The first Hes1 dimer inhibitors from natural products

Midori A. Arai, Ayako Masada, Toshiyuki Ohtsuka, Ryoichiro Kageyama, Masami Ishibashi

研究成果: Article査読

25 被引用数 (Scopus)

抄録

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.

本文言語English
ページ(範囲)5778-5781
ページ数4
ジャーナルBioorganic and Medicinal Chemistry Letters
19
19
DOI
出版ステータスPublished - 2009 10月 1
外部発表はい

ASJC Scopus subject areas

  • 生化学
  • 分子医療
  • 分子生物学
  • 薬科学
  • 創薬
  • 臨床生化学
  • 有機化学

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