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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Deoxyverrucosidin,a Novel GRP78/BiP Down-regulator,Produced by Penicillium sp.
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Deoxyverrucosidin,a Novel GRP78/BiP Down-regulator,Produced by Penicillium sp.

机译:Deoxyverrucosidin,一种新型的GRP78 / BiP下调剂,由Penicillium sp。生产。

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摘要

Glucose-regulated protein 78 (GRP78) resides in endoplasmic reticulum (ER) and plays a role in protecting tumor cells against the toxic effects of anticancer agents.During the search for down-regulators of GRP78 using a reporter gene (luciferase) assay system,we isolated a novel compound designated as deoxyverrucosidin (1),a congener of verrucosidin (2),from Penicillium sp.and identified it as a down-regulator of the grp78 gene.The structure of 1 was determined by mainly ESI-mass and two-dimensional NMR spectra.1 dose-dependently inhibited the expression of GRP78 promoter with an IC_50 of 30 nM.
机译:葡萄糖调节蛋白78(GRP78)位于内质网(ER)中,在保护肿瘤细胞免受抗癌药的毒性作用中发挥作用。在使用报告基因(荧光素酶)分析系统寻找GRP78的下调剂时,我们从青霉属菌中分离出一种新化合物,称为Veroxycosrudin(2)的同源物,称为deoxyverrucosidin(1),并将其鉴定为grp78基因的下调因子。1的结构主要由ESI-mass和两个核磁共振波谱。1剂量依赖性地抑制GRP78启动子的表达,IC_50为30 nM。

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