Trierixin, a novel inhibitor of ER stress-induced XBP1 activation from Streptomyces sp. I. Taxonomy, fermentation, isolation, and biological activities

Etsu Tashiro, Naoka Hironiwa, Mitsuhiro Kitagawa, Yushi Futamura, Shin Ichi Suzuki, Maki Nishio, Masaya Imoto

研究成果: Article査読

37 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, trierixin, from a culture broth of Streptomyces sp. AC 654. Trierixin was purified by column chromatography on silica gel and by HPLC. The molecular formula of trierixin is C37H52N2O8S. Trierixin inhibited thapsigargin-induced XBP1-luciferase activation in HeLa/XBP1-luc cells and endogenous XBP1 splicing in HeLa cells with an IC 50 of 14 ng/ml and 19 ng/ml, respectively. Moreover, in the process of isolating trierixin, we isolated structurally related mycotrienin II and trienomycin A as inhibitors of ER stress-induced XBP1 activation from a culture broth of a trierixin-producing strain. This study provides the first observation that triene-ansamycins have a novel inhibitory effect against XBP1 activation.

本文言語English
ページ(範囲)547-553
ページ数7
ジャーナルJournal of Antibiotics
60
9
DOI
出版ステータスPublished - 2007 9

ASJC Scopus subject areas

  • 薬理学
  • 創薬

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