Unprecedented NES non-antagonistic inhibitor for nuclear export of Rev from Sida cordifolia

Satoru Tamura, Masafumi Kaneko, Atsushi Shiomi, Guang Ming Yang, Toshiaki Yamaura, Nobutoshi Murakami

Research output: Contribution to journalArticlepeer-review

12 Citations (Scopus)

Abstract

Bioassay-guided separation from the MeOH extract of the South American medicinal plant Sida cordifolia resulted in isolation of (10E,12Z)-9-hydroxyoctadeca-10,12-dienoic acid (1) as an unprecedented NES non-antagonistic inhibitor for nuclear export of Rev. This mechanism of action was established by competitive experiment by the biotinylated probe derived from leptomycin B, the known NES antagonistic inhibitor. Additionally, structure-activity relationship analysis by use of the synthesized analogs clarified cooperation of several functionalities in the Rev-export inhibitory activity of 1.

Original languageEnglish
Pages (from-to)1837-1839
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number6
DOIs
Publication statusPublished - 2010 Mar 15

Keywords

  • (10E,12Z)-9-hydroxyoctadeca-10,12-dienoic acid
  • Anti-HIV
  • NES non-antagonistic inhibitor
  • Rev-export inhibitor
  • Sida cordifolia

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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