The first Hes1 dimer inhibitors from natural products

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

Research output: Contribution to journalArticle

20 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)5778-5781
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number19
DOIs
Publication statusPublished - 2009 Oct 1
Externally publishedYes

Keywords

  • bHLH
  • Hes1
  • High-throughput screening
  • Inhibitor
  • Neural stem cells

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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