dual antagonist effect of the 4-hydroxytamoxifen moiety and photo-degradation of ER-alpha. hydroxytamoxifen 163-181 estrogen receptor 1 Homo sapiens 362-370 21906315-0 2011 Upstream molecular signaling pathways of p27(Kip1) expression in human breast cancer cells in vitro: differential effects of 4-hydroxytamoxifen and deficiency of either D-(+)-glucose or L-leucine. hydroxytamoxifen 125-143 cyclin dependent kinase inhibitor 1B Homo sapiens 45-49 21906315-4 2011 We found that 4-hydroxytamoxifen - but not tamoxifen - up-regulated the expression of p27 using pathway #1 which consisted mainly of receptor tyrosine kinases and mTORC1. hydroxytamoxifen 14-32 dynactin subunit 6 Homo sapiens 86-89 21906315-4 2011 We found that 4-hydroxytamoxifen - but not tamoxifen - up-regulated the expression of p27 using pathway #1 which consisted mainly of receptor tyrosine kinases and mTORC1. hydroxytamoxifen 14-32 CREB regulated transcription coactivator 1 Mus musculus 163-169 21906315-8 2011 Furthermore, the results indicated that, although 4-hydroxytamoxifen used primarily pathway #1 to down-regulate the phosphorylation of 4E-BP1 and up-regulate the expression of p27, it also secondarily down-regulated the phosphorylation of S6K1. hydroxytamoxifen 50-68 eukaryotic translation initiation factor 4E binding protein 1 Homo sapiens 135-141 21906315-8 2011 Furthermore, the results indicated that, although 4-hydroxytamoxifen used primarily pathway #1 to down-regulate the phosphorylation of 4E-BP1 and up-regulate the expression of p27, it also secondarily down-regulated the phosphorylation of S6K1. hydroxytamoxifen 50-68 dynactin subunit 6 Homo sapiens 176-179 21906315-8 2011 Furthermore, the results indicated that, although 4-hydroxytamoxifen used primarily pathway #1 to down-regulate the phosphorylation of 4E-BP1 and up-regulate the expression of p27, it also secondarily down-regulated the phosphorylation of S6K1. hydroxytamoxifen 50-68 ribosomal protein S6 kinase B1 Homo sapiens 239-243 21777996-2 2011 We located the binding sites of tamoxifen, 4-hydroxytamoxifen and endoxifen on bovine serum albumin (BSA). hydroxytamoxifen 43-61 albumin Homo sapiens 86-99 21906462-4 2011 TAM is known to be metabolised to its active metabolites N-desmethyl TAM and 4-hydroxytamoxifen by a number of CYP450 enzymes, including CYP2D6, CYP3A4, CYP2C9, CYP2C19 and CYP2B6. hydroxytamoxifen 77-95 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 137-143 30780881-9 2011 This study found that cells harboring p53 mutations were more resistant to the cytotoxic effects of 4-hydroxytamoxifen than their p53 wild-type counterparts. hydroxytamoxifen 100-118 tumor protein p53 Homo sapiens 38-41 30780881-10 2011 Furthermore, mutant p53 cells were actually stimulated by low concentrations of 4-hydroxytamoxifen, with evidence that this may be mediated through enhanced growth factor signaling. hydroxytamoxifen 80-98 tumor protein p53 Homo sapiens 20-23 21906462-4 2011 TAM is known to be metabolised to its active metabolites N-desmethyl TAM and 4-hydroxytamoxifen by a number of CYP450 enzymes, including CYP2D6, CYP3A4, CYP2C9, CYP2C19 and CYP2B6. hydroxytamoxifen 77-95 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 153-159 21906462-4 2011 TAM is known to be metabolised to its active metabolites N-desmethyl TAM and 4-hydroxytamoxifen by a number of CYP450 enzymes, including CYP2D6, CYP3A4, CYP2C9, CYP2C19 and CYP2B6. hydroxytamoxifen 77-95 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 161-168 21906462-4 2011 TAM is known to be metabolised to its active metabolites N-desmethyl TAM and 4-hydroxytamoxifen by a number of CYP450 enzymes, including CYP2D6, CYP3A4, CYP2C9, CYP2C19 and CYP2B6. hydroxytamoxifen 77-95 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 173-179 21056929-8 2011 The inhibitory effects of E(2), genistein and daidzein on CRE-mediated transcription activity were enhanced by estrogen receptor (ER) alpha overexpression in MG-63 cells, which could be blocked by nonselective ER antagonists ICI182780, 4-OH tamoxifen and specific ERalpha antagonist MPP. hydroxytamoxifen 236-250 estrogen receptor 1 Homo sapiens 111-139 21056929-9 2011 Genistein and daidzein, but not E(2) treatment, caused a significant decrease in CRE-mediated transcription activity in ERbeta-transfected MG-63 cells, which could be blocked by ICI182780, 4-OH tamoxifen and the selective ERbeta antagonist (R,R)-5,11-diethyl-5.6,11,12-tetradro-2,8-chrysenediol. hydroxytamoxifen 189-203 estrogen receptor 2 Homo sapiens 120-126 21378205-0 2011 P-glycoprotein (ABCB1) transports the primary active tamoxifen metabolites endoxifen and 4-hydroxytamoxifen and restricts their brain penetration. hydroxytamoxifen 89-107 phosphoglycolate phosphatase Mus musculus 0-14 21744342-5 2011 Here we establish an inducible oncogenic zebrafish cell model, in which oncogenic human Raf-1(DeltaRaf1) can be post-transcriptionally activated in zebrafish liver cells by administration of 4-hydroxytamoxifen (4HT). hydroxytamoxifen 191-209 Raf-1 proto-oncogene, serine/threonine kinase Homo sapiens 88-103 21727187-3 2011 We generated a conditional zebrafish model of T-ALL in which 4-hydroxytamoxifen (4HT) treatment induces MYC activation and disease, and withdrawal of 4HT results in T-ALL apoptosis and tumor regression. hydroxytamoxifen 61-79 MYC proto-oncogene, bHLH transcription factor a Danio rerio 104-107 21840388-10 2011 The combination of annonacin (0.1 muM) and 4-hydroxytamoxifen (1 muM) decreased Bcl-2 protein expression and ERalpha transcriptional activity more than annonacin (0.1 muM) did alone. hydroxytamoxifen 43-61 latexin Homo sapiens 65-68 21840388-10 2011 The combination of annonacin (0.1 muM) and 4-hydroxytamoxifen (1 muM) decreased Bcl-2 protein expression and ERalpha transcriptional activity more than annonacin (0.1 muM) did alone. hydroxytamoxifen 43-61 BCL2 apoptosis regulator Homo sapiens 80-85 21840388-10 2011 The combination of annonacin (0.1 muM) and 4-hydroxytamoxifen (1 muM) decreased Bcl-2 protein expression and ERalpha transcriptional activity more than annonacin (0.1 muM) did alone. hydroxytamoxifen 43-61 estrogen receptor 1 Homo sapiens 109-116 21840388-10 2011 The combination of annonacin (0.1 muM) and 4-hydroxytamoxifen (1 muM) decreased Bcl-2 protein expression and ERalpha transcriptional activity more than annonacin (0.1 muM) did alone. hydroxytamoxifen 43-61 latexin Homo sapiens 65-68 21840388-16 2011 Annonacin and 4-hydroxytamoxifen were additive in inhibiting cell survival and ERalpha transcriptional activity. hydroxytamoxifen 14-32 estrogen receptor 1 Homo sapiens 79-86 21525417-4 2011 On the administration of 4-hydroxytamoxifen (4-OHT), the Dppa3-MCM strains recombined the sequence flanked by the loxP elements (the floxed sequence) specifically in primordial germ cells as early as Embryonic Day (E) 7.0, and this recombination became robust after E9.5. hydroxytamoxifen 25-43 developmental pluripotency-associated 3 Mus musculus 57-62 21525417-4 2011 On the administration of 4-hydroxytamoxifen (4-OHT), the Dppa3-MCM strains recombined the sequence flanked by the loxP elements (the floxed sequence) specifically in primordial germ cells as early as Embryonic Day (E) 7.0, and this recombination became robust after E9.5. hydroxytamoxifen 25-43 APOBEC1 complementation factor Mus musculus 63-66 21439346-0 2011 Binding of antitumor tamoxifen and its metabolites 4-hydroxytamoxifen and endoxifen to human serum albumin. hydroxytamoxifen 51-69 albumin Homo sapiens 93-106 21439346-2 2011 The aim of this study was to examine the interaction of human serum albumin (HSA) with tamoxifen and its metabolites 4-hydroxytamoxifen and endoxifen at physiological conditions, using constant protein concentration and various drug contents. hydroxytamoxifen 117-135 albumin Homo sapiens 62-75 21378205-0 2011 P-glycoprotein (ABCB1) transports the primary active tamoxifen metabolites endoxifen and 4-hydroxytamoxifen and restricts their brain penetration. hydroxytamoxifen 89-107 ATP-binding cassette, sub-family B (MDR/TAP), member 1B Mus musculus 16-21 21087932-0 2011 Prolylcarboxypeptidase regulates proliferation, autophagy, and resistance to 4-hydroxytamoxifen-induced cytotoxicity in estrogen receptor-positive breast cancer cells. hydroxytamoxifen 77-95 prolylcarboxypeptidase Homo sapiens 0-22 21167227-4 2011 The Cre-ER protein could be induced to translocate from the cytoplasm to the nucleus by 4-hydroxytamoxifen to make SV40LTAg, hTERT and the Cre-ER gene itself excise without a secondary gene transfer. hydroxytamoxifen 88-106 telomerase reverse transcriptase Homo sapiens 125-130 21451508-4 2011 CYP2D6 genotypes explained 39 and 9% of the variability of steady-state concentrations of (Z)-endoxifen and (Z)-4-hydroxytamoxifen, respectively. hydroxytamoxifen 108-130 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 0-6 21372145-5 2011 ER antagonists, ICI 182,780 and 4-hydroxytamoxifen, prevent estradiol-induced stimulation of the endogenously expressed HSD17B7, suggesting that these inhibitors not only block estradiol action but also its production. hydroxytamoxifen 32-50 hydroxysteroid 17-beta dehydrogenase 7 Homo sapiens 120-127 21233487-3 2011 Here we report that 4-hydroxytamoxifen (4-OHT), with an EC(50) of ~1.7 nM, increases NRF-1 expression by recruiting ERbeta, cJun, cFos, CBP, and RNA polymerase II to and dismissing NCoR from the NRF1 promoter. hydroxytamoxifen 20-38 nuclear respiratory factor 1 Homo sapiens 85-90 21233487-3 2011 Here we report that 4-hydroxytamoxifen (4-OHT), with an EC(50) of ~1.7 nM, increases NRF-1 expression by recruiting ERbeta, cJun, cFos, CBP, and RNA polymerase II to and dismissing NCoR from the NRF1 promoter. hydroxytamoxifen 20-38 estrogen receptor 2 Homo sapiens 116-122 21233487-3 2011 Here we report that 4-hydroxytamoxifen (4-OHT), with an EC(50) of ~1.7 nM, increases NRF-1 expression by recruiting ERbeta, cJun, cFos, CBP, and RNA polymerase II to and dismissing NCoR from the NRF1 promoter. hydroxytamoxifen 20-38 Jun proto-oncogene, AP-1 transcription factor subunit Homo sapiens 124-128 21233487-3 2011 Here we report that 4-hydroxytamoxifen (4-OHT), with an EC(50) of ~1.7 nM, increases NRF-1 expression by recruiting ERbeta, cJun, cFos, CBP, and RNA polymerase II to and dismissing NCoR from the NRF1 promoter. hydroxytamoxifen 20-38 Fos proto-oncogene, AP-1 transcription factor subunit Homo sapiens 130-134 21233487-3 2011 Here we report that 4-hydroxytamoxifen (4-OHT), with an EC(50) of ~1.7 nM, increases NRF-1 expression by recruiting ERbeta, cJun, cFos, CBP, and RNA polymerase II to and dismissing NCoR from the NRF1 promoter. hydroxytamoxifen 20-38 CREB binding protein Homo sapiens 136-139 21233487-3 2011 Here we report that 4-hydroxytamoxifen (4-OHT), with an EC(50) of ~1.7 nM, increases NRF-1 expression by recruiting ERbeta, cJun, cFos, CBP, and RNA polymerase II to and dismissing NCoR from the NRF1 promoter. hydroxytamoxifen 20-38 nuclear receptor corepressor 1 Homo sapiens 181-185 21233487-3 2011 Here we report that 4-hydroxytamoxifen (4-OHT), with an EC(50) of ~1.7 nM, increases NRF-1 expression by recruiting ERbeta, cJun, cFos, CBP, and RNA polymerase II to and dismissing NCoR from the NRF1 promoter. hydroxytamoxifen 20-38 nuclear respiratory factor 1 Homo sapiens 195-199 21121684-0 2011 Synthetic and mechanistic pathways of cis and trans-hydroxytamoxifen drug derivatives reacting with Cp*Rh complexes that involve eta1-N, eta2-N,O, eta1-O, and eta6 bonding modes, via a novel N-pi rearrangement; relative binding affinities and computer docking studies of cis and trans-eta6-Cp*Rh-hydroxytamoxifen complexes at the estrogen, ERalpha and ERbeta receptors, and growth inhibition to breast cancer cells. hydroxytamoxifen 46-68 secreted phosphoprotein 1 Homo sapiens 129-133 21113150-7 2011 To this end, we engineered a knock-in allele encoding a 4-hydroxytamoxifen (4-OHT)-inducible telomerase reverse transcriptase-oestrogen receptor (TERT-ER) under transcriptional control of the endogenous TERT promoter. hydroxytamoxifen 56-74 telomerase reverse transcriptase Mus musculus 146-150 21113150-7 2011 To this end, we engineered a knock-in allele encoding a 4-hydroxytamoxifen (4-OHT)-inducible telomerase reverse transcriptase-oestrogen receptor (TERT-ER) under transcriptional control of the endogenous TERT promoter. hydroxytamoxifen 56-74 telomerase reverse transcriptase Mus musculus 203-207 21121684-0 2011 Synthetic and mechanistic pathways of cis and trans-hydroxytamoxifen drug derivatives reacting with Cp*Rh complexes that involve eta1-N, eta2-N,O, eta1-O, and eta6 bonding modes, via a novel N-pi rearrangement; relative binding affinities and computer docking studies of cis and trans-eta6-Cp*Rh-hydroxytamoxifen complexes at the estrogen, ERalpha and ERbeta receptors, and growth inhibition to breast cancer cells. hydroxytamoxifen 46-68 DNA polymerase iota Homo sapiens 137-141 21121684-0 2011 Synthetic and mechanistic pathways of cis and trans-hydroxytamoxifen drug derivatives reacting with Cp*Rh complexes that involve eta1-N, eta2-N,O, eta1-O, and eta6 bonding modes, via a novel N-pi rearrangement; relative binding affinities and computer docking studies of cis and trans-eta6-Cp*Rh-hydroxytamoxifen complexes at the estrogen, ERalpha and ERbeta receptors, and growth inhibition to breast cancer cells. hydroxytamoxifen 46-68 secreted phosphoprotein 1 Homo sapiens 147-151 21121684-0 2011 Synthetic and mechanistic pathways of cis and trans-hydroxytamoxifen drug derivatives reacting with Cp*Rh complexes that involve eta1-N, eta2-N,O, eta1-O, and eta6 bonding modes, via a novel N-pi rearrangement; relative binding affinities and computer docking studies of cis and trans-eta6-Cp*Rh-hydroxytamoxifen complexes at the estrogen, ERalpha and ERbeta receptors, and growth inhibition to breast cancer cells. hydroxytamoxifen 46-68 estrogen receptor 1 Homo sapiens 340-347 21121684-0 2011 Synthetic and mechanistic pathways of cis and trans-hydroxytamoxifen drug derivatives reacting with Cp*Rh complexes that involve eta1-N, eta2-N,O, eta1-O, and eta6 bonding modes, via a novel N-pi rearrangement; relative binding affinities and computer docking studies of cis and trans-eta6-Cp*Rh-hydroxytamoxifen complexes at the estrogen, ERalpha and ERbeta receptors, and growth inhibition to breast cancer cells. hydroxytamoxifen 46-68 estrogen receptor 2 Homo sapiens 352-358 21121684-0 2011 Synthetic and mechanistic pathways of cis and trans-hydroxytamoxifen drug derivatives reacting with Cp*Rh complexes that involve eta1-N, eta2-N,O, eta1-O, and eta6 bonding modes, via a novel N-pi rearrangement; relative binding affinities and computer docking studies of cis and trans-eta6-Cp*Rh-hydroxytamoxifen complexes at the estrogen, ERalpha and ERbeta receptors, and growth inhibition to breast cancer cells. hydroxytamoxifen 52-68 secreted phosphoprotein 1 Homo sapiens 129-133 21121684-0 2011 Synthetic and mechanistic pathways of cis and trans-hydroxytamoxifen drug derivatives reacting with Cp*Rh complexes that involve eta1-N, eta2-N,O, eta1-O, and eta6 bonding modes, via a novel N-pi rearrangement; relative binding affinities and computer docking studies of cis and trans-eta6-Cp*Rh-hydroxytamoxifen complexes at the estrogen, ERalpha and ERbeta receptors, and growth inhibition to breast cancer cells. hydroxytamoxifen 52-68 DNA polymerase iota Homo sapiens 137-141 21121684-0 2011 Synthetic and mechanistic pathways of cis and trans-hydroxytamoxifen drug derivatives reacting with Cp*Rh complexes that involve eta1-N, eta2-N,O, eta1-O, and eta6 bonding modes, via a novel N-pi rearrangement; relative binding affinities and computer docking studies of cis and trans-eta6-Cp*Rh-hydroxytamoxifen complexes at the estrogen, ERalpha and ERbeta receptors, and growth inhibition to breast cancer cells. hydroxytamoxifen 52-68 secreted phosphoprotein 1 Homo sapiens 147-151 21121684-0 2011 Synthetic and mechanistic pathways of cis and trans-hydroxytamoxifen drug derivatives reacting with Cp*Rh complexes that involve eta1-N, eta2-N,O, eta1-O, and eta6 bonding modes, via a novel N-pi rearrangement; relative binding affinities and computer docking studies of cis and trans-eta6-Cp*Rh-hydroxytamoxifen complexes at the estrogen, ERalpha and ERbeta receptors, and growth inhibition to breast cancer cells. hydroxytamoxifen 52-68 estrogen receptor 1 Homo sapiens 340-347 21121684-0 2011 Synthetic and mechanistic pathways of cis and trans-hydroxytamoxifen drug derivatives reacting with Cp*Rh complexes that involve eta1-N, eta2-N,O, eta1-O, and eta6 bonding modes, via a novel N-pi rearrangement; relative binding affinities and computer docking studies of cis and trans-eta6-Cp*Rh-hydroxytamoxifen complexes at the estrogen, ERalpha and ERbeta receptors, and growth inhibition to breast cancer cells. hydroxytamoxifen 52-68 estrogen receptor 2 Homo sapiens 352-358 21056663-2 2011 The synthetic estrogen receptor ligands 4-hydroxytamoxifen and diethylstilbestrol have, however, been shown to bind to and abolish the constitutive transcriptional activity of ERRgamma. hydroxytamoxifen 40-58 estrogen related receptor gamma Homo sapiens 176-184 21138979-4 2011 We further generated transgenic zebrafish that express ubiquitous 4-hydroxytamoxifen-controlled Cre recombinase activity from a ubi:cre(ERt2) transgene, as well as ubi:loxP-EGFP-loxP-mCherry (ubi:Switch) transgenics and show their use as a constitutive fluorescent lineage tracing reagent. hydroxytamoxifen 66-84 ubiquitin B Danio rerio 55-58 21138979-4 2011 We further generated transgenic zebrafish that express ubiquitous 4-hydroxytamoxifen-controlled Cre recombinase activity from a ubi:cre(ERt2) transgene, as well as ubi:loxP-EGFP-loxP-mCherry (ubi:Switch) transgenics and show their use as a constitutive fluorescent lineage tracing reagent. hydroxytamoxifen 66-84 ubiquitin B Danio rerio 128-131 21138979-4 2011 We further generated transgenic zebrafish that express ubiquitous 4-hydroxytamoxifen-controlled Cre recombinase activity from a ubi:cre(ERt2) transgene, as well as ubi:loxP-EGFP-loxP-mCherry (ubi:Switch) transgenics and show their use as a constitutive fluorescent lineage tracing reagent. hydroxytamoxifen 66-84 ubiquitin B Danio rerio 128-131 20951138-3 2011 METHODS: We investigated the effects of decreased sumoylation in adult mammals by generating mice with an inducible knockout (by injection of 4-hydroxytamoxifen) of the E2 enzyme Ubc9 (Ubc9fl/-/ROSA26-CreERT2 mice). hydroxytamoxifen 142-160 ubiquitin-conjugating enzyme E2I Mus musculus 179-183 20951138-6 2011 Ubc9fl/-/ROSA26-CreERT2 mice died within 6 days of 4-hydroxytamoxifen injection, losing 20% or less of their body weight and developing severe diarrhea on the second day after injection. hydroxytamoxifen 51-69 ubiquitin-conjugating enzyme E2I Mus musculus 0-4 21924163-6 2011 Lastly, we will introduce protocols for 4-hydroxytamoxifen-mediated CreER(T2) induction to perform spatio-temporal lox transgene regulation experiments in zebrafish embryos. hydroxytamoxifen 40-58 lysyl oxidase a Danio rerio 115-118 20543998-2 2010 Among the compounds, the diisopropyl and piperidinyl derivatives were found to be more active than 4-hydroxytamoxifen (HO-Tam), the active metabolite of tamoxifen based upon IC(50) values. hydroxytamoxifen 99-117 Myeloproliferative syndrome, transient (transient abnormal myelopoiesis) Homo sapiens 122-125 21041310-6 2010 TPSF also inhibits ERalpha-dependent growth in three cellular models for tamoxifen resistance; that is, 4-hydroxytamoxifen-stimulated MCF7ERalphaHA cells that overexpress ERalpha, fully tamoxifen-resistant BT474 cells that have amplified HER-2 and AIB1, and partially tamoxifen-resistant ZR-75 cells. hydroxytamoxifen 104-122 estrogen receptor 1 Homo sapiens 138-145 21086978-1 2010 Tamoxifen (Tam), the antiestrogen used to treat estrogen receptor-positive breast cancer is a pro-drug that is converted to its major active metabolites, endoxifen and 4-hydroxy-tamoxifen (4-OH-Tam) by various biotransformation enzymes of which cytochrome P450-2D6 (CYP2D6) is key. hydroxytamoxifen 189-197 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 245-264 21086978-1 2010 Tamoxifen (Tam), the antiestrogen used to treat estrogen receptor-positive breast cancer is a pro-drug that is converted to its major active metabolites, endoxifen and 4-hydroxy-tamoxifen (4-OH-Tam) by various biotransformation enzymes of which cytochrome P450-2D6 (CYP2D6) is key. hydroxytamoxifen 189-197 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 266-272 20926391-2 2010 Using a cell line in which deletion of the O-GlcNAc transferase (OGT; the enzyme that adds O-GlcNAc) can be induced by 4-hydroxytamoxifen, we screened the expression of 84 HSPs using quantitative reverse transcriptase PCR. hydroxytamoxifen 119-137 O-linked N-acetylglucosamine (GlcNAc) transferase Homo sapiens 43-63 20926391-2 2010 Using a cell line in which deletion of the O-GlcNAc transferase (OGT; the enzyme that adds O-GlcNAc) can be induced by 4-hydroxytamoxifen, we screened the expression of 84 HSPs using quantitative reverse transcriptase PCR. hydroxytamoxifen 119-137 O-linked N-acetylglucosamine (GlcNAc) transferase Homo sapiens 65-68 20808831-8 2010 Using MDA-MB-231 cells, in which FOXO3a activity can be induced by 4-hydroxytamoxifen, we showed that FOXO3a induction up-regulates PI3K-Akt activity and enhanced doxorubicin resistance. hydroxytamoxifen 67-85 forkhead box O3 Homo sapiens 33-39 20808831-8 2010 Using MDA-MB-231 cells, in which FOXO3a activity can be induced by 4-hydroxytamoxifen, we showed that FOXO3a induction up-regulates PI3K-Akt activity and enhanced doxorubicin resistance. hydroxytamoxifen 67-85 forkhead box O3 Homo sapiens 102-108 20808831-8 2010 Using MDA-MB-231 cells, in which FOXO3a activity can be induced by 4-hydroxytamoxifen, we showed that FOXO3a induction up-regulates PI3K-Akt activity and enhanced doxorubicin resistance. hydroxytamoxifen 67-85 AKT serine/threonine kinase 1 Homo sapiens 137-140 20542892-0 2010 Distinction of the binding modes for human nuclear receptor ERRgamma between bisphenol A and 4-hydroxytamoxifen. hydroxytamoxifen 93-111 estrogen related receptor gamma Homo sapiens 60-68 20542892-3 2010 BPA functions as an inverse-type antagonist of ERRgamma to retain its high basal constitutive activity by inhibiting the deactivating inverse agonist activity of 4-hydroxytamoxifen (4-OHT). hydroxytamoxifen 162-180 estrogen related receptor gamma Homo sapiens 47-55 20578288-7 2010 METHODS: K14-Raf:ER transgenic mice, in which the 4-hydroxytamoxifen (4OHT)-responsive mutant estrogen receptor (ER) ligand binding domain-Raf fusion gene was expressed under control of the keratin 14 promoter, were used to characterize inflammatory reactions induced by Raf expression in the epidermis. hydroxytamoxifen 50-68 estrogen receptor 1 (alpha) Mus musculus 94-111 20578288-7 2010 METHODS: K14-Raf:ER transgenic mice, in which the 4-hydroxytamoxifen (4OHT)-responsive mutant estrogen receptor (ER) ligand binding domain-Raf fusion gene was expressed under control of the keratin 14 promoter, were used to characterize inflammatory reactions induced by Raf expression in the epidermis. hydroxytamoxifen 50-68 estrogen receptor 1 (alpha) Mus musculus 113-115 20348541-6 2010 Differences in ERalpha complex composition with the ER ligands 17beta-estradiol, 4-hydroxytamoxifen, and ICI-182,780 could also be observed. hydroxytamoxifen 81-99 estrogen receptor 1 Homo sapiens 15-22 21143970-4 2010 We combined digitonin-based cell fractionation analyses with fluorescence and immuno-electron microscopy to determine the intracellular distribution of ligand-bound ERalpha and/or GFP-ERalpha.Using fluorescence- and electron microscopy we demonstrate that both endogenous ERalpha and GFP-ERalpha form numerous nuclear focal accumulations upon addition of agonist, 17beta-estradiol (E2), and pure antagonists (selective estrogen regulator disruptor; SERD), ICI 182,780 or RU58,668, while in the presence of partial antagonists (selective estrogen regulator modulator; SERM), 4-hydroxytamoxifen (OHT) or RU39,411, diffuse nuclear staining persisted.Digitonin based cell fractionation analyses confirmed that endogenous ERalpha and GFP-ERalpha predominantly reside in the nuclear fraction. hydroxytamoxifen 574-592 estrogen receptor 1 Homo sapiens 165-172 20479004-9 2010 Importantly, 4-hydroxy tamoxifen, when used in combination with silencing of Pin1 or LC-3, increased cleaved poly(ADP-ribose) polymerase and DNA fragmentation to inhibit cologenic growth of MCF7 cells. hydroxytamoxifen 13-32 peptidylprolyl cis/trans isomerase, NIMA-interacting 1 Homo sapiens 77-81 20479004-9 2010 Importantly, 4-hydroxy tamoxifen, when used in combination with silencing of Pin1 or LC-3, increased cleaved poly(ADP-ribose) polymerase and DNA fragmentation to inhibit cologenic growth of MCF7 cells. hydroxytamoxifen 13-32 microtubule associated protein 1 light chain 3 alpha Homo sapiens 85-89 20479004-9 2010 Importantly, 4-hydroxy tamoxifen, when used in combination with silencing of Pin1 or LC-3, increased cleaved poly(ADP-ribose) polymerase and DNA fragmentation to inhibit cologenic growth of MCF7 cells. hydroxytamoxifen 13-32 poly(ADP-ribose) polymerase 1 Homo sapiens 109-136 20387803-2 2010 Binding affinities of tethered full length human estrogen receptor alpha (ERalpha) with 17beta-estradiol, diethylstilbestrol, raloxifene, 4-hydroxytamoxifen, tamoxifen, and genistein were measured to be 100 (as reference), 100, 35, 21, 8, and 1.5, respectively. hydroxytamoxifen 138-156 estrogen receptor 1 Homo sapiens 49-72 20387803-2 2010 Binding affinities of tethered full length human estrogen receptor alpha (ERalpha) with 17beta-estradiol, diethylstilbestrol, raloxifene, 4-hydroxytamoxifen, tamoxifen, and genistein were measured to be 100 (as reference), 100, 35, 21, 8, and 1.5, respectively. hydroxytamoxifen 138-156 estrogen receptor 1 Homo sapiens 74-81 20026264-4 2010 In previous reports, 2.3-kb Col1a1-CreERT2 mice that expressed a Cre recombinase that is transiently inducible by 4-hydroxytamoxifen (4-OHT) were intercrossed with Rosa26R (R26R) reporter mice, which resulted in the production of Cre-expressing osteoblasts that were detected upon X-gal staining. hydroxytamoxifen 114-132 collagen, type I, alpha 1 Mus musculus 28-34 19427779-3 2010 Genistein- and equol-induced cell proliferation and S-phase entry were blocked by the ERalpha antagonists 4-hydroxytamoxifen and ICI 182,780 and by the mitogen-activated protein kinase 1/2 inhibitor U0126. hydroxytamoxifen 106-124 estrogen receptor 1 Homo sapiens 86-93 20116857-0 2010 A ferrocenyl derivative of hydroxytamoxifen elicits an estrogen receptor-independent mechanism of action in breast cancer cell lines. hydroxytamoxifen 27-43 estrogen receptor 1 Homo sapiens 55-72 20179196-5 2010 FGFR1-amplified cell lines show resistance to 4-hydroxytamoxifen, which is reversed by small interfering RNA silencing of FGFR1, suggesting that FGFR1 overexpression also promotes endocrine therapy resistance. hydroxytamoxifen 46-64 fibroblast growth factor receptor 1 Homo sapiens 0-5 19526339-2 2010 We used a novel approach to detect changes in the hormone-binding domain of ERalpha, based on the evidence that antiestrogens, such as 4-hydroxytamoxifen (ZOHT) and ICI 182,780, block the function of ERalpha by binding and folding the AF-2 transcriptional domain in a way that inhibits its association with coactivator proteins. hydroxytamoxifen 135-153 estrogen receptor 1 Homo sapiens 76-83 19526339-2 2010 We used a novel approach to detect changes in the hormone-binding domain of ERalpha, based on the evidence that antiestrogens, such as 4-hydroxytamoxifen (ZOHT) and ICI 182,780, block the function of ERalpha by binding and folding the AF-2 transcriptional domain in a way that inhibits its association with coactivator proteins. hydroxytamoxifen 135-153 estrogen receptor 1 Homo sapiens 200-207 20188517-5 2010 METHODS: K14-Raf:ER transgenic mice, in which the 4-hydroxytamoxifen (4OHT)-responsive mutant estrogen receptor (ER) ligand binding domain-Raf fusion gene was expressed under control of the keratin 14 promoter, were used to characterize inflammatory reactions induced by Raf expression in the epidermis. hydroxytamoxifen 50-68 estrogen receptor 1 (alpha) Mus musculus 94-111 20188517-5 2010 METHODS: K14-Raf:ER transgenic mice, in which the 4-hydroxytamoxifen (4OHT)-responsive mutant estrogen receptor (ER) ligand binding domain-Raf fusion gene was expressed under control of the keratin 14 promoter, were used to characterize inflammatory reactions induced by Raf expression in the epidermis. hydroxytamoxifen 50-68 estrogen receptor 1 (alpha) Mus musculus 113-115 20376192-3 2010 METHODOLOGY/PRINCIPAL FINDINGS: Using a virtual screening approach, 4-hydroxytamoxifen, the active metabolite of the anti-estrogen drug tamoxifen, was identified as a putative Hsp90 ligand. hydroxytamoxifen 68-86 heat shock protein 90 alpha family class A member 1 Homo sapiens 176-181 20376192-4 2010 Surprisingly, while all drugs targeting Hsp90 inhibit the chaperone ATPase activity, it was found experimentally that 4-hydroxytamoxifen and tamoxifen enhance rather than inhibit Hsp90 ATPase. hydroxytamoxifen 118-136 heat shock protein 90 alpha family class A member 1 Homo sapiens 179-184 20376192-4 2010 Surprisingly, while all drugs targeting Hsp90 inhibit the chaperone ATPase activity, it was found experimentally that 4-hydroxytamoxifen and tamoxifen enhance rather than inhibit Hsp90 ATPase. hydroxytamoxifen 118-136 dynein axonemal heavy chain 8 Homo sapiens 185-191 20544555-4 2010 It was found that some of the PBDE compounds with antiestrogenic activity extended into the channel of the estrogen receptor (ER), which is usually occupied by the alkylamine side chain of the ER antagonists raloxifene (RAL) and 4-hydroxytamoxifen (OHT), while most PBDE compounds without antiestrogenic activity adopted binding modes similar to that of ER agonist 17beta-estradiol (E2), located in the binding cavity and which did not protrude into the channel. hydroxytamoxifen 229-247 estrogen receptor 1 Homo sapiens 107-124 20544555-4 2010 It was found that some of the PBDE compounds with antiestrogenic activity extended into the channel of the estrogen receptor (ER), which is usually occupied by the alkylamine side chain of the ER antagonists raloxifene (RAL) and 4-hydroxytamoxifen (OHT), while most PBDE compounds without antiestrogenic activity adopted binding modes similar to that of ER agonist 17beta-estradiol (E2), located in the binding cavity and which did not protrude into the channel. hydroxytamoxifen 229-247 estrogen receptor 1 Homo sapiens 126-128 20124171-10 2010 CYP2D6 variants were associated with lower plasma levels of endoxifen and 4-hydroxytamoxifen (P = .0000043 and .00052), whereas no significant difference was found among ABCC2 genotype groups. hydroxytamoxifen 74-92 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 0-6 20018866-5 2010 Here, we established a dual-regulatable FL5.12 pre-B cell line in which myristoylated Akt is expressed under the control of doxycycline, and c-Myc, fused to the hormone-binding domain of the human estrogen receptor, is activated by 4-hydroxytamoxifen. hydroxytamoxifen 232-250 thymoma viral proto-oncogene 1 Mus musculus 86-89 20018866-5 2010 Here, we established a dual-regulatable FL5.12 pre-B cell line in which myristoylated Akt is expressed under the control of doxycycline, and c-Myc, fused to the hormone-binding domain of the human estrogen receptor, is activated by 4-hydroxytamoxifen. hydroxytamoxifen 232-250 estrogen receptor 1 Homo sapiens 197-214 20179196-5 2010 FGFR1-amplified cell lines show resistance to 4-hydroxytamoxifen, which is reversed by small interfering RNA silencing of FGFR1, suggesting that FGFR1 overexpression also promotes endocrine therapy resistance. hydroxytamoxifen 46-64 fibroblast growth factor receptor 1 Homo sapiens 122-127 20179196-5 2010 FGFR1-amplified cell lines show resistance to 4-hydroxytamoxifen, which is reversed by small interfering RNA silencing of FGFR1, suggesting that FGFR1 overexpression also promotes endocrine therapy resistance. hydroxytamoxifen 46-64 fibroblast growth factor receptor 1 Homo sapiens 122-127 20170512-0 2010 Upstream molecular signaling pathways of p27(Kip1) expression: effects of 4-hydroxytamoxifen, dexamethasone, and retinoic acids. hydroxytamoxifen 74-92 cyclin dependent kinase inhibitor 1B Homo sapiens 45-49 20170512-6 2010 1) The evidence indicated that 4-hydroxytamoxifen, dexamethasone, and various retinoic acids up-regulated expression of p27 in both estrogen receptor-positive and negative human breast cancer cells in vitro. hydroxytamoxifen 31-49 interferon alpha inducible protein 27 Homo sapiens 120-123 20170512-12 2010 CONCLUSIONS: 4-Hydroxytamoxifen and dexamethasone up-regulated translation initiation of p27 by down-regulating 4E-BP1 phosphorylated at Ser65 and this down-regulation seemed to be mediated by upstream RTKs/PI3K/Akt/AMPK/mTOR protein kinase signaling pathways. hydroxytamoxifen 13-31 interferon alpha inducible protein 27 Homo sapiens 89-92 20170512-12 2010 CONCLUSIONS: 4-Hydroxytamoxifen and dexamethasone up-regulated translation initiation of p27 by down-regulating 4E-BP1 phosphorylated at Ser65 and this down-regulation seemed to be mediated by upstream RTKs/PI3K/Akt/AMPK/mTOR protein kinase signaling pathways. hydroxytamoxifen 13-31 eukaryotic translation initiation factor 4E binding protein 1 Homo sapiens 112-118 20170512-12 2010 CONCLUSIONS: 4-Hydroxytamoxifen and dexamethasone up-regulated translation initiation of p27 by down-regulating 4E-BP1 phosphorylated at Ser65 and this down-regulation seemed to be mediated by upstream RTKs/PI3K/Akt/AMPK/mTOR protein kinase signaling pathways. hydroxytamoxifen 13-31 AKT serine/threonine kinase 1 Homo sapiens 212-215 19935718-0 2010 c-Jun activation is required for 4-hydroxytamoxifen-induced cell death in breast cancer cells. hydroxytamoxifen 33-51 Jun proto-oncogene, AP-1 transcription factor subunit Homo sapiens 0-5 20170512-12 2010 CONCLUSIONS: 4-Hydroxytamoxifen and dexamethasone up-regulated translation initiation of p27 by down-regulating 4E-BP1 phosphorylated at Ser65 and this down-regulation seemed to be mediated by upstream RTKs/PI3K/Akt/AMPK/mTOR protein kinase signaling pathways. hydroxytamoxifen 13-31 protein kinase AMP-activated catalytic subunit alpha 1 Homo sapiens 216-220 19935718-4 2010 We show that before DNA fragmentation and caspase 3/7 activation, cytotoxic concentrations of 4-hydroxytamoxifen (OHT) induced JNK-dependent phosphorylation of c-Jun at JNK sites earlier shown to regulate c-Jun-mediated apoptosis. hydroxytamoxifen 94-112 mitogen-activated protein kinase 8 Homo sapiens 127-130 19935718-4 2010 We show that before DNA fragmentation and caspase 3/7 activation, cytotoxic concentrations of 4-hydroxytamoxifen (OHT) induced JNK-dependent phosphorylation of c-Jun at JNK sites earlier shown to regulate c-Jun-mediated apoptosis. hydroxytamoxifen 94-112 Jun proto-oncogene, AP-1 transcription factor subunit Homo sapiens 160-165 20170512-12 2010 CONCLUSIONS: 4-Hydroxytamoxifen and dexamethasone up-regulated translation initiation of p27 by down-regulating 4E-BP1 phosphorylated at Ser65 and this down-regulation seemed to be mediated by upstream RTKs/PI3K/Akt/AMPK/mTOR protein kinase signaling pathways. hydroxytamoxifen 13-31 mechanistic target of rapamycin kinase Homo sapiens 221-225 19935718-4 2010 We show that before DNA fragmentation and caspase 3/7 activation, cytotoxic concentrations of 4-hydroxytamoxifen (OHT) induced JNK-dependent phosphorylation of c-Jun at JNK sites earlier shown to regulate c-Jun-mediated apoptosis. hydroxytamoxifen 94-112 mitogen-activated protein kinase 8 Homo sapiens 169-172 19935718-4 2010 We show that before DNA fragmentation and caspase 3/7 activation, cytotoxic concentrations of 4-hydroxytamoxifen (OHT) induced JNK-dependent phosphorylation of c-Jun at JNK sites earlier shown to regulate c-Jun-mediated apoptosis. hydroxytamoxifen 94-112 Jun proto-oncogene, AP-1 transcription factor subunit Homo sapiens 205-210 20086172-6 2010 In Ca(2+) mobilization studies, GPR30, but not ERalpha, mediated E(2)-induced Ca(2+) responses because E(2), 4-hydroxytamoxifen (activates GPR30), and G-1, but not DES, elicited cytosolic Ca(2+) increases not only in MCF-7 cells but also in ER-negative SKBr3 cells. hydroxytamoxifen 109-127 G protein-coupled estrogen receptor 1 Homo sapiens 139-144 21537383-0 2010 Expression of sulfotransferase isoform 1A1 (SULT1A1) in breast cancer cells significantly increases 4-hydroxytamoxifen-induced apoptosis. hydroxytamoxifen 100-118 sulfotransferase family 1A member 1 Homo sapiens 14-42 21537383-0 2010 Expression of sulfotransferase isoform 1A1 (SULT1A1) in breast cancer cells significantly increases 4-hydroxytamoxifen-induced apoptosis. hydroxytamoxifen 100-118 sulfotransferase family 1A member 1 Homo sapiens 44-51 21537383-1 2010 Previously, we reported a strong association of the high activity SULT1A1*1 allele and overall survival of patients receiving tamoxifen therapy, indicating that sulfation of 4-hydroxytamoxifen (4-OHT) via SULT1A1 may contribute to the therapeutic efficacy of tamoxifen treatment. hydroxytamoxifen 174-192 sulfotransferase family 1A member 1 Homo sapiens 66-73 21537383-1 2010 Previously, we reported a strong association of the high activity SULT1A1*1 allele and overall survival of patients receiving tamoxifen therapy, indicating that sulfation of 4-hydroxytamoxifen (4-OHT) via SULT1A1 may contribute to the therapeutic efficacy of tamoxifen treatment. hydroxytamoxifen 174-192 sulfotransferase family 1A member 1 Homo sapiens 205-212 19654266-11 2009 Pretreatment with PIP(2) significantly decreased the inhibition induced by tamoxifen, 4-hydroxytamoxifen, and raloxifene on Kir2.3 channels. hydroxytamoxifen 86-104 potassium inwardly rectifying channel subfamily J member 4 Homo sapiens 124-130 20086172-6 2010 In Ca(2+) mobilization studies, GPR30, but not ERalpha, mediated E(2)-induced Ca(2+) responses because E(2), 4-hydroxytamoxifen (activates GPR30), and G-1, but not DES, elicited cytosolic Ca(2+) increases not only in MCF-7 cells but also in ER-negative SKBr3 cells. hydroxytamoxifen 109-127 G protein-coupled estrogen receptor 1 Homo sapiens 32-37 19455332-3 2010 METHODS: Concurrent treatment with 4-OH-TAM and paclitaxel (Ptx) was investigated in estrogen receptor (ER)-positive breast cancer cells. hydroxytamoxifen 35-43 estrogen receptor 1 Homo sapiens 85-102 19455332-3 2010 METHODS: Concurrent treatment with 4-OH-TAM and paclitaxel (Ptx) was investigated in estrogen receptor (ER)-positive breast cancer cells. hydroxytamoxifen 35-43 estrogen receptor 1 Homo sapiens 104-106 19455332-5 2010 RESULTS: Concurrent treatment with 4-OH-TAM and Ptx yielded less than additive antitumor effects in ER-positive breast cancer cells, as observed with Dox in our previous study. hydroxytamoxifen 35-43 estrogen receptor 1 Homo sapiens 100-102 19455332-9 2010 Estrogen depletion down-regulated the level of expression of one of the molecules related to 5-FU resistance, thymidylate synthase, as observed with 4-OH-TAM in our previous study. hydroxytamoxifen 149-157 thymidylate synthetase Homo sapiens 110-130 19635455-0 2009 Implication of protein tyrosine phosphatase 1B in MCF-7 cell proliferation and resistance to 4-OH tamoxifen. hydroxytamoxifen 93-107 protein tyrosine phosphatase non-receptor type 1 Homo sapiens 15-46 19809024-1 2009 CONTEXT: The growth inhibitory effect of tamoxifen, which is used for the treatment of hormone receptor-positive breast cancer, is mediated by its metabolites, 4-hydroxytamoxifen and endoxifen. hydroxytamoxifen 160-178 nuclear receptor subfamily 4 group A member 1 Homo sapiens 87-103 19635455-6 2009 siRNA experiments showed that PTP1B, but not TC-PTP, is necessary for resistance to 4-OH tamoxifen. hydroxytamoxifen 84-98 protein tyrosine phosphatase non-receptor type 1 Homo sapiens 30-35 19706837-4 2009 Tamoxifen-resistant (TamR) MCF-7 cells selected by prolonged exposure to 4-hydroxytamoxifen, exhibited higher levels in SphK1 expression and activity, compared with the control cells. hydroxytamoxifen 73-91 sphingosine kinase 1 Homo sapiens 120-125 19574470-2 2009 CONTENT: Tamoxifen requires enzymatic activation by cytochrome P450 (CYP) enzymes for the formation of active metabolites 4-hydroxytamoxifen and endoxifen. hydroxytamoxifen 122-140 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 52-67 19574470-2 2009 CONTENT: Tamoxifen requires enzymatic activation by cytochrome P450 (CYP) enzymes for the formation of active metabolites 4-hydroxytamoxifen and endoxifen. hydroxytamoxifen 122-140 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 69-72 19553561-2 2009 To study mechanisms mediating effects of FoxO proteins on muscle wasting, FoxO1-estrogen receptor fusion proteins that are activated by treatment with 4-hydroxytamoxifen (4-OH-T) were stably transfected in C(2)C(12) skeletal myoblasts using the pBABE retroviral system and grown into multinucleated skeletal myotubes. hydroxytamoxifen 151-169 forkhead box O1 Homo sapiens 74-79 19661335-6 2009 To determine that the resistance to 4-OH-Tam-inducing cell killing after the KGF treatment was due to the inactivation of the apoptotic pathway, low molecular weight DNA was isolated from cells of different treatments and inter-nucleosomal DNA fragmentation was investigated. hydroxytamoxifen 36-44 fibroblast growth factor 7 Homo sapiens 77-80 20641702-6 2004 Active metabolites such as 4-hydroxytamoxifen and N-desmethyl-4-hydroxytamoxifen have 30-100 times more affinity with the ER than TAM itself. hydroxytamoxifen 27-45 Myeloproliferative syndrome, transient (transient abnormal myelopoiesis) Homo sapiens 130-133 19830888-2 2009 The purpose of this study was to investigate whether modulation of Src activity in endocrine-sensitive and endocrine-resistant breast cancer cells directly affected their phenotype and sensitivity to 4-hydroxy Tamoxifen (tamoxifen) and to determine whether Src activity in breast cancer tissue affected patient outcome. hydroxytamoxifen 200-219 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 67-70 19549820-6 2009 Fusion of EBF and Pax5 with the ligand-binding domain of ERalpha allowed for 4-hydroxytamoxifen-dependent, synergistic activation of mb-1 transcription in plasmacytoma cells. hydroxytamoxifen 77-95 EBF transcription factor 1 Homo sapiens 10-13 19549820-6 2009 Fusion of EBF and Pax5 with the ligand-binding domain of ERalpha allowed for 4-hydroxytamoxifen-dependent, synergistic activation of mb-1 transcription in plasmacytoma cells. hydroxytamoxifen 77-95 paired box 5 Homo sapiens 18-22 19549820-6 2009 Fusion of EBF and Pax5 with the ligand-binding domain of ERalpha allowed for 4-hydroxytamoxifen-dependent, synergistic activation of mb-1 transcription in plasmacytoma cells. hydroxytamoxifen 77-95 estrogen receptor 1 Homo sapiens 57-64 19391117-2 2009 We generated mice expressing 4-hydroxytamoxifen (4HT)-regulated human ROCK II (ROCKII:mER) under the transcriptional control of the cytokeratin14 (K14) promoter. hydroxytamoxifen 29-47 Rho associated coiled-coil containing protein kinase 2 Homo sapiens 70-77 19391117-2 2009 We generated mice expressing 4-hydroxytamoxifen (4HT)-regulated human ROCK II (ROCKII:mER) under the transcriptional control of the cytokeratin14 (K14) promoter. hydroxytamoxifen 29-47 keratin 14 Homo sapiens 132-145 19391117-2 2009 We generated mice expressing 4-hydroxytamoxifen (4HT)-regulated human ROCK II (ROCKII:mER) under the transcriptional control of the cytokeratin14 (K14) promoter. hydroxytamoxifen 29-47 keratin 14 Homo sapiens 147-150 19347870-1 2009 In previous studies on HeLa cells we demonstrated estrogen-responsiveness of the epidermal growth factor receptor (EGFR) gene, as 17beta-estradiol (E(2)) and selective estrogen receptor modulators (SERMs) genistein (G), daidzein (D), and 4-hydroxytamoxifen (4OH-T) modulated its transcription in a ligand- and estrogen receptor (ER) isoform-specific way. hydroxytamoxifen 238-256 epidermal growth factor receptor Homo sapiens 81-113 19347870-1 2009 In previous studies on HeLa cells we demonstrated estrogen-responsiveness of the epidermal growth factor receptor (EGFR) gene, as 17beta-estradiol (E(2)) and selective estrogen receptor modulators (SERMs) genistein (G), daidzein (D), and 4-hydroxytamoxifen (4OH-T) modulated its transcription in a ligand- and estrogen receptor (ER) isoform-specific way. hydroxytamoxifen 238-256 epidermal growth factor receptor Homo sapiens 115-119 19244109-2 2009 A major mode of metabolism of the major active metabolites of TAM, 4-OH-TAM and endoxifen, is by glucuronidation via the UDP-glucuronosyltransferase (UGT) family of enzymes. hydroxytamoxifen 67-75 UDP glucuronosyltransferase family 1 member A complex locus Homo sapiens 121-148 19661335-12 2009 In the cell proliferation assay, KGF maintained MCF-7 cell survival in the presence of 4-OH-Tam which could be blocked by LY. hydroxytamoxifen 87-95 fibroblast growth factor 7 Homo sapiens 33-36 19289494-5 2009 We show using a 4-hydroxytamoxifen-inducible Cre that the loss of PRMT1 in MEFs leads to a higher incidence of chromosome losses, gains, structural rearrangements, and polyploidy, as documented by spectral karyotyping. hydroxytamoxifen 16-34 protein arginine N-methyltransferase 1 Mus musculus 66-71 19179445-5 2009 MCF-7 cells exposed to PM but not Pre-M conditions exhibited up-regulation of basal epidermal growth factor (EGF) receptor (EGFR) levels, an effect exaggerated in cells exposed to 4-hydroxytamoxifen. hydroxytamoxifen 180-198 epidermal growth factor receptor Homo sapiens 84-122 19179445-5 2009 MCF-7 cells exposed to PM but not Pre-M conditions exhibited up-regulation of basal epidermal growth factor (EGF) receptor (EGFR) levels, an effect exaggerated in cells exposed to 4-hydroxytamoxifen. hydroxytamoxifen 180-198 epidermal growth factor receptor Homo sapiens 124-128 19179445-7 2009 Long-term treatment with both 4-hydroxytamoxifen and ICI182,780 increased EGFR levels, but this was not seen in response to TAM. hydroxytamoxifen 30-48 epidermal growth factor receptor Homo sapiens 74-78 19264808-4 2009 The E(2)-induced reduction in miR-21 was inhibited by 4-hydroxytamoxifen (4-OHT), ICI 182 780 (Faslodex), and siRNA ER alpha indicating that the suppression is ER alpha-mediated. hydroxytamoxifen 54-72 microRNA 21 Homo sapiens 30-36 19221464-6 2009 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. hydroxytamoxifen 199-217 beclin 1 Homo sapiens 122-130 19153601-3 2009 We show here for ER-negative human breast cancer cells that the activation of GPR30 signalling by oestrogen or by hydroxytamoxifen (OHT), an ER antagonist but GPR30 agonist, induces a transcription factor network, which resembles that induced by serum in fibroblasts. hydroxytamoxifen 114-130 G protein-coupled estrogen receptor 1 Homo sapiens 78-83 19153601-3 2009 We show here for ER-negative human breast cancer cells that the activation of GPR30 signalling by oestrogen or by hydroxytamoxifen (OHT), an ER antagonist but GPR30 agonist, induces a transcription factor network, which resembles that induced by serum in fibroblasts. hydroxytamoxifen 114-130 G protein-coupled estrogen receptor 1 Homo sapiens 159-164 19244109-6 2009 For active hepatic UGTs, the UGT2B7(268Tyr) variant exhibited significant (P < 0.01) 2- and 5-fold decreases in activity against the trans isomers of 4-OH-TAM and endoxifen, respectively, compared with wild-type UGT2B7(268His). hydroxytamoxifen 153-161 UDP glucuronosyltransferase family 2 member B7 Homo sapiens 29-35 19244109-6 2009 For active hepatic UGTs, the UGT2B7(268Tyr) variant exhibited significant (P < 0.01) 2- and 5-fold decreases in activity against the trans isomers of 4-OH-TAM and endoxifen, respectively, compared with wild-type UGT2B7(268His). hydroxytamoxifen 153-161 UDP glucuronosyltransferase family 2 member B7 Homo sapiens 215-221 19244109-2 2009 A major mode of metabolism of the major active metabolites of TAM, 4-OH-TAM and endoxifen, is by glucuronidation via the UDP-glucuronosyltransferase (UGT) family of enzymes. hydroxytamoxifen 67-75 UDP glucuronosyltransferase family 1 member A complex locus Homo sapiens 150-153 18974135-6 2008 Selection for resistance to 4-hydroxytamoxifen led to the development of the SUM44/LCCTam cell line, which exhibits decreased expression of ERalpha and increased expression of the estrogen-related receptor gamma (ERRgamma). hydroxytamoxifen 28-46 estrogen receptor 1 Homo sapiens 140-147 19212635-2 2009 In addition, using proteolysis assays, we tested the conformational changes induced in ERalpha and ERbeta by CH4893237, fulvestrant, and 4-OH tamoxifen (4OHT). hydroxytamoxifen 137-151 estrogen receptor 1 Homo sapiens 87-94 19212635-2 2009 In addition, using proteolysis assays, we tested the conformational changes induced in ERalpha and ERbeta by CH4893237, fulvestrant, and 4-OH tamoxifen (4OHT). hydroxytamoxifen 137-151 estrogen receptor 2 Homo sapiens 99-105 19202055-6 2009 We found that AID-ER, but not JP8Bdel-ER, caused a CSR to IgA from the addition of 4-hydroxy tamoxifen. hydroxytamoxifen 83-102 activation induced cytidine deaminase Homo sapiens 14-17 18822397-9 2009 In addition, the ERR antagonists 4-hydroxytamoxifen and diethylstilbestrol inhibited the Hr-ERR-mediated transactivation, whereas Hr-ERR activity on ERE was further induced by genistein, an ERRalpha agonist. hydroxytamoxifen 33-51 solute carrier family 7 member 1 Homo sapiens 17-20 18822397-9 2009 In addition, the ERR antagonists 4-hydroxytamoxifen and diethylstilbestrol inhibited the Hr-ERR-mediated transactivation, whereas Hr-ERR activity on ERE was further induced by genistein, an ERRalpha agonist. hydroxytamoxifen 33-51 solute carrier family 7 member 1 Homo sapiens 92-95 18822397-9 2009 In addition, the ERR antagonists 4-hydroxytamoxifen and diethylstilbestrol inhibited the Hr-ERR-mediated transactivation, whereas Hr-ERR activity on ERE was further induced by genistein, an ERRalpha agonist. hydroxytamoxifen 33-51 solute carrier family 7 member 1 Homo sapiens 92-95 18822397-9 2009 In addition, the ERR antagonists 4-hydroxytamoxifen and diethylstilbestrol inhibited the Hr-ERR-mediated transactivation, whereas Hr-ERR activity on ERE was further induced by genistein, an ERRalpha agonist. hydroxytamoxifen 33-51 estrogen related receptor alpha Homo sapiens 190-198 19197145-4 2009 In cultured cells, activation of a conditional, KLF4-estrogen receptor fusion protein by 4-hydroxytamoxifen resulted in rapid upregulation of transcripts for nuclear receptors including RARgamma and RXRalpha. hydroxytamoxifen 89-107 Kruppel-like factor 4 (gut) Mus musculus 48-52 19197145-4 2009 In cultured cells, activation of a conditional, KLF4-estrogen receptor fusion protein by 4-hydroxytamoxifen resulted in rapid upregulation of transcripts for nuclear receptors including RARgamma and RXRalpha. hydroxytamoxifen 89-107 retinoic acid receptor, gamma Mus musculus 186-194 19197145-4 2009 In cultured cells, activation of a conditional, KLF4-estrogen receptor fusion protein by 4-hydroxytamoxifen resulted in rapid upregulation of transcripts for nuclear receptors including RARgamma and RXRalpha. hydroxytamoxifen 89-107 retinoid X receptor alpha Mus musculus 199-207 18974135-6 2008 Selection for resistance to 4-hydroxytamoxifen led to the development of the SUM44/LCCTam cell line, which exhibits decreased expression of ERalpha and increased expression of the estrogen-related receptor gamma (ERRgamma). hydroxytamoxifen 28-46 estrogen related receptor gamma Homo sapiens 213-221 18974135-6 2008 Selection for resistance to 4-hydroxytamoxifen led to the development of the SUM44/LCCTam cell line, which exhibits decreased expression of ERalpha and increased expression of the estrogen-related receptor gamma (ERRgamma). hydroxytamoxifen 28-46 estrogen related receptor gamma Homo sapiens 180-211 19016759-4 2008 The ERalpha-positive human breast adenocarcinoma derived-MCF-7 cells used in this study have acquired both cross-resistance to hydroxy-tamoxifen (OH-Tam) and to fulvestrant and strong activation of the Akt/mTOR pathway. hydroxytamoxifen 127-144 estrogen receptor 1 Homo sapiens 4-11 18922978-0 2008 An autocrine VEGF/VEGFR2 and p38 signaling loop confers resistance to 4-hydroxytamoxifen in MCF-7 breast cancer cells. hydroxytamoxifen 70-88 vascular endothelial growth factor A Homo sapiens 13-17 18922978-0 2008 An autocrine VEGF/VEGFR2 and p38 signaling loop confers resistance to 4-hydroxytamoxifen in MCF-7 breast cancer cells. hydroxytamoxifen 70-88 kinase insert domain receptor Homo sapiens 18-24 18922978-0 2008 An autocrine VEGF/VEGFR2 and p38 signaling loop confers resistance to 4-hydroxytamoxifen in MCF-7 breast cancer cells. hydroxytamoxifen 70-88 mitogen-activated protein kinase 14 Homo sapiens 29-32 18678925-9 2008 The 3ERT PDB crystal structure has the estrogen receptor bound to the cancer drug 4-hydroxytamoxifen. hydroxytamoxifen 82-100 estrogen receptor 1 Homo sapiens 39-56 18782222-5 2008 First, we employed an embryonic forelimb organ culture of transgenic mice expressing an Akt-Mer (a ligand-binding domain of a mutated estrogen receptor) fusion protein whose kinase activity was conditionally activated by treatment with 4-hydroxytamoxifen (4OHT). hydroxytamoxifen 236-254 AKT serine/threonine kinase 1 Homo sapiens 88-91 18499701-6 2008 However, treatment with 4-hydroxytamoxifen (4-OHT), an antiestrogen, abrogates the ERalpha-mediated suppression in cancer cells. hydroxytamoxifen 24-42 estrogen receptor 1 Homo sapiens 83-90 18790785-6 2008 4-hydroxytamoxifen (TAM; 10(-7) mol/L) alone resulted in cell cycle arrest but no apoptosis, whereas MSA alone (10 micromol/L) induced apoptosis in tamoxifen-sensitive cells. hydroxytamoxifen 0-18 Myeloproliferative syndrome, transient (transient abnormal myelopoiesis) Homo sapiens 20-23 18264725-11 2008 Cell cycle analysis showed AZA + TSA treated cells showed S phase arrest, which was partially attenuated by addition of estradiol (E2); furthermore, the effect of E2 on stimulation of cell cycle could be reversed by 4-OHT in the treated cells with induced ER alpha. hydroxytamoxifen 216-221 estrogen receptor 1 Homo sapiens 256-264 18508261-7 2008 We show that ICI-182780, raloxifene, 4-hydroxytamoxifen and estradiol all exhibit differential agonistic activities on the MMP1 promoter by suppressing activity by 20-80%. hydroxytamoxifen 37-55 matrix metallopeptidase 1 Homo sapiens 123-127 18338336-7 2008 This could have been because the contribution of CYP3A to the formation of 4-hydroxytamoxifen is not considerable in rats. hydroxytamoxifen 75-93 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 49-54 18337247-7 2008 In tamoxifen-resistant breast cancer cells that overexpress ERalpha, TPBM inhibited 17beta-estradiol (E(2))-ERalpha (IC(50) 9 microm) and 4-hydroxytamoxifen-ERalpha-mediated gene expression. hydroxytamoxifen 138-156 estrogen receptor 1 Homo sapiens 60-67 18294285-1 2008 The clinical outcomes of breast cancer patients treated with tamoxifen may be influenced by the activity of cytochrome P450 2D6 (CYP2D6) enzyme because tamixifen is metabolized by CYP2D6 to its active forms of antiestrogenic metabolite, 4-hydroxytamoxifen and endoxifen. hydroxytamoxifen 237-255 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 108-127 18299335-0 2008 Role of human pregnane X receptor in tamoxifen- and 4-hydroxytamoxifen-mediated CYP3A4 induction in primary human hepatocytes and LS174T cells. hydroxytamoxifen 52-70 nuclear receptor subfamily 1 group I member 2 Homo sapiens 14-33 18299335-0 2008 Role of human pregnane X receptor in tamoxifen- and 4-hydroxytamoxifen-mediated CYP3A4 induction in primary human hepatocytes and LS174T cells. hydroxytamoxifen 52-70 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 80-86 18299335-1 2008 Previously we observed that the antiestrogens tamoxifen and 4-hydroxytamoxifen (4OHT) induce CYP3A4 in primary human hepatocytes and activate human pregnane X receptor (PXR) in cell-based reporter assays. hydroxytamoxifen 60-78 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 93-99 18299335-1 2008 Previously we observed that the antiestrogens tamoxifen and 4-hydroxytamoxifen (4OHT) induce CYP3A4 in primary human hepatocytes and activate human pregnane X receptor (PXR) in cell-based reporter assays. hydroxytamoxifen 60-78 nuclear receptor subfamily 1 group I member 2 Homo sapiens 148-167 18299335-1 2008 Previously we observed that the antiestrogens tamoxifen and 4-hydroxytamoxifen (4OHT) induce CYP3A4 in primary human hepatocytes and activate human pregnane X receptor (PXR) in cell-based reporter assays. hydroxytamoxifen 60-78 nuclear receptor subfamily 1 group I member 2 Homo sapiens 169-172 18294285-1 2008 The clinical outcomes of breast cancer patients treated with tamoxifen may be influenced by the activity of cytochrome P450 2D6 (CYP2D6) enzyme because tamixifen is metabolized by CYP2D6 to its active forms of antiestrogenic metabolite, 4-hydroxytamoxifen and endoxifen. hydroxytamoxifen 237-255 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 129-135 18294285-1 2008 The clinical outcomes of breast cancer patients treated with tamoxifen may be influenced by the activity of cytochrome P450 2D6 (CYP2D6) enzyme because tamixifen is metabolized by CYP2D6 to its active forms of antiestrogenic metabolite, 4-hydroxytamoxifen and endoxifen. hydroxytamoxifen 237-255 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 180-186 18006630-3 2008 This activation was blocked by treatment with estrogen receptor (ER) antagonists 4-hydroxytamoxifen and ICI-182,780. hydroxytamoxifen 81-99 estrogen receptor 1 Homo sapiens 46-63 21479421-4 2008 Transient expression of p72, AIB1 and erbB-2 in human embryonic kidney 293T cells led to a synergistic promotion of the transactivation function of ERalpha in the presence of 17alpha-estradiol or 4-hydroxytamoxifen, an ERalpha AF-1 agonist/AF-2 antagonist, as a ligand. hydroxytamoxifen 196-214 DEAD-box helicase 17 Homo sapiens 24-27 21479421-4 2008 Transient expression of p72, AIB1 and erbB-2 in human embryonic kidney 293T cells led to a synergistic promotion of the transactivation function of ERalpha in the presence of 17alpha-estradiol or 4-hydroxytamoxifen, an ERalpha AF-1 agonist/AF-2 antagonist, as a ligand. hydroxytamoxifen 196-214 ANIB1 Homo sapiens 29-33 21479421-4 2008 Transient expression of p72, AIB1 and erbB-2 in human embryonic kidney 293T cells led to a synergistic promotion of the transactivation function of ERalpha in the presence of 17alpha-estradiol or 4-hydroxytamoxifen, an ERalpha AF-1 agonist/AF-2 antagonist, as a ligand. hydroxytamoxifen 196-214 erb-b2 receptor tyrosine kinase 2 Homo sapiens 38-44 21479421-4 2008 Transient expression of p72, AIB1 and erbB-2 in human embryonic kidney 293T cells led to a synergistic promotion of the transactivation function of ERalpha in the presence of 17alpha-estradiol or 4-hydroxytamoxifen, an ERalpha AF-1 agonist/AF-2 antagonist, as a ligand. hydroxytamoxifen 196-214 estrogen receptor 1 Homo sapiens 148-155 18409049-4 2008 Treatment with H-89, a specific PKA inhibitor, suppressed 4-hydroxytamoxifen-induced ErbB2 expression in control MCF-7 cells. hydroxytamoxifen 58-76 erb-b2 receptor tyrosine kinase 2 Homo sapiens 85-90 18216173-5 2008 We used transgenic mice that expressed an AKT-MER fusion protein, the kinase activity of which could be regulated by the ligand of modified estrogen receptor (MER), 4-hydroxytamoxifen. hydroxytamoxifen 165-183 thymoma viral proto-oncogene 1 Mus musculus 42-45 18216173-5 2008 We used transgenic mice that expressed an AKT-MER fusion protein, the kinase activity of which could be regulated by the ligand of modified estrogen receptor (MER), 4-hydroxytamoxifen. hydroxytamoxifen 165-183 G protein-coupled estrogen receptor 1 Mus musculus 46-49 18216173-5 2008 We used transgenic mice that expressed an AKT-MER fusion protein, the kinase activity of which could be regulated by the ligand of modified estrogen receptor (MER), 4-hydroxytamoxifen. hydroxytamoxifen 165-183 estrogen receptor 1 (alpha) Mus musculus 140-157 18288420-5 2008 Treatment with ligand 17-beta estradiol diminished the HER2 expression in MCF-7 wild-type cells, an effect partially inhibited by treatment with 4-OH tamoxifen. hydroxytamoxifen 145-159 erb-b2 receptor tyrosine kinase 2 Homo sapiens 55-59 18372406-6 2008 Further, we show that, although S118 is important for the stimulation of ERalpha activity by the selective ER modulator 4-hydroxytamoxifen (OHT), S104 and S106 are also required for the agonist activity of OHT. hydroxytamoxifen 120-138 estrogen receptor 1 Homo sapiens 73-80 18347152-3 2008 Analysis of transfected K562, KD30, and KD225 cells in which FOXO3a activity can be induced by 4-hydroxytamoxifen showed that FOXO3a up-regulates ABCB1 expression at protein, mRNA, and gene promoter levels. hydroxytamoxifen 95-113 forkhead box O3 Homo sapiens 61-67 18347152-3 2008 Analysis of transfected K562, KD30, and KD225 cells in which FOXO3a activity can be induced by 4-hydroxytamoxifen showed that FOXO3a up-regulates ABCB1 expression at protein, mRNA, and gene promoter levels. hydroxytamoxifen 95-113 forkhead box O3 Homo sapiens 126-132 18347152-3 2008 Analysis of transfected K562, KD30, and KD225 cells in which FOXO3a activity can be induced by 4-hydroxytamoxifen showed that FOXO3a up-regulates ABCB1 expression at protein, mRNA, and gene promoter levels. hydroxytamoxifen 95-113 ATP binding cassette subfamily B member 1 Homo sapiens 146-151 18006630-3 2008 This activation was blocked by treatment with estrogen receptor (ER) antagonists 4-hydroxytamoxifen and ICI-182,780. hydroxytamoxifen 81-99 estrogen receptor 1 Homo sapiens 65-67 18223215-8 2008 Importantly, CEACAM6 silencing restored sensitivity of TAMr cells to 4-hydroxytamoxifen and proliferative response to 17beta-estradiol. hydroxytamoxifen 69-87 CEA cell adhesion molecule 6 Homo sapiens 13-20 17986386-4 2008 Similarly, SeP mRNA was upregulated in response to activation of FoxO1a in rat hepatoma cells stably transfected with a hydroxytamoxifen-regulatable form of FoxO1a. hydroxytamoxifen 120-136 selenoprotein P Homo sapiens 11-14 17986386-4 2008 Similarly, SeP mRNA was upregulated in response to activation of FoxO1a in rat hepatoma cells stably transfected with a hydroxytamoxifen-regulatable form of FoxO1a. hydroxytamoxifen 120-136 forkhead box O1 Rattus norvegicus 65-71 17986386-4 2008 Similarly, SeP mRNA was upregulated in response to activation of FoxO1a in rat hepatoma cells stably transfected with a hydroxytamoxifen-regulatable form of FoxO1a. hydroxytamoxifen 120-136 forkhead box O1 Rattus norvegicus 157-163 18637494-4 2008 Tamoxifen requires "metabolic activation" catalyzed by cytochrome P450 2D6 (CYP2D6) to form hydroxylated metabolites-4-hydroxytamoxifen and endoxifen (N-desmethyl-4-hydroxytamoxifen)-both of which are much more potent than is the parent drug. hydroxytamoxifen 117-135 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 55-74 17947222-1 2008 BACKGROUND: Tamoxifen is hydroxylated by cytochrome P450 (CYP) 2D6 to the potent metabolites 4-hydroxytamoxifen (4OHtam) and 4-hydroxy-N-demethyltamoxifen (4OHNDtam), which are both conjugated by sulphotransferase (SULT)1A1. hydroxytamoxifen 93-111 sulfotransferase family 1A member 1 Homo sapiens 215-223 18637494-4 2008 Tamoxifen requires "metabolic activation" catalyzed by cytochrome P450 2D6 (CYP2D6) to form hydroxylated metabolites-4-hydroxytamoxifen and endoxifen (N-desmethyl-4-hydroxytamoxifen)-both of which are much more potent than is the parent drug. hydroxytamoxifen 117-135 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 76-82 18043895-7 2008 Only two metabolites 4-hydroxytamoxifen and N-desmethyl-4-hydroxytamoxifen had significant antiproliferative activity and were able to induce TGFbeta2 and TbetaRII. hydroxytamoxifen 21-39 transforming growth factor beta 2 Homo sapiens 142-150 18043895-7 2008 Only two metabolites 4-hydroxytamoxifen and N-desmethyl-4-hydroxytamoxifen had significant antiproliferative activity and were able to induce TGFbeta2 and TbetaRII. hydroxytamoxifen 21-39 transforming growth factor beta receptor 2 Homo sapiens 155-163 18197296-2 2008 We have recently demonstrated that BPA binds strongly to human estrogen-related receptor-gamma (ERR-gamma ) in a binding assay using [3H]4-hydroxytamoxifen ([3H]4-OHT). hydroxytamoxifen 137-155 estrogen related receptor gamma Homo sapiens 63-94 18197296-2 2008 We have recently demonstrated that BPA binds strongly to human estrogen-related receptor-gamma (ERR-gamma ) in a binding assay using [3H]4-hydroxytamoxifen ([3H]4-OHT). hydroxytamoxifen 137-155 estrogen related receptor gamma Homo sapiens 96-105 17900262-4 2007 To this end, we generated a 4-hydroxytamoxifen-inducible active FKHRL1 (FKHRL1-TM; a triple mutant of FKHRL1 in which all three Akt phosphorylation sites have been mutated)-estrogen receptor fusion protein expression system in CML-derived imatinib-resistant cell lines. hydroxytamoxifen 28-46 forkhead box O3 Homo sapiens 64-70 17964775-4 2008 These ligands were further characterized and found to be competitive for 4-hydroxytamoxifen (4OHT) binding, a known reported antagonist ligand for ERRgamma, but functionally they did not enhance or disrupt affinity of the receptor for co-activator peptides. hydroxytamoxifen 73-91 estrogen related receptor gamma Homo sapiens 147-155 18827493-5 2008 The expression of AIB1, ERalpha, HER2 and pS2 was analyzed in the presence of 17beta-estradiol or 4-hydroxytamoxifen (Tam) by Western blot analysis. hydroxytamoxifen 98-116 HEAT repeat containing 6 Homo sapiens 18-22 18827493-5 2008 The expression of AIB1, ERalpha, HER2 and pS2 was analyzed in the presence of 17beta-estradiol or 4-hydroxytamoxifen (Tam) by Western blot analysis. hydroxytamoxifen 98-116 trefoil factor 1 Homo sapiens 42-45 17900262-5 2007 4-Hydroxytamoxifen inhibited cell growth and cell cycle progression, and subsequently induced apoptosis, accompanied by upregulation of tumor necrosis factor-related apoptosis-inducing ligand (TRAIL). hydroxytamoxifen 0-18 TNF superfamily member 10 Homo sapiens 136-191 17900262-4 2007 To this end, we generated a 4-hydroxytamoxifen-inducible active FKHRL1 (FKHRL1-TM; a triple mutant of FKHRL1 in which all three Akt phosphorylation sites have been mutated)-estrogen receptor fusion protein expression system in CML-derived imatinib-resistant cell lines. hydroxytamoxifen 28-46 forkhead box O3 Homo sapiens 72-78 17900262-5 2007 4-Hydroxytamoxifen inhibited cell growth and cell cycle progression, and subsequently induced apoptosis, accompanied by upregulation of tumor necrosis factor-related apoptosis-inducing ligand (TRAIL). hydroxytamoxifen 0-18 TNF superfamily member 10 Homo sapiens 193-198 17900262-4 2007 To this end, we generated a 4-hydroxytamoxifen-inducible active FKHRL1 (FKHRL1-TM; a triple mutant of FKHRL1 in which all three Akt phosphorylation sites have been mutated)-estrogen receptor fusion protein expression system in CML-derived imatinib-resistant cell lines. hydroxytamoxifen 28-46 forkhead box O3 Homo sapiens 72-78 18005256-4 2007 Bisphenol A functions as an inverse antagonist of estrogen-related receptor gamma to sustain the high basal constitutive activity of the latter and to reverse the deactivating inverse agonist activity of 4-hydroxytamoxifen. hydroxytamoxifen 204-222 estrogen related receptor gamma Homo sapiens 50-81 18365873-4 2007 Following treatment with the oestrogen analogue 4-hydroxy tamoxifen of murine embryonic stem cells expressing this protein, we have identified by microarray analysis, several potential targets of Dnmt3a mediated transcriptional repression including the cancer associated genes Ssx2ip, Hmga1 and Wrnip. hydroxytamoxifen 48-67 DNA methyltransferase 3A Mus musculus 196-202 18365873-4 2007 Following treatment with the oestrogen analogue 4-hydroxy tamoxifen of murine embryonic stem cells expressing this protein, we have identified by microarray analysis, several potential targets of Dnmt3a mediated transcriptional repression including the cancer associated genes Ssx2ip, Hmga1 and Wrnip. hydroxytamoxifen 48-67 synovial sarcoma, X 2 interacting protein Mus musculus 277-283 18365873-4 2007 Following treatment with the oestrogen analogue 4-hydroxy tamoxifen of murine embryonic stem cells expressing this protein, we have identified by microarray analysis, several potential targets of Dnmt3a mediated transcriptional repression including the cancer associated genes Ssx2ip, Hmga1 and Wrnip. hydroxytamoxifen 48-67 high mobility group AT-hook 1 Mus musculus 285-290 18365873-4 2007 Following treatment with the oestrogen analogue 4-hydroxy tamoxifen of murine embryonic stem cells expressing this protein, we have identified by microarray analysis, several potential targets of Dnmt3a mediated transcriptional repression including the cancer associated genes Ssx2ip, Hmga1 and Wrnip. hydroxytamoxifen 48-67 Werner helicase interacting protein 1 Mus musculus 295-300 17761695-4 2007 BPA preserves the ERR gamma"s basal constitutive activity, and protects the selective ER modulator 4-hydroxytamoxifen from its deactivation of ERR gamma. hydroxytamoxifen 99-117 estrogen related receptor gamma Homo sapiens 143-152 17929966-3 2007 A polymer conjugated to the 4-hydroxytamoxifen analogue with a six-carbon linker showed high affinity for both estrogen receptor alpha and estrogen receptor beta and potent antagonism of the estrogen receptor in cell-based transcriptional reporter assays. hydroxytamoxifen 28-46 estrogen receptor 1 Homo sapiens 111-134 17929966-3 2007 A polymer conjugated to the 4-hydroxytamoxifen analogue with a six-carbon linker showed high affinity for both estrogen receptor alpha and estrogen receptor beta and potent antagonism of the estrogen receptor in cell-based transcriptional reporter assays. hydroxytamoxifen 28-46 estrogen receptor 2 Homo sapiens 139-161 17929966-3 2007 A polymer conjugated to the 4-hydroxytamoxifen analogue with a six-carbon linker showed high affinity for both estrogen receptor alpha and estrogen receptor beta and potent antagonism of the estrogen receptor in cell-based transcriptional reporter assays. hydroxytamoxifen 28-46 estrogen receptor 1 Homo sapiens 111-128 17929966-4 2007 These results suggest that the conjugation of 4-hydroxytamoxifen to a polymer results in a macromolecular conjugate that can display ligand in a manner that can be recognized by estrogen receptor and still act as a potent antiestrogen in cells. hydroxytamoxifen 46-64 estrogen receptor 1 Homo sapiens 178-195 17664247-4 2007 In the present study, characterization of the glucuronidating activities of human UDP glucuronosyltransferases (UGTs) against isomers of 4-OH-TAM and endoxifen was performed. hydroxytamoxifen 137-145 beta-1,3-glucuronyltransferase 2 Homo sapiens 82-110 17664247-4 2007 In the present study, characterization of the glucuronidating activities of human UDP glucuronosyltransferases (UGTs) against isomers of 4-OH-TAM and endoxifen was performed. hydroxytamoxifen 137-145 beta-1,3-glucuronyltransferase 2 Homo sapiens 112-116 17664247-10 2007 These data suggest that several UGTs, including UGTs 1A10, 2B7, and 1A8 play an important role in the metabolism of 4-OH-TAM and endoxifen. hydroxytamoxifen 116-124 beta-1,3-glucuronyltransferase 2 Homo sapiens 32-36 17664247-10 2007 These data suggest that several UGTs, including UGTs 1A10, 2B7, and 1A8 play an important role in the metabolism of 4-OH-TAM and endoxifen. hydroxytamoxifen 116-124 beta-1,3-glucuronyltransferase 2 Homo sapiens 48-52 17716978-1 2007 Low concentrations of tamoxifen or its active metabolite 4-hydroxytamoxifen (OHT) induce estrogen receptor alpha (ERalpha)-dependent apoptosis. hydroxytamoxifen 57-75 estrogen receptor 1 Homo sapiens 89-112 17716978-1 2007 Low concentrations of tamoxifen or its active metabolite 4-hydroxytamoxifen (OHT) induce estrogen receptor alpha (ERalpha)-dependent apoptosis. hydroxytamoxifen 57-75 estrogen receptor 1 Homo sapiens 114-121 17646931-0 2007 Regulation of intracellular calcium release and PP1alpha in a mechanism for 4-hydroxytamoxifen-induced cytotoxicity. hydroxytamoxifen 76-94 protein phosphatase 1 catalytic subunit alpha Homo sapiens 48-56 17714751-0 2007 Delayed and persistent ERK1/2 activation is required for 4-hydroxytamoxifen-induced cell death. hydroxytamoxifen 57-75 mitogen-activated protein kinase 3 Homo sapiens 23-29 17637499-4 2007 MATERIALS AND METHODS: Multipotent FDCP-mix cell lines engineered to permit the conditional induction of the constitutively active intracellular domain of mNotch1 (mN1(IC)) by the 4-hydroxytamoxifen (OHT)-inducible system were used to analyze the effects of activated mNotch1 on erythroid differentiation and on expression of Gata1, Fog1, Eklf, NF-E2, and beta-globin. hydroxytamoxifen 180-198 notch 1 Mus musculus 155-162 17637499-4 2007 MATERIALS AND METHODS: Multipotent FDCP-mix cell lines engineered to permit the conditional induction of the constitutively active intracellular domain of mNotch1 (mN1(IC)) by the 4-hydroxytamoxifen (OHT)-inducible system were used to analyze the effects of activated mNotch1 on erythroid differentiation and on expression of Gata1, Fog1, Eklf, NF-E2, and beta-globin. hydroxytamoxifen 180-198 notch 1 Mus musculus 164-167 17297448-3 2007 We examined the effect of Akt signaling in epidermal cells in transgenic mice expressing an Akt-Mer fusion protein whose kinase activity was conditionally activated by treatment with 4-hydroxytamoxifen (4OHT). hydroxytamoxifen 183-201 thymoma viral proto-oncogene 1 Mus musculus 92-95 17615152-0 2007 A functional serine 118 phosphorylation site in estrogen receptor-alpha is required for down-regulation of gene expression by 17beta-estradiol and 4-hydroxytamoxifen. hydroxytamoxifen 147-165 estrogen receptor 1 Homo sapiens 48-71 17458895-7 2007 Finally, the IGF-I-induced response on cell growth and ER-mediated transactivation can be inhibited with either ICI or 4-OH-Tam. hydroxytamoxifen 119-127 insulin-like growth factor 1 Mus musculus 13-18 17556356-8 2007 This is in contrast to ERRgamma but resembles the situation for ERalpha (raloxifene or 4-hydroxytamoxifen complexes). hydroxytamoxifen 87-105 estrogen receptor 1 Homo sapiens 64-71 17384075-4 2007 Specifically, we have used QCM-D, in combination with surface plasmon resonance (SPR) spectroscopy, to monitor the binding of ERalpha to a specific DNA (estrogen response element, ERE) and a nonspecific DNA in the presence of either the agonist ligand, 17b-estradiol, the partial antagonist ligand, 4-hydroxytamoxifen, or vehicle alone. hydroxytamoxifen 299-317 estrogen receptor 1 Homo sapiens 126-133 17009105-4 2007 The effect of E2 on psoriasin/S100A7 was inhibited by 4-hydroxytamoxifen and ICI 182780 but not with a selective ERalpha antagonist. hydroxytamoxifen 54-72 S100 calcium binding protein A7 Homo sapiens 30-36 17482685-6 2007 Indeed, a 4-hydroxytamoxifen activated E2F-1-ER fusion protein induced FOXO expression in the presence of cycloheximide. hydroxytamoxifen 10-28 E2F transcription factor 1 Rattus norvegicus 39-44 17173074-4 2007 An E2F1-estrogen receptor fusion protein activated the endogenous p57 promoter in response to hydroxytamoxifen treatment in the presence of cycloheximide. hydroxytamoxifen 94-110 E2F transcription factor 1 Homo sapiens 3-7 17173074-4 2007 An E2F1-estrogen receptor fusion protein activated the endogenous p57 promoter in response to hydroxytamoxifen treatment in the presence of cycloheximide. hydroxytamoxifen 94-110 cyclin dependent kinase inhibitor 1C Homo sapiens 66-69 17272397-6 2007 In HEK293 cells, SHP-1 was inhibited by raloxifene and 4-hydroxytamoxifen, whereas the latter additionally inhibited SHP-2. hydroxytamoxifen 55-73 protein tyrosine phosphatase non-receptor type 6 Homo sapiens 17-22 17348852-8 2007 The structure-activity relationships for the active ligands were further explored in a computational study where docked structures of the active compounds were compared with the X-ray crystal structures for the complexes of ER alpha with 4-hydroxytamoxifen and ER beta with raloxifene. hydroxytamoxifen 238-256 estrogen receptor 1 Homo sapiens 224-232 17339440-6 2007 By temporally controlling the expression of T-bet-estrogen receptor alpha by the addition or removal of 4-hydroxytamoxifen (4-HT), we show that IFN-gamma, CD122, and CxCR3 are direct gene targets of T-bet whose expression are acutely regulated by T-bet activity. hydroxytamoxifen 104-122 T-box transcription factor 21 Homo sapiens 44-49 17339440-6 2007 By temporally controlling the expression of T-bet-estrogen receptor alpha by the addition or removal of 4-hydroxytamoxifen (4-HT), we show that IFN-gamma, CD122, and CxCR3 are direct gene targets of T-bet whose expression are acutely regulated by T-bet activity. hydroxytamoxifen 104-122 estrogen receptor 1 Homo sapiens 50-73 17339440-6 2007 By temporally controlling the expression of T-bet-estrogen receptor alpha by the addition or removal of 4-hydroxytamoxifen (4-HT), we show that IFN-gamma, CD122, and CxCR3 are direct gene targets of T-bet whose expression are acutely regulated by T-bet activity. hydroxytamoxifen 104-122 interferon gamma Homo sapiens 144-153 17339440-6 2007 By temporally controlling the expression of T-bet-estrogen receptor alpha by the addition or removal of 4-hydroxytamoxifen (4-HT), we show that IFN-gamma, CD122, and CxCR3 are direct gene targets of T-bet whose expression are acutely regulated by T-bet activity. hydroxytamoxifen 104-122 interleukin 2 receptor subunit beta Homo sapiens 155-160 17339440-6 2007 By temporally controlling the expression of T-bet-estrogen receptor alpha by the addition or removal of 4-hydroxytamoxifen (4-HT), we show that IFN-gamma, CD122, and CxCR3 are direct gene targets of T-bet whose expression are acutely regulated by T-bet activity. hydroxytamoxifen 104-122 C-X-C motif chemokine receptor 3 Homo sapiens 166-171 17339440-6 2007 By temporally controlling the expression of T-bet-estrogen receptor alpha by the addition or removal of 4-hydroxytamoxifen (4-HT), we show that IFN-gamma, CD122, and CxCR3 are direct gene targets of T-bet whose expression are acutely regulated by T-bet activity. hydroxytamoxifen 104-122 T-box transcription factor 21 Homo sapiens 199-204 17339440-6 2007 By temporally controlling the expression of T-bet-estrogen receptor alpha by the addition or removal of 4-hydroxytamoxifen (4-HT), we show that IFN-gamma, CD122, and CxCR3 are direct gene targets of T-bet whose expression are acutely regulated by T-bet activity. hydroxytamoxifen 104-122 T-box transcription factor 21 Homo sapiens 199-204 17464340-0 2007 Effects of estradiol and 4-hydroxytamoxifen on the conformation, thermal stability, and DNA recognition of estrogen receptor beta. hydroxytamoxifen 25-43 estrogen receptor 2 Homo sapiens 107-129 17135255-4 2007 Binding of SRC1a to flERE.ERalpha and to flERE.ERbeta was 17beta-estradiol (E2)-dependent and was nearly absent when ICI 182,780, raloxifene, or 4-hydroxytamoxifen were bound to the ERs. hydroxytamoxifen 145-163 estrogen receptor 2 Homo sapiens 47-53 17464340-2 2007 We examined the effects of estradiol (E2), 4-hydroxytamoxifen (HT), and the estrogen response element (ERE) on the helical content and thermal unfolding of ERbeta. hydroxytamoxifen 43-61 estrogen receptor 2 Homo sapiens 156-162 17047084-4 2006 The orphan nuclear receptor chicken ovalbumin upstream promoter transcription factor (COUP-TF)-I interacts directly with 4-hydroxytamoxifen (4-OHT)- and estradiol (E(2))-occupied ERalpha, corepressors NCoR and SMRT, and inhibit E(2)-induced gene transcription in breast cancer cells. hydroxytamoxifen 121-139 nuclear receptor subfamily 2 group F member 1 Gallus gallus 86-96 17108112-2 2006 In this study, we investigated the effect of chronic PKB activation on cellular survival and proliferation using cytokine-dependent bone marrow-derived Ba/F3 cells, in which PKBalpha activation can be directly, and specifically, induced by addition of 4-hydroxytamoxifen (4-OHT). hydroxytamoxifen 252-270 thymoma viral proto-oncogene 1 Mus musculus 174-182 16926159-6 2006 In the presence of 4-hydroxytamoxifen STAT3-ER was translocated in the nucleus of HepG2 cells in a phosphorylation-independent manner, and treatment with PDTC mitigated the response. hydroxytamoxifen 19-37 signal transducer and activator of transcription 3 Homo sapiens 38-43 17897439-12 2007 Furthermore, Wnt1 rescues estrogen receptor-positive (ER+) breast cancer cells from the anti-proliferative effects of 4-hydroxytamoxifen (4-HT) and this activity can be blocked by an EGFR tyrosine kinase inhibitor. hydroxytamoxifen 118-136 Wnt family member 1 Homo sapiens 13-17 17897439-12 2007 Furthermore, Wnt1 rescues estrogen receptor-positive (ER+) breast cancer cells from the anti-proliferative effects of 4-hydroxytamoxifen (4-HT) and this activity can be blocked by an EGFR tyrosine kinase inhibitor. hydroxytamoxifen 118-136 epidermal growth factor receptor Homo sapiens 183-187 17216603-6 2007 administration of 4-OHT on Cre-mediated, heart-specific inactivation of thioredoxin reductase 2. hydroxytamoxifen 18-23 thioredoxin reductase 2 Mus musculus 72-95 17008385-5 2007 We studied the effects of estradiol and the clinically useful SERMs 4-hydroxytamoxifen and fulvestrant on the conformation of the full-length ERalpha dimer complex by comparing, in living human breast cancer cells, the amounts of energy transfer between fluorophores attached to different domains of ERalpha. hydroxytamoxifen 68-86 estrogen receptor 1 Homo sapiens 142-149 17008385-6 2007 Estradiol, 4-hydroxytamoxifen, and fulvestrant all promoted the rapid formation of ERalpha dimers with equivalent interaction kinetics. hydroxytamoxifen 11-29 estrogen receptor 1 Homo sapiens 83-90 17008385-7 2007 The amino- and carboxyl-terminal ERalpha domains both contain activation functions differentially affected by these ligands, but the positions of only the carboxyl termini differed upon binding with estradiol, 4-hydroxytamoxifen, or fulvestrant. hydroxytamoxifen 210-228 estrogen receptor 1 Homo sapiens 33-40 17047084-4 2006 The orphan nuclear receptor chicken ovalbumin upstream promoter transcription factor (COUP-TF)-I interacts directly with 4-hydroxytamoxifen (4-OHT)- and estradiol (E(2))-occupied ERalpha, corepressors NCoR and SMRT, and inhibit E(2)-induced gene transcription in breast cancer cells. hydroxytamoxifen 121-139 estrogen receptor 1 Gallus gallus 179-186 16889744-2 2006 Although its physiological ligand is unknown, ERRgamma has been shown to interact with synthetic estrogenic compounds such as 4-hydroxytamoxifen (4-OHT), tamoxifen, and diethylstilbestrol (DES). hydroxytamoxifen 126-144 estrogen related receptor gamma Homo sapiens 46-54 16828306-4 2006 By crossing neurogenin 2 (Ngn2-CreER) with Cre-reporter mice expressing YFP or GFP reporter genes, it was possible to observe living cells after treating slice cultures with 4-hydroxytamoxifen to induce Cre recombinase activation. hydroxytamoxifen 174-192 neurogenin 2 Mus musculus 12-24 16782818-0 2006 A second binding site for hydroxytamoxifen within the coactivator-binding groove of estrogen receptor beta. hydroxytamoxifen 26-42 estrogen receptor 2 Homo sapiens 84-106 16782818-1 2006 Evidence is presented that the estrogen antagonist 4-hydroxytamoxifen (HT) can occupy not only the core binding pocket within the ligand-binding domain of estrogen receptor (ER) beta but also a second site on its surface. hydroxytamoxifen 51-69 estrogen receptor 2 Homo sapiens 155-182 16517757-4 2006 The enzyme activities of the SULT1A1 allozymes were studied with a variety of substrates, including PNP, 17beta-estradiol, 2-methoxyestradiol, catecholestrogens, the antiestrogen 4-hydroxytamoxifen (OHT), and dietary flavonoids. hydroxytamoxifen 179-197 sulfotransferase family 1A member 1 Homo sapiens 29-36 16835357-0 2006 17beta-estradiol, genistein, and 4-hydroxytamoxifen induce the proliferation of thyroid cancer cells through the g protein-coupled receptor GPR30. hydroxytamoxifen 33-51 G protein-coupled estrogen receptor 1 Homo sapiens 140-145 16899133-11 2006 (b) 4-Hydroxytamoxifen (but not tamoxifen), genistein (but not genistin), daidzein, and probably other nutritional and chemopreventive anti-cancer agents could up-regulate expression of p27 via receptor protein tyrosine kinases (RPTKs), phosphoinositide 3-kinase (PI3K), phosphoinosite-dependent kinase (PDK), Akt/PKB and mTOR. hydroxytamoxifen 4-22 interferon alpha inducible protein 27 Homo sapiens 186-189 16899133-11 2006 (b) 4-Hydroxytamoxifen (but not tamoxifen), genistein (but not genistin), daidzein, and probably other nutritional and chemopreventive anti-cancer agents could up-regulate expression of p27 via receptor protein tyrosine kinases (RPTKs), phosphoinositide 3-kinase (PI3K), phosphoinosite-dependent kinase (PDK), Akt/PKB and mTOR. hydroxytamoxifen 4-22 AKT serine/threonine kinase 1 Homo sapiens 310-317 16899133-11 2006 (b) 4-Hydroxytamoxifen (but not tamoxifen), genistein (but not genistin), daidzein, and probably other nutritional and chemopreventive anti-cancer agents could up-regulate expression of p27 via receptor protein tyrosine kinases (RPTKs), phosphoinositide 3-kinase (PI3K), phosphoinosite-dependent kinase (PDK), Akt/PKB and mTOR. hydroxytamoxifen 4-22 mechanistic target of rapamycin kinase Homo sapiens 322-326 16828306-4 2006 By crossing neurogenin 2 (Ngn2-CreER) with Cre-reporter mice expressing YFP or GFP reporter genes, it was possible to observe living cells after treating slice cultures with 4-hydroxytamoxifen to induce Cre recombinase activation. hydroxytamoxifen 174-192 neurogenin 2 Mus musculus 26-30 16567807-8 2006 The interruption of this signaling pathway by specific phosphatidylinositol 3-kinase or Akt inhibitors suppresses the cytokine-mediated effects on GABA(A)R, whereas activation of the conditionally active form of Akt1 (myr-Akt1.ER*) with 4-hydroxytamoxifen reproduces the effects. hydroxytamoxifen 237-255 AKT serine/threonine kinase 1 Homo sapiens 212-216 16617145-6 2006 Using the H1299 ER-E2F1 cell line where E2F1 activity can be conditionally induced, E2F1 has been shown to upregulate the Smac/DIABLO expression at both mRNA and protein levels upon 4-hydroxytamoxifen treatment, resulting in an enhanced mitochondria-mediated apoptosis. hydroxytamoxifen 182-200 E2F transcription factor 1 L homeolog Xenopus laevis 40-44 16676322-2 2006 Here, we generated and characterized mice harboring a 4-hydroxytamoxifen (OHT)-inducible Cre recombinase-estrogen receptor fusion transgene under the control of the melanocyte-specific tyrosinase promoter, designated Tyr::CreER(T2). hydroxytamoxifen 54-72 estrogen receptor 1 (alpha) Mus musculus 105-122 16480962-0 2006 Quaternary ammonium-linked glucuronidation of trans-4-hydroxytamoxifen, an active metabolite of tamoxifen, by human liver microsomes and UDP-glucuronosyltransferase 1A4. hydroxytamoxifen 46-70 UDP glucuronosyltransferase family 1 member A4 Homo sapiens 137-168 16617145-6 2006 Using the H1299 ER-E2F1 cell line where E2F1 activity can be conditionally induced, E2F1 has been shown to upregulate the Smac/DIABLO expression at both mRNA and protein levels upon 4-hydroxytamoxifen treatment, resulting in an enhanced mitochondria-mediated apoptosis. hydroxytamoxifen 182-200 E2F transcription factor 1 L homeolog Xenopus laevis 40-44 16617145-6 2006 Using the H1299 ER-E2F1 cell line where E2F1 activity can be conditionally induced, E2F1 has been shown to upregulate the Smac/DIABLO expression at both mRNA and protein levels upon 4-hydroxytamoxifen treatment, resulting in an enhanced mitochondria-mediated apoptosis. hydroxytamoxifen 182-200 diablo, IAP-binding mitochondrial protein L homeolog Xenopus laevis 122-126 16617145-6 2006 Using the H1299 ER-E2F1 cell line where E2F1 activity can be conditionally induced, E2F1 has been shown to upregulate the Smac/DIABLO expression at both mRNA and protein levels upon 4-hydroxytamoxifen treatment, resulting in an enhanced mitochondria-mediated apoptosis. hydroxytamoxifen 182-200 diablo, IAP-binding mitochondrial protein L homeolog Xenopus laevis 127-133 16787364-10 2006 In a computational study, docked structures of the active compounds were compared with the X-ray crystal structures for the complexes of ERalpha with 4-hydroxytamoxifen and ERbeta with raloxifene. hydroxytamoxifen 150-168 estrogen receptor 1 Homo sapiens 137-144 16884532-9 2006 Higher glucuronidation activities were found by kinetic analysis for microsomes from the variant UGT1A424Pro/48Val-overexpressing cell line as compared with microsomes from wild-type UGT1A424Pro/48Leu-overexpressing cells against TAM and against both the trans and cis isomers of 4-OH-TAM. hydroxytamoxifen 280-288 UDP glucuronosyltransferase family 1 member A complex locus Homo sapiens 97-102 16239258-0 2006 The G protein-coupled receptor GPR30 mediates the proliferative effects induced by 17beta-estradiol and hydroxytamoxifen in endometrial cancer cells. hydroxytamoxifen 104-120 G protein-coupled estrogen receptor 1 Homo sapiens 31-36 16475008-2 2006 A 4-hydroxytamoxifen (4-OHT)-eluting PDD was applied around the carotid or femoral artery of a mouse strain carrying both the tamoxifen-inducible and smooth muscle cell (SMC)-specific Cre-recombinase (SM-Cre-ER(T2)) transgene and a stop-floxed beta-galactosidase gene in the Rosa26 locus: the SM-CreER(T2)(ki)/rosa26 mouse. hydroxytamoxifen 2-20 galactosidase, beta 1 Mus musculus 244-262 16475008-2 2006 A 4-hydroxytamoxifen (4-OHT)-eluting PDD was applied around the carotid or femoral artery of a mouse strain carrying both the tamoxifen-inducible and smooth muscle cell (SMC)-specific Cre-recombinase (SM-Cre-ER(T2)) transgene and a stop-floxed beta-galactosidase gene in the Rosa26 locus: the SM-CreER(T2)(ki)/rosa26 mouse. hydroxytamoxifen 2-20 gene trap ROSA 26, Philippe Soriano Mus musculus 275-281 16475008-2 2006 A 4-hydroxytamoxifen (4-OHT)-eluting PDD was applied around the carotid or femoral artery of a mouse strain carrying both the tamoxifen-inducible and smooth muscle cell (SMC)-specific Cre-recombinase (SM-Cre-ER(T2)) transgene and a stop-floxed beta-galactosidase gene in the Rosa26 locus: the SM-CreER(T2)(ki)/rosa26 mouse. hydroxytamoxifen 2-20 gene trap ROSA 26, Philippe Soriano Mus musculus 310-316 16317586-1 2006 Human sulfotransferase 1A1 (SULT1A1) is involved in the metabolism of a number of substances including 4-hydroxytamoxifen. hydroxytamoxifen 103-121 sulfotransferase family 1A member 1 Homo sapiens 6-26 16317586-1 2006 Human sulfotransferase 1A1 (SULT1A1) is involved in the metabolism of a number of substances including 4-hydroxytamoxifen. hydroxytamoxifen 103-121 sulfotransferase family 1A member 1 Homo sapiens 28-35 16884532-10 2006 A significantly (P < 0.02) lower Km value (approximately 1.6-fold to 1.8-fold) was observed for both 4-OH-TAM isomers, while a near-significant (P = 0.053) decrease in Km was observed for TAM for the UGT1A424Pro/48Val variant as compared with wild-type UGT1A4. hydroxytamoxifen 104-112 UDP glucuronosyltransferase family 1 member A complex locus Homo sapiens 203-208 16884532-10 2006 A significantly (P < 0.02) lower Km value (approximately 1.6-fold to 1.8-fold) was observed for both 4-OH-TAM isomers, while a near-significant (P = 0.053) decrease in Km was observed for TAM for the UGT1A424Pro/48Val variant as compared with wild-type UGT1A4. hydroxytamoxifen 104-112 UDP glucuronosyltransferase family 1 member A4 Homo sapiens 203-209 16884532-11 2006 The Vmax/Km ratio for the UGT1A424Pro/48Val variant was significantly (P < or = 0.005) higher than that observed for the wild-type UGT1A4 isoform for both the trans and cis isomers of 4-OH-TAM after normalization for UGT1A4 expression by western blotting. hydroxytamoxifen 187-195 UDP glucuronosyltransferase family 1 member A complex locus Homo sapiens 26-31 16884532-11 2006 The Vmax/Km ratio for the UGT1A424Pro/48Val variant was significantly (P < or = 0.005) higher than that observed for the wild-type UGT1A4 isoform for both the trans and cis isomers of 4-OH-TAM after normalization for UGT1A4 expression by western blotting. hydroxytamoxifen 187-195 UDP glucuronosyltransferase family 1 member A4 Homo sapiens 26-32 16884532-11 2006 The Vmax/Km ratio for the UGT1A424Pro/48Val variant was significantly (P < or = 0.005) higher than that observed for the wild-type UGT1A4 isoform for both the trans and cis isomers of 4-OH-TAM after normalization for UGT1A4 expression by western blotting. hydroxytamoxifen 187-195 UDP glucuronosyltransferase family 1 member A4 Homo sapiens 134-140 16515477-10 2006 The selective estrogen receptor modulators 4-hydroxytamoxifen and 4-hydroxytoremifene antagonize ERRgamma. hydroxytamoxifen 43-61 estrogen related receptor gamma Homo sapiens 97-105 16093440-8 2005 Growth inhibition by MSA and MSA + 4-hydroxytamoxifen in all cell lines was preceded by a specific decrease in ER(alpha) mRNA and protein without an effect on ER(beta) levels. hydroxytamoxifen 35-53 estrogen receptor 1 Homo sapiens 111-113 16367757-3 2006 Here, we show that the 4-hydroxytamoxifen (4-OHT) mediated activation of a C-Raf-estrogen receptor fusion protein leads to the induction of both the PPARbeta and Cox-2 genes, concomitant with a dramatic increase in PGI2 synthesis. hydroxytamoxifen 23-41 peroxisome proliferator activated receptor delta Homo sapiens 149-157 16367757-3 2006 Here, we show that the 4-hydroxytamoxifen (4-OHT) mediated activation of a C-Raf-estrogen receptor fusion protein leads to the induction of both the PPARbeta and Cox-2 genes, concomitant with a dramatic increase in PGI2 synthesis. hydroxytamoxifen 23-41 mitochondrially encoded cytochrome c oxidase II Homo sapiens 162-167 16037132-13 2005 Finally, ERalpha dissociation from CHIP by various ERalpha ligands, including 17beta-estradiol, 4-hydroxytamoxifen, and ICI 182,780, interrupted CHIP-mediated ERalpha degradation. hydroxytamoxifen 96-114 estrogen receptor 1 Homo sapiens 9-16 16037132-13 2005 Finally, ERalpha dissociation from CHIP by various ERalpha ligands, including 17beta-estradiol, 4-hydroxytamoxifen, and ICI 182,780, interrupted CHIP-mediated ERalpha degradation. hydroxytamoxifen 96-114 estrogen receptor 1 Homo sapiens 51-58 16037132-13 2005 Finally, ERalpha dissociation from CHIP by various ERalpha ligands, including 17beta-estradiol, 4-hydroxytamoxifen, and ICI 182,780, interrupted CHIP-mediated ERalpha degradation. hydroxytamoxifen 96-114 estrogen receptor 1 Homo sapiens 51-58 16216906-5 2005 Evaluating the response to ER antagonists like 4-hydroxytamoxifen (OHT) and ICI 182 780 (ICI), we observed an up-regulation of ER beta and a dose-dependent inhibition of H295R cell proliferation. hydroxytamoxifen 47-65 estrogen receptor 2 Homo sapiens 127-134 16091424-4 2005 N-cadherin was fused at its C-terminus to a modified estrogen receptor ligand-binding domain (NcadER) that binds 4-hydroxytamoxifen (4OHT) and expressed in L cells, which lack an endogenous cadherin. hydroxytamoxifen 113-131 cadherin 2 Homo sapiens 0-10 16884532-0 2006 Characterization of tamoxifen and 4-hydroxytamoxifen glucuronidation by human UGT1A4 variants. hydroxytamoxifen 34-52 UDP glucuronosyltransferase family 1 member A4 Homo sapiens 78-84 16533026-10 2005 However, when 4-hydroxytamoxifen (100 microM) was used as the substrate, P450 2B6, P450 3A4, P450 3A5, P450 1B1, P450 1A1, and P450 2D6 all produced detectable concentrations of alpha,4-dihydroxytamoxifen. hydroxytamoxifen 14-32 cytochrome P450 family 1 subfamily B member 1 Homo sapiens 73-121 16093440-9 2005 Estradiol and 4-hydroxytamoxifen induction of endogenous ER-dependent gene expression (pS2 and c-myc) as well as ER-dependent reporter gene expression (ERE(2)e1b-luciferase) was also attenuated by MSA in all cell lines before effect on growth inhibition. hydroxytamoxifen 14-32 estrogen receptor 1 Homo sapiens 57-59 16093440-9 2005 Estradiol and 4-hydroxytamoxifen induction of endogenous ER-dependent gene expression (pS2 and c-myc) as well as ER-dependent reporter gene expression (ERE(2)e1b-luciferase) was also attenuated by MSA in all cell lines before effect on growth inhibition. hydroxytamoxifen 14-32 trefoil factor 1 Homo sapiens 87-90 16093440-9 2005 Estradiol and 4-hydroxytamoxifen induction of endogenous ER-dependent gene expression (pS2 and c-myc) as well as ER-dependent reporter gene expression (ERE(2)e1b-luciferase) was also attenuated by MSA in all cell lines before effect on growth inhibition. hydroxytamoxifen 14-32 MYC proto-oncogene, bHLH transcription factor Homo sapiens 95-100 16093440-10 2005 Taken together, these data strongly suggest that specific decrease in ER(alpha) levels by MSA is required for both MSA potentiation of the growth inhibitory effects of 4-hydroxytamoxifen and resensitization of tamoxifen-resistant cell lines. hydroxytamoxifen 168-186 estrogen receptor 1 Homo sapiens 70-72 15788686-0 2005 4-Hydroxytamoxifen inhibits proliferation of multiple myeloma cells in vitro through down-regulation of c-Myc, up-regulation of p27Kip1, and modulation of Bcl-2 family members. hydroxytamoxifen 0-18 MYC proto-oncogene, bHLH transcription factor Homo sapiens 104-109 15685451-6 2005 We, therefore, determined the effect of endoxifen and 4-OH-Tam on 17beta-estradiol (E2)-induced PR mRNA expression in an estrogen receptor-positive human breast cancer cell line. hydroxytamoxifen 54-62 progesterone receptor Homo sapiens 96-98 15685451-12 2005 When 10(-10) M E2 was used, induction of the PR expression was observed in 2 h and reached its maximum at 24 h. In this assay, neither endoxifen nor 4-OH-Tam alone produced any change in the PR mRNA expression. hydroxytamoxifen 149-157 progesterone receptor Homo sapiens 45-47 15685451-13 2005 However, both endoxifen and 4-OH-Tam decreased the E2-induced PR expression with similar potency. hydroxytamoxifen 28-36 progesterone receptor Homo sapiens 62-64 15828819-4 2005 The relative binding affinity values for estrogen receptor alpha (ERalpha) for n = 2 and 3 were very high (85 and 53%) and surpassed even that of hydroxytamoxifen (38.5%), the active metabolite of tamoxifen. hydroxytamoxifen 146-162 estrogen receptor 1 Homo sapiens 41-64 15828819-4 2005 The relative binding affinity values for estrogen receptor alpha (ERalpha) for n = 2 and 3 were very high (85 and 53%) and surpassed even that of hydroxytamoxifen (38.5%), the active metabolite of tamoxifen. hydroxytamoxifen 146-162 estrogen receptor 1 Homo sapiens 66-73 15828819-5 2005 Ruthenocene derivatives act as anti-estrogens as effective (n = 2) or slightly more effective (n = 3-5) than hydroxytamoxifen on ERalpha-positive breast cancer cell lines but, unlike ferrocifens, do not show antiproliferative effects on ERalpha-negative breast cancer cell lines. hydroxytamoxifen 109-125 estrogen receptor 1 Homo sapiens 129-136 15788686-0 2005 4-Hydroxytamoxifen inhibits proliferation of multiple myeloma cells in vitro through down-regulation of c-Myc, up-regulation of p27Kip1, and modulation of Bcl-2 family members. hydroxytamoxifen 0-18 cyclin dependent kinase inhibitor 1B Homo sapiens 128-135 15788686-0 2005 4-Hydroxytamoxifen inhibits proliferation of multiple myeloma cells in vitro through down-regulation of c-Myc, up-regulation of p27Kip1, and modulation of Bcl-2 family members. hydroxytamoxifen 0-18 BCL2 apoptosis regulator Homo sapiens 155-160 15728727-6 2005 In vivo, an engineered coactivator containing the peptide motif is able to strongly enhance the transcriptional activity of liganded ERalpha, particularly in the presence of 4-hydroxytamoxifen. hydroxytamoxifen 174-192 estrogen receptor 1 Homo sapiens 133-140 15737202-2 2005 After topical treatment with the inducing agent 4-hydroxytamoxifen (4OHT), ODC activity and putrescine levels were dramatically increased in the epidermis but not in the dermis of transgenic mice. hydroxytamoxifen 48-66 ornithine decarboxylase, structural 1 Mus musculus 75-78 15647843-3 2005 To address this issue, we have established M1/STAT3ER cells, where STAT3 is selectively activated by 4-hydroxytamoxifen (4HT). hydroxytamoxifen 101-119 signal transducer and activator of transcription 3 Mus musculus 46-51 15647843-3 2005 To address this issue, we have established M1/STAT3ER cells, where STAT3 is selectively activated by 4-hydroxytamoxifen (4HT). hydroxytamoxifen 101-119 signal transducer and activator of transcription 3 Mus musculus 67-72 15361836-5 2004 This construct, v-ErbB:ER, requires beta-estradiol or 4-OH tamoxifen for activation. hydroxytamoxifen 54-68 epidermal growth factor receptor Mus musculus 18-22 15595833-5 2004 To test the role of Nef oligomerization in Hck activation, we fused Nef to the hormone-binding domain of the estrogen receptor (Nef-ER), allowing us to control its dimerization with 4-hydroxytamoxifen (4-HT). hydroxytamoxifen 182-200 estrogen receptor 1 Homo sapiens 109-126 15588086-0 2004 Antiestrogen binding site and estrogen receptor mediate uptake and distribution of 4-hydroxytamoxifen-targeted doxorubicin-formaldehyde conjugate in breast cancer cells. hydroxytamoxifen 83-101 estrogen receptor 1 Homo sapiens 30-47 15588086-3 2004 We have recently reported the design, synthesis, and preliminary evaluation of a doxorubicin-formaldehyde conjugate targeted, via 4-hydroxytamoxifen, to the estrogen receptor (ER) and antiestrogen binding site (AEBS), which are commonly present in breast cancer cells. hydroxytamoxifen 130-148 estrogen receptor 1 Homo sapiens 157-174 15588086-3 2004 We have recently reported the design, synthesis, and preliminary evaluation of a doxorubicin-formaldehyde conjugate targeted, via 4-hydroxytamoxifen, to the estrogen receptor (ER) and antiestrogen binding site (AEBS), which are commonly present in breast cancer cells. hydroxytamoxifen 130-148 estrogen receptor 1 Homo sapiens 176-178 15588086-12 2004 The data support the hypothesis that uptake of 4-hydroxytamoxifen targeted doxorubicin-formaldehyde conjugate is mediated by both the antiestrogen binding site and estrogen receptor. hydroxytamoxifen 47-65 estrogen receptor 1 Homo sapiens 164-181 15531727-1 2004 The anti-estrogen 4-hydroxytamoxifen (TAM) and vitamin A-related compounds, the retinoids, in combination act synergistically to inhibit growth of breast cancer cells in vitro and in vivo. hydroxytamoxifen 18-36 Myeloproliferative syndrome, transient (transient abnormal myelopoiesis) Homo sapiens 38-41 15684716-8 2005 Expression of MybER, a 4-hydroxytamoxifen-activatable form of c-Myb, blocks differentiation in wildtype and APC mutant Immorto-cell lines as well as LIM1215 human colon carcinoma cells. hydroxytamoxifen 23-41 MYB proto-oncogene, transcription factor Homo sapiens 62-67 15375189-6 2005 These studies indicated that ER agonists, such as 17beta-estradiol or estrone, promoted the interaction of ER with the coactivator peptides, whereas antagonists such as 4-hydroxytamoxifen or ICI-182,780 did not. hydroxytamoxifen 169-187 estrogen receptor 1 Homo sapiens 29-31 15361836-5 2004 This construct, v-ErbB:ER, requires beta-estradiol or 4-OH tamoxifen for activation. hydroxytamoxifen 54-68 estrogen receptor 1 (alpha) Mus musculus 23-25 15317858-5 2004 Transfection of constitutive or 4-hydroxytamoxifen-inducible versions of Akt1 results in higher messenger RNA and protein levels of Cu/Zn-SOD. hydroxytamoxifen 32-50 AKT serine/threonine kinase 1 Homo sapiens 73-77 15351741-0 2004 SRA coactivation of estrogen receptor-alpha is phosphorylation-independent, and enhances 4-hydroxytamoxifen agonist activity. hydroxytamoxifen 89-107 steroid receptor RNA activator 1 Homo sapiens 0-3 15351741-0 2004 SRA coactivation of estrogen receptor-alpha is phosphorylation-independent, and enhances 4-hydroxytamoxifen agonist activity. hydroxytamoxifen 89-107 estrogen receptor 1 Homo sapiens 20-43 15351741-6 2004 SRA enhanced ERalpha activity stimulated by 4-hydroxytamoxifen, but was unable to convert this mixed antiestrogen to an ERbeta agonist. hydroxytamoxifen 44-62 steroid receptor RNA activator 1 Homo sapiens 0-3 15351741-6 2004 SRA enhanced ERalpha activity stimulated by 4-hydroxytamoxifen, but was unable to convert this mixed antiestrogen to an ERbeta agonist. hydroxytamoxifen 44-62 estrogen receptor 1 Homo sapiens 13-20 15525597-8 2004 These data demonstrated that the ERE sequence impacts estradiol-and 4-hydroxytamoxifen-occupied ERalpha and ERbeta interaction with coregulators as measured by transcriptional activity in mammalian cells. hydroxytamoxifen 68-86 estrogen receptor 1 Homo sapiens 96-103 15525597-8 2004 These data demonstrated that the ERE sequence impacts estradiol-and 4-hydroxytamoxifen-occupied ERalpha and ERbeta interaction with coregulators as measured by transcriptional activity in mammalian cells. hydroxytamoxifen 68-86 estrogen receptor 2 Homo sapiens 108-114 15304079-4 2004 The enzymatic activity of the PKCdelta catalytic domain fusion protein was induced in human keratinocytes treated with 4-hydroxytamoxifen, and its activation triggered loss of mitochondrial membrane potential and apoptosis. hydroxytamoxifen 119-137 protein kinase C delta Homo sapiens 30-38 15161930-0 2004 Structural basis for the deactivation of the estrogen-related receptor gamma by diethylstilbestrol or 4-hydroxytamoxifen and determinants of selectivity. hydroxytamoxifen 102-120 estrogen related receptor gamma Homo sapiens 45-76 15161930-2 2004 Although no natural ligand is known, ERRgamma is deactivated by the estrogen receptor (ER) agonist diethylstilbestrol and the selective ER modulator 4-hydroxytamoxifen but does not significantly respond to estradiol or raloxifene. hydroxytamoxifen 149-167 estrogen related receptor gamma Homo sapiens 37-45 15161930-3 2004 Here we report the crystal structures of the ERRgamma ligand binding domain (LBD) complexed with diethylstilbestrol or 4-hydroxytamoxifen. hydroxytamoxifen 119-137 estrogen related receptor gamma Homo sapiens 45-53 15161930-7 2004 Comparison of the ligand-bound LBDs of ERRgamma and ERalpha reveals small but significant differences in the architecture of the ligand binding pockets that result in a slightly shifted binding position of diethylstilbestrol and a small rotation of 4-hydroxytamoxifen in the cavity of ERRgamma relative to ERalpha. hydroxytamoxifen 249-267 estrogen related receptor gamma Homo sapiens 39-47 15161930-7 2004 Comparison of the ligand-bound LBDs of ERRgamma and ERalpha reveals small but significant differences in the architecture of the ligand binding pockets that result in a slightly shifted binding position of diethylstilbestrol and a small rotation of 4-hydroxytamoxifen in the cavity of ERRgamma relative to ERalpha. hydroxytamoxifen 249-267 estrogen receptor 1 Homo sapiens 52-59 15161930-7 2004 Comparison of the ligand-bound LBDs of ERRgamma and ERalpha reveals small but significant differences in the architecture of the ligand binding pockets that result in a slightly shifted binding position of diethylstilbestrol and a small rotation of 4-hydroxytamoxifen in the cavity of ERRgamma relative to ERalpha. hydroxytamoxifen 249-267 estrogen related receptor gamma Homo sapiens 285-293 15161930-7 2004 Comparison of the ligand-bound LBDs of ERRgamma and ERalpha reveals small but significant differences in the architecture of the ligand binding pockets that result in a slightly shifted binding position of diethylstilbestrol and a small rotation of 4-hydroxytamoxifen in the cavity of ERRgamma relative to ERalpha. hydroxytamoxifen 249-267 estrogen receptor 1 Homo sapiens 306-313 15386482-0 2004 Interactions of tamoxifen, N-desmethyltamoxifen and 4-hydroxytamoxifen with P-glycoprotein and CYP3A. hydroxytamoxifen 52-70 ATP binding cassette subfamily B member 1 Homo sapiens 76-90 15386482-0 2004 Interactions of tamoxifen, N-desmethyltamoxifen and 4-hydroxytamoxifen with P-glycoprotein and CYP3A. hydroxytamoxifen 52-70 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 95-100 15386482-1 2004 The effects of tamoxifen, N-desmethyltamoxifen and 4-hydroxytamoxifen on transport attributable to P-glycoprotein were studied using Caco-2 cell monolayers in a transwell system, with rhodamine-123 as an index substrate for inhibition studies. hydroxytamoxifen 51-69 ATP binding cassette subfamily B member 1 Homo sapiens 99-113 15313422-5 2004 In human cancer cells, inhibition of HDACs controls the expression of the ERalpha gene and the transcriptional activity in response to partial antiestrogens such as 4-hydroxytamoxifen. hydroxytamoxifen 165-183 estrogen receptor 1 Homo sapiens 74-81 15316080-4 2004 To investigate FOXN1 function we expressed an inducible form of the protein, FOXN1ER, that is activated by 4-hydroxytamoxifen in primary human epidermal keratinocytes. hydroxytamoxifen 107-125 forkhead box N1 Homo sapiens 15-20 15317858-5 2004 Transfection of constitutive or 4-hydroxytamoxifen-inducible versions of Akt1 results in higher messenger RNA and protein levels of Cu/Zn-SOD. hydroxytamoxifen 32-50 superoxide dismutase 1 Homo sapiens 132-141 15280403-9 2004 VEGF-D expression was enhanced by oestrogen in MCF-7 and T47D breast cancer cells, and was blocked by hydroxytamoxifen. hydroxytamoxifen 102-118 vascular endothelial growth factor D Homo sapiens 0-6 15067010-5 2004 In culture with stem cell factor, FLT3 ligand, and IL-6, a 4-hydroxytamoxifen-inducible form of c-Myc (Myc/ERT) enabled murine Lin(-)Sca-1(+) HSCs to proliferate with the surface phenotype compatible with HSCs for more than 28 days. hydroxytamoxifen 59-77 kit ligand Mus musculus 16-32 15245432-7 2004 Cyclin D2 expression was enhanced by antiestrogens, ICI 182,780 and 4-hydroxytamoxifen, and membrane-impermeable bovine serum albumin-conjugated E2, indicating the effects via membrane E2-binding sites. hydroxytamoxifen 68-86 cyclin D2 Homo sapiens 0-9 15056732-4 2004 A kinase assay showed that antiestrogens (4-hydroxytamoxifen and ICI 182.780) rapidly induce p38 activity. hydroxytamoxifen 42-60 mitogen-activated protein kinase 14 Homo sapiens 93-96 15067010-5 2004 In culture with stem cell factor, FLT3 ligand, and IL-6, a 4-hydroxytamoxifen-inducible form of c-Myc (Myc/ERT) enabled murine Lin(-)Sca-1(+) HSCs to proliferate with the surface phenotype compatible with HSCs for more than 28 days. hydroxytamoxifen 59-77 FMS-like tyrosine kinase 3 Mus musculus 34-38 15067010-5 2004 In culture with stem cell factor, FLT3 ligand, and IL-6, a 4-hydroxytamoxifen-inducible form of c-Myc (Myc/ERT) enabled murine Lin(-)Sca-1(+) HSCs to proliferate with the surface phenotype compatible with HSCs for more than 28 days. hydroxytamoxifen 59-77 interleukin 6 Mus musculus 51-55 15067010-5 2004 In culture with stem cell factor, FLT3 ligand, and IL-6, a 4-hydroxytamoxifen-inducible form of c-Myc (Myc/ERT) enabled murine Lin(-)Sca-1(+) HSCs to proliferate with the surface phenotype compatible with HSCs for more than 28 days. hydroxytamoxifen 59-77 myelocytomatosis oncogene Mus musculus 98-101 15067010-5 2004 In culture with stem cell factor, FLT3 ligand, and IL-6, a 4-hydroxytamoxifen-inducible form of c-Myc (Myc/ERT) enabled murine Lin(-)Sca-1(+) HSCs to proliferate with the surface phenotype compatible with HSCs for more than 28 days. hydroxytamoxifen 59-77 myelocytomatosis oncogene Mus musculus 103-106 15067010-5 2004 In culture with stem cell factor, FLT3 ligand, and IL-6, a 4-hydroxytamoxifen-inducible form of c-Myc (Myc/ERT) enabled murine Lin(-)Sca-1(+) HSCs to proliferate with the surface phenotype compatible with HSCs for more than 28 days. hydroxytamoxifen 59-77 SH2 domain containing 1B2 Mus musculus 107-110 15067010-6 2004 c-Myc activated by 4-hydroxytamoxifen augmented telomerase activities and increased the number of CFU-Mix about 2-fold in colony assays. hydroxytamoxifen 19-37 myelocytomatosis oncogene Mus musculus 2-5 15174161-3 2004 Photocaged derivatives of hydroxytamoxifen (NB-Htam) and guanidine tamoxifen (NB-Gtam) have been synthesized that selectively antagonize ER alpha- and ER beta-mediated transcription at classic estrogen response elements (EREs) in response to light. hydroxytamoxifen 26-42 estrogen receptor 1 Homo sapiens 137-145 15174161-3 2004 Photocaged derivatives of hydroxytamoxifen (NB-Htam) and guanidine tamoxifen (NB-Gtam) have been synthesized that selectively antagonize ER alpha- and ER beta-mediated transcription at classic estrogen response elements (EREs) in response to light. hydroxytamoxifen 26-42 estrogen receptor 2 Homo sapiens 151-158 15157572-11 2004 The estrogen receptor antagonist 4-hydroxytamoxifen could attenuate these inhibitive effects of both E2 and ZEA. hydroxytamoxifen 33-51 cystatin 12, pseudogene Homo sapiens 101-111