A pair of sulfur-containing geldanamycin analogs, 19-S-methylgeldanamycin and 4,5-dihydro-19-S-methylgeldanamycin, from Streptomyces hygroscopicus 17997
A pair of sulfur-containing geldanamycin analogs, 19-S-methylgeldanamycin and 4,5-dihydro-19-S-methylgeldanamycin, from Streptomyces hygroscopicus 17997
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一对含硫格尔德霉素类似物，19-S-甲基格尔德霉素和 4,5-二氢-19-S-甲基格尔德霉素，来自吸水链霉菌 17997
DOI：
10.1038/ja.2011.39
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发表时间：
2011-07-01
影响因子：
3.3
通讯作者：
Wang, Yiguang
中科院分区：
文献类型：
--
作者：
Liu, Xin;Li, Jingyan;Wang, Yiguang
格尔达霉素（GDM，图1）是一种由吸湿链霉菌产生的苯醌类ansamycin。1,2,3它是人热休克蛋白90 （Hsp90）的特异性抑制剂，是一种辅助蛋白质折叠、细胞信号传导和肿瘤抑制的分子伴侣，是抗肿瘤药物的潜在细胞靶点。由于其水溶性差和严重的肝毒性，GDM仅被用作抗癌药物开发的有前途的先导化合物。4,5,6
Geldanamycin (GDM, Figure 1) is a benzoquinone ansamycin produced by Streptomyces hygroscopicus.1, 2, 3 It is a specific inhibitor of human heat shock protein 90 (Hsp90), which is a molecular chaperone assisting in protein folding, cell signaling and tumor repression, and a potential cellular target for anti-tumor agent. GDM is only used as a promising lead compound for anti-cancer drug development because of its poor water solubility and severe liver toxicity.4, 5, 6