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格尔德霉素(Geldanamycin,GA)属于苯醌安莎,是重要的抗肿瘤先导化合物.GA 通过竞争性结合Hsp90 N 末端ATP/ADP 结构域,特异性地抑制Hsp90 所必需的ATP 酶活性,从而改变Hsp90 构象,抑制其分子伴侣功能1-2.
17-芳酰基-17-去甲氧基格尔德霉素衍生物的设计、合成及抗肿瘤活性和肝毒性研究
【摘 要】
：
格尔德霉素(Geldanamycin,GA)属于苯醌安莎,是重要的抗肿瘤先导化合物.GA 通过竞争性结合Hsp90 N 末端ATP/ADP 结构域,特异性地抑制Hsp90 所必需的ATP 酶活性,从而改变Hsp90 构象,抑制其分子伴侣功能1-2.
【机 构】
：
天然产物化学生物学教育部重点实验室,山东大学药学院,山东 济南 250012
【出 处】
：
全国药物化学学术会议暨第四届中英药物化学学术会议
【发表日期】
：
2013年11期
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