The first Hes1 dimer inhibitors from natural products

被引：23
作者：
Arai, Midori A. [1 ]
Masada, Ayako [1 ]
Ohtsuka, Toshiyuki [2 ]
Kageyama, Ryoichiro [2 ]
Ishibashi, Masami [1 ]
机构：
[1] Chiba Univ, Grad Sch Pharmaceut Sci, Chiba 2638522, Japan
[2] Kyoto Univ, Inst Virus Res, Sakyo Ku, Kyoto 6068507, Japan
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 19期
基金：
日本学术振兴会;
关键词：
Neural stem cells; bHLH; Hes1; Inhibitor; High-throughput screening; MYXOMYCETE LINDBLADIA-TUBULINA; LYCOGALA-EPIDENDRUM; NEURONAL DIFFERENTIATION; NAPHTHOQUINONE PIGMENTS; BISINDOLE ALKALOIDS; PROGENITOR CELLS; STEM-CELLS; CONSTITUENTS; RECRUITMENT; GLYCOSIDES;
D O I：
10.1016/j.bmcl.2009.07.146
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
In the present study, we developed a high-throughput screening system for small molecule-inhibitors of the basic helix-loop-helix (bHLH) transcriptional repressor factor Hes1. Successful dimerization of Hes1 immobilized on a microplate and fluorophore (Cy3)-labelled Hes1 was confirmed. Using this system, several natural products were identified as the first Hes1 dimer inhibitors. Of these, two compounds which were isolated from myxomycetes (true slime molds) inhibited Hes1 from N box-dependent suppression of the gene expression in C3H10T1/2 cells. (C) 2009 Published by Elsevier Ltd.
引用
收藏
页码：5778 / 5781
页数：4
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