New Rev-export inhibitor from Alpinia galanga and structure–activity relationship

…, M Kaneko, Y Ye, M Yoshida, M Yoshikawa…

Index: Tamura, Satoru; Shiomi, Atsushi; Kaneko, Masafumi; Ye, Ying; Yoshida, Minoru; Yoshikawa, Masayuki; Kimura, Tominori; Kobayashi, Motomasa; Murakami, Nobutoshi Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 9 p. 2555 - 2557

Full Text: HTML

Citation Number: 24

Abstract

Bioassay-guided separation by use of the fission yeast expressing NES of Rev, an HIV-1 viral regulatory protein, disclosed 1′-acetoxychavicol acetate (ACA, 1) as a new inhibitor for nuclear export of Rev from the roots of Alpinia galanga. Both analysis for mechanism of action with biotinylated probe (2) and several synthesized analogs established crucial portions in 1 for Rev-export inhibitory activity.