通过神经干细胞分化激活剂的靶向蛋白质导向天然产物分离（TPO-NAPI）分离得到的Hes1抑制剂。
Hes1 inhibitor isolated by target protein oriented natural products isolation (TPO-NAPI) of differentiation activators of neural stem cells.
作者信息
Arai Midori A, Ishikawa Naoki, Tanaka Mitsuha, Uemura Kenji, Sugimitsu Noriko, Suganami Akiko, Tamura Yutaka, Koyano Takashi, Kowithayakorn Thaworn, Ishibashi Masami
机构信息
Graduate School of Pharmaceutical Sciences , Chiba University , 1-8-1 Inohana, Chuo-ku , Chiba 260-8675 , Japan . Email:
Graduate School of Medicine , Chiba University , 1-8-1 Inohana, Chuo-ku , Chiba 260-8670 , Japan.
出版信息
Chem Sci. 2016 Feb 1;7(2):1514-1520. doi: 10.1039/c5sc03540f. Epub 2015 Dec 1.
The Hes1 dimer inhibitor, agalloside (), which can accelerate the differentiation of neural stem cells is described. Six natural products, including one new natural product, which bind to Hes1 were rapidly isolated by a developed "target protein oriented natural products isolation" (TPO-NAPI) method using Hes1-immobilized beads. Of the six compounds, inhibited Hes1 dimer formation at both the protein- and cellular level. Neural stem cells treated with differentiated to neurons with longer neurites than cells treated with varproic acid or retinoic acid. Moreover, exhibited specificity for neurons. This promotion of differentiation was supported by an increase in the mRNA expression of the proneural genes, and , which were inhibited by Hes1.
描述了一种可加速神经干细胞分化的Hes1二聚体抑制剂——刺五加苷（）。通过使用固定有Hes1的磁珠的先进“靶向蛋白质导向天然产物分离”（TPO-NAPI）方法，快速分离出六种与Hes1结合的天然产物，其中包括一种新的天然产物。在这六种化合物中， 在蛋白质和细胞水平上均抑制Hes1二聚体的形成。用 处理的神经干细胞分化为神经元时，其神经突比用丙戊酸或视黄酸处理的细胞更长。此外， 对神经元具有特异性。神经源性基因 和 的mRNA表达增加支持了这种分化促进作用，而这两种基因的表达受到Hes1的抑制。
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