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

作者：Tamura Satoru; Kaneko Masafumi; Shiomi Atsushi; Yang Guang Ming; Yamaura Toshiaki; Murakami Nobutoshi^*

来源：Bioorganic & Medicinal Chemistry Letters, 2010, 20(6): 1837-1839.

DOI：10.1016/j.bmcl.2010.01.165

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

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.

• 出版日期2010-3-15