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査読

19 被引用数 (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.

本文言語English
ページ(範囲)303-311
ページ数9
ジャーナルJournal of Antibiotics
61
5
DOI
出版ステータスPublished - 2008 5

ASJC Scopus subject areas

  • 薬理学
  • 創薬

フィンガープリント

「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」の研究トピックを掘り下げます。これらがまとまってユニークなフィンガープリントを構成します。

引用スタイル