A novel action of terpendole E on the motor activity of mitotic kinesin Eg5

Junko Nakazawa, Junichiro Yajima, Takeo Usui, Masashi Ueki, Akira Takatsuki, Masaya Imoto, Yoko Y. Toyoshima, Hiroyuki Osada

研究成果: Article査読

100 被引用数 (Scopus)

抄録

To reveal the mechanism of mitosis, the development of M phase-specific inhibitors is an important strategy. We have been screening microbial products to find specific M phase inhibitors that do not directly target tubulins, and rediscovered terpendole E (TerE) as a novel Eg5 inhibitor. TerE did not affect microtubule integrity in interphase, but induced formation of a monoastral spindle in M phase. TerE inhibited both motor and microtubule-stimulated ATPase activities of human Eg5, but did not affect conventional kinesin from either Drosophila or bovine brain. Although terpendoles have been reported as inhibitors of acyl-CoA:cholesterol O-acyltransferase (ACAT), the Eg5 inhibitory activity of TerE was independent of ACAT inhibition. Taken together, we demonstrate that TerE is a novel Eg5 inhibitor isolated from a fungal strain.

本文言語English
ページ(範囲)131-137
ページ数7
ジャーナルChemistry and Biology
10
2
DOI
出版ステータスPublished - 2003 2月 1
外部発表はい

ASJC Scopus subject areas

  • 生化学
  • 分子医療
  • 分子生物学
  • 薬理学
  • 創薬
  • 臨床生化学

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