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

doi:10.1016/j.bmcl.2010.01.165

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

Bioorg Med Chem Lett. 2010 Mar 15;20(6):1837-9. doi: 10.1016/j.bmcl.2010.01.165. Epub 2010 Feb 6.

Authors

Satoru Tamura¹, Masafumi Kaneko, Atsushi Shiomi, Guang-Ming Yang, Toshiaki Yamaura, Nobutoshi Murakami

Affiliation

¹ Graduate School of Pharmaceutical Sciences, Osaka University, Suita, Osaka, Japan.

PMID: 20176483
DOI: 10.1016/j.bmcl.2010.01.165

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Chromatography, High Pressure Liquid
Gene Products, rev / metabolism*
Malvaceae / metabolism*
Nuclear Export Signals*
Plant Extracts / pharmacology*
Protein Transport / drug effects*

Substances

Gene Products, rev
Nuclear Export Signals
Plant Extracts