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

Research output: Contribution to journalArticlepeer-review

88 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)131-137
Number of pages7
JournalChemistry and Biology
Volume10
Issue number2
DOIs
Publication statusPublished - 2003 Feb 1

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmacology
  • Drug Discovery
  • Clinical Biochemistry

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