作为雌激素受体介导转录抑制剂的细胞穿透性R7片段缀合螺旋肽的开发。
Development of cell-penetrating R7 fragment-conjugated helical peptides as inhibitors of estrogen receptor-mediated transcription.
作者信息
Nagakubo Takaya, Demizu Yosuke, Kanda Yasunari, Misawa Takashi, Shoda Takuji, Okuhira Keiichiro, Sekino Yuko, Naito Mikihiko, Kurihara Masaaki
机构信息
National Institute of Health Sciences , Tokyo 158-8501, Japan.
出版信息
Bioconjug Chem. 2014 Nov 19;25(11):1921-4. doi: 10.1021/bc500480e. Epub 2014 Nov 7.
The heptaarginine (R7)-conjugated peptide 5 was designed and synthesized as an inhibitor of ER-coactivator interactions and ER-mediated transcription at the cellular level. The R7-conjugated peptide 5 was able to enter ER-positive T47D cells efficiently, and treatment with 3 μM of 5 downregulated the mRNA expression of pS2 (an ER-mediated gene) by 87%.
七聚精氨酸（R7）缀合肽5被设计并合成为一种在细胞水平上抑制雌激素受体（ER）-共激活因子相互作用和ER介导转录的抑制剂。R7缀合肽5能够有效地进入ER阳性的T47D细胞，用3 μM的肽5处理可使pS2（一种ER介导的基因）的mRNA表达下调87%。
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