Prunustatin A, a novel GRP78 molecular chaperone down-regulator isolated from Streptomyces violaceoniger

Prunustatin A, a novel GRP78 molecular chaperone down-regulator isolated from Streptomyces violaceoniger
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DOI:
10.1038/ja.2005.25
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发表时间:
2005-03-01
影响因子:
3.3
通讯作者:
Shin-ya, K
Shin-ya, K
中科院分区:
医学4区
文献类型:
--
作者:
Umeda, Y;Chijiwa, S;Shin-ya, K

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在分子伴侣 GRP78 表达调节剂的筛选过程中,我们从紫罗兰链霉菌 4521-SVS3 中分离出一种新型 GRP78 表达抑制剂,命名为 prunustatin A。通过一系列 NMR 分析确定 prunustatin A 的结构是新抗霉素家族的氧化型。 Prunustatin A 抑制人纤维肉瘤 HT1080 细胞中 2-脱氧葡萄糖诱导的 GRP78 表达,并伴有整体细胞死亡,但在正常营养条件下不表现出细胞毒性。
In the course of our screening program for regulators of a molecular chaperone GRP78 expression, we isolated a novel inhibitor of GRP78 expression, designated as prunustatin A, from Streptomyces violaceoniger 4521-SVS3. The structure of prunustatin A was determined by a series of NMR analyses to be an oxidized type of the neoantimycin family. Prunustatin A inhibited the expression of GRP78 induced by 2-deoxyglucose in human fibrosarcoma HT1080 cells accompanied by global cell death without showing cytotoxicity under normal nutrient condition.