New Hedgehog/GLI signaling inhibitors from Excoecaria agallocha

Yusnita Rifai, Midori A. Arai, Samir K. Sadhu, Firoj Ahmed, Masami Ishibashi

研究成果: Article査読

44 被引用数 (Scopus)

抄録

The inhibition of the Hedgehog (Hh) signaling pathway has emerged as an anti-cancer strategy. Three flavonoid glycosides including 2 new compounds (1-2) were isolated from Excoecaria agallocha as Hedgehog/GLI1-mediated transcriptional inhibitors and exhibited cytotoxicity against human pancreatic (PANC1) and prostate (DU145) cancer cells. Our data revealed that compound 1 clearly inhibited the expression of GLI-related proteins (PTCH and BCL-2) and blocked the translocation of GLI1 transcription factors into the nucleus in PANC1. Deleting the Smoothened (Smo) function in PANC1 treated with 1 led to downregulation of the mRNA expression of Ptch. This study describes the first Hh signaling inhibitor which blocks GLI1 movement into the nucleus without interfering with Smo.

本文言語English
ページ(範囲)718-722
ページ数5
ジャーナルBioorganic and Medicinal Chemistry Letters
21
2
DOI
出版ステータスPublished - 2011 1月 15
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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