New Rev-export inhibitor from Alpinia galanga and structure-activity relationship.
New Rev-export inhibitor from Alpinia galanga and structure-activity relationship.
复制标题
DOI：
10.1016/j.bmcl.2009.03.047
复制
发表时间：
2009-05
影响因子：
2.7
通讯作者：
S. Tamura;A. Shiomi;M. Kaneko;Y. Ye;Minoru Yoshida;M. Yoshikawa;Tominori Kimura;Motomasa Kobayashi;N. Murakami
中科院分区：
文献类型：
--
作者：
S. Tamura;A. Shiomi;M. Kaneko;Y. Ye;Minoru Yoshida;M. Yoshikawa;Tominori Kimura;Motomasa Kobayashi;N. Murakami
利用表达HIV-1病毒调节蛋白Rev的内斯的裂殖酵母进行生物测定导向分离，发现1′-乙酰氧基胡椒酚乙酸酯（ACA，1）是大高良姜根中Rev核输出的新抑制剂。用生物素化探针（2）和几种合成的类似物对作用机制的分析都建立了1中Rev-输出抑制活性的关键部分。
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.