SAR study of a novel triene-ansamycin group compound, quinotrierixin, and related compounds, as inhibitors of ER stress-induced XBP1 activation I. Taxonomy, fermentation, isolation, biological activities and SAR study

Tatsuro Kawamura, Etsu Tashiro, Kohta Yamamoto, Kazutoshi Shindo, Masaya Imoto

研究成果: Article

17 引用 (Scopus)

抄録

In the course of screening for an inhibitor of ER stress-induced XBP1 activation, we isolated a new member of the triene-ansamycin group compound, quinotrierixin, from a culture broth of Streptomyces sp. PAE37. Quinotrierixin inhibited thapsigargin-induced XBP1 activation in HeLa cells with an IC 50 of 0.067 μM. We found that other triene-ansamycin group compounds such as demethyltrienomycin A and mycotrienin I also inhibited ER stress-induced XBP1 activation. Moreover, we performed SAR study of twelve triene-ansamycin group compounds. The study showed that OH group at C-13 was crucial, and CH3 group at C-14 would be important for the XBP1 inhibitory activity.

元の言語English
ページ(範囲)303-311
ページ数9
ジャーナルJournal of Antibiotics
61
発行部数5
DOI
出版物ステータスPublished - 2008 5

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Rifabutin
Fermentation
Thapsigargin
Streptomyces
HeLa Cells
quinotrierixin

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

これを引用

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AU - Tashiro, Etsu

AU - Yamamoto, Kohta

AU - Shindo, Kazutoshi

AU - Imoto, Masaya

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