Unprecedented NES non-antagonistic inhibitor for nuclear export of Rev from 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.
Tamura
Satoru
S
Graduate School of Pharmaceutical Sciences, Osaka University, Suita, Osaka, Japan.
Kaneko
Masafumi
M
Shiomi
Atsushi
A
Yang
Guang-Ming
GM
Yamaura
Toshiaki
T
Murakami
Nobutoshi
N
D002851:Chromatography, High Pressure Liquid; D015694:Gene Products, rev / Q000378:metabolism*; D019660:Malvaceae / Q000378:metabolism*; D049790:Nuclear Export Signals; D010936:Plant Extracts / Q000494:pharmacology*; D021381:Protein Transport / Q000187:drug effects*
D015694:Gene Products, rev; D049790:Nuclear Export Signals; D010936:Plant Extracts