Unprecedented NES non-antagonistic inhibitor for nuclear export of Rev from Sida cordifolia
作者:Satoru Tamura、Masafumi Kaneko、Atsushi Shiomi、Guang-Ming Yang、Toshiaki Yamaura、Nobutoshi Murakami
DOI:10.1016/j.bmcl.2010.01.165
日期:2010.3
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. (C) 2010 Elsevier Ltd. All rights reserved.