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4-Hydroxytamoxifen是tamoxifen的活性代谢产物,是一种选择性的雌激素受体调节分子,在乳腺癌的治疗和化学疗法中应用广泛化疗药物它莫西芬的代谢产物,抑制许多潜在雌激素的活性,也能激活如膜间脂质过氧化反应的抑制剂。 4-hydroxytamoxifen (OHT), an active metabolite of tamoxifen, is a selective estrogen receptor mo...
Lim YC, Li L, Desta Z, Zhao Q, Rae JM, Flockhart DA, et al. Endoxifen, a secondary metabolite of tamoxifen, and 4-OH-tamoxifen induce similar changes in global gene expression patterns in MCF-7 breast cancer cells. J Pharmacol Exp Ther 2006;318:503-12....
Effect of PUGNAc+GlcN on ESR1 promoter and ER伪 expression in presence of 4-OH-tamoxifen. (A) MCF-7 cells were co-transfected with ESR1 promoter-Firefly luciferase reporter gene (ESR1-luc) and Renilla luciferase cDNAs. 12 hours after tra... Y Fardini,E Masson,O Boudah,... - 《Diabet...
Coopman P, Garcia M, Brunner N, Derocq D, Clarke R, Rochefort H. Anti-proliferative and anti-estrogenic effects of ICI 164,384 and ICI 182,780 in 4-OH-tamoxifen-resistant human breast-cancer cells. Int J Cancer 1994;56:295–300....
Protection of MCF-7 cells from 4-OH-tamoxifen-induced cell death is not abrogated by inhibition of the PI-3 kinase/Akt pathway.Shahzina, KanwalYann, FardiniPatrick, PagesyThierry, N’TumbaBynCécile, PierreEugeneElodie, MassonCornelia, Hampe...
IGF-1 treatment does not protect MCF-7 cells from 4OH-tamoxifen-induced cell death.Shahzina KanwalYann FardiniPatrick PagesyThierry N’TumbaBynCécile PierreEugeneElodie MassonCornelia HampeTarik Issad
Pharmacological characterization of 4-hydroxy-N-desmethyl tamoxifen, a novel active metabolite of tamoxifen . Breast Cancer Res Treat 2004 ; 85 : 151 - 159 .Pharmacological Characterization of 4-hydroxy-N-desmethyl Tamoxifen, a Novel Active Metabolite of Tamoxifen[J] . Michael D. Johnson,Hong Zuo...
PUGNAc+GlcNAc treatment inhibited the effect of 4-OH-tamoxifen on p21 and Egr1 gene expression.Shahzina, KanwalYann, FardiniPatrick, PagesyThierry, N’TumbaBynCécile, PierreEugeneElodie, MassonCornelia, HampeTarik, Issad
TAMOXIFENCANCER cellsMETABOLITESApproximately 80% of breast cancer (BC) cases are estrogen receptor positive (ER+) and sensitive to hormone treatment; Tamoxifen is a prodrug, and its main plasmatic active metabolites are 4-hydroxytamoxifen (4-OH Tam) and endoxifen. Despite the effectiveness of ...