Unprecedented NES non-antagonistic inhibitor for nuclear export of Rev from Sida cordifolia - PubMed (original) (raw)

. 2010 Mar 15;20(6):1837-9.

doi: 10.1016/j.bmcl.2010.01.165. Epub 2010 Feb 6.

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

Satoru Tamura et al. Bioorg Med Chem Lett. 2010.

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.

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