4-Hydroxytamoxifen作為雌激素受體拮抗劑的基因調控機制
4-Hydroxytamoxifen（4-OHT，AbMole，M10252）是一種選擇性雌激素受體調節(jié)劑（SERM），在研究中主要作為雌激素受體拮抗劑發(fā)揮作用，其作用機制涉及抑制雌激素受體活性并影響轉錄因子的招募[1, 2]。4-Hydroxytamoxifen在細胞實驗中，常用于人乳腺癌細胞系（如MCF-7、MDA-MB 231、T-47D）的研究，例如通過濃度梯度誘導細胞以（100-1000 nM）建立耐藥細胞模型（如MCF-7-TamR）[3]。4-Hydroxytamoxifen在MCF-7細胞中，可顯著抑制細胞增殖并調控凋亡相關基因的表達[3]。4-Hydroxytamoxifen（ CAS No.：68047-06-3）在分子與細胞生物學中還是一種可以調控外源基因表達的常用化合物，例如4-Hydroxytamoxifen通過激活CreER-T2酶，介導loxP位點特異性重組，實現外源基因在轉基因小鼠模型中的條件性敲除或表達。
在動物實驗中，4-Hydroxytamoxifen通過腹腔注射用于雙轉基因Cspg4-cre/Esr1/ROSA26Sortm14(CAG-tdTomato)小鼠模型，誘導重組并觸發(fā)紅色熒光蛋白表達[4]。4-Hydroxytamoxifen還可用于動物腫瘤模型和某些病毒模型，常見于小鼠實驗。例如4-Hydroxytamoxifen（4-OHT，AbMole，M10252）在異種移植或同種移植腫瘤模型中，被用于評估抗腫瘤效果。在VSV（水皰性口炎病毒）模型中，4-Hydroxytamoxifen作為小分子誘導劑，可激活Intein剪接以調節(jié)病毒復制[5]。
參考文獻及鳴謝
[1] Shtaiwi, A.; Adnan, R.; Khairuddean, M.; et al. Computational investigations of the binding mechanism of novel benzophenone imine inhibitors for the treatment of breast cancer. RSC advances 2019, 9 (61), 35401-35416.
[2] Somsen, B. A.; Sijbesma, E.; Leysen, S.; et al. Molecular basis and dual ligand regulation of tetrameric estrogen receptor alpha/14-3-3zeta protein complex. The Journal of biological chemistry 2023, 299 (7), 104855.
[3] Cheng, S.; Castillo, V.; Welty, M.; et al. BreastDefend enhances effect of tamoxifen in estrogen receptor-positive human breast cancer in vitro and in vivo. BMC complementary and alternative medicine 2017, 17 (1), 115.
[4] Valny, M.; Honsa, P.; Kirdajova, D.; et al. Tamoxifen in the Mouse Brain: Implications for Fate-Mapping Studies Using the Tamoxifen-Inducible Cre-loxP System. Frontiers in cellular neuroscience 2016, 10, 243.
[5] Zhao, Z.; Wang, B.; Wu, S.; et al. Regulated control of virus replication by 4-hydroxytamoxifen-induced splicing. Frontiers in microbiology 2023, 14, 1112580.
在動物實驗中，4-Hydroxytamoxifen通過腹腔注射用于雙轉基因Cspg4-cre/Esr1/ROSA26Sortm14(CAG-tdTomato)小鼠模型，誘導重組并觸發(fā)紅色熒光蛋白表達[4]。4-Hydroxytamoxifen還可用于動物腫瘤模型和某些病毒模型，常見于小鼠實驗。例如4-Hydroxytamoxifen（4-OHT，AbMole，M10252）在異種移植或同種移植腫瘤模型中，被用于評估抗腫瘤效果。在VSV（水皰性口炎病毒）模型中，4-Hydroxytamoxifen作為小分子誘導劑，可激活Intein剪接以調節(jié)病毒復制[5]。
參考文獻及鳴謝
[1] Shtaiwi, A.; Adnan, R.; Khairuddean, M.; et al. Computational investigations of the binding mechanism of novel benzophenone imine inhibitors for the treatment of breast cancer. RSC advances 2019, 9 (61), 35401-35416.
[2] Somsen, B. A.; Sijbesma, E.; Leysen, S.; et al. Molecular basis and dual ligand regulation of tetrameric estrogen receptor alpha/14-3-3zeta protein complex. The Journal of biological chemistry 2023, 299 (7), 104855.
[3] Cheng, S.; Castillo, V.; Welty, M.; et al. BreastDefend enhances effect of tamoxifen in estrogen receptor-positive human breast cancer in vitro and in vivo. BMC complementary and alternative medicine 2017, 17 (1), 115.
[4] Valny, M.; Honsa, P.; Kirdajova, D.; et al. Tamoxifen in the Mouse Brain: Implications for Fate-Mapping Studies Using the Tamoxifen-Inducible Cre-loxP System. Frontiers in cellular neuroscience 2016, 10, 243.
[5] Zhao, Z.; Wang, B.; Wu, S.; et al. Regulated control of virus replication by 4-hydroxytamoxifen-induced splicing. Frontiers in microbiology 2023, 14, 1112580.
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乳腺癌
