Hes1-Binding Compounds Isolated by Target Protein Oriented Natural Products Isolation (TPO-NAPI)

Midori A. Arai, Mitsuha Tanaka, Kana Tanouchi, Naoki Ishikawa, Firoj Ahmed, Samir K. Sadhu, Masami Ishibashi

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

Hairy and enhancer of split 1 (Hes1) is a transcription factor that acts in neural stem cells to inhibit differentiation. We recently developed target protein oriented natural products isolation (TPO-NAPI) using Hes1-immobilized beads to identify activators of neural stem cells. Isomicromonolactam (1), staurosporin (2), and linarin (3) were isolated as Hes1-binding compounds using the TPO-NAPI method. Of these, compound 1 enhanced neural stem cell differentiation. Using truncated Hes1 proteins, the binding region of Hes1 for 1 was estimated to be in the C-terminal half that includes a TLE/Grg binding site. The differentiation-promoting activity of inohanamine (4) is also reported.

Original languageEnglish
Pages (from-to)538-543
Number of pages6
JournalJournal of Natural Products
Volume80
Issue number2
DOIs
Publication statusPublished - 2017 Feb 24
Externally publishedYes

ASJC Scopus subject areas

  • Analytical Chemistry
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Complementary and alternative medicine
  • Organic Chemistry

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