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长春花结构域微管抑制剂药效团的结构洞察复制

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Y Wang， FW Benz， Y Wu， Q Wang， Y Chen...
Molecular ...， 2016
爱思唯尔
近年来，抗体药物偶联物（ADCs）在癌症治疗中取得了巨大成功。一些由天然和非天然氨基酸组成的肽基微管抑制剂，例如单甲基奥瑞他汀 E （MMAE） 和 F （MMAF），具有极强的细胞毒性，已被用作 ADC 中的有效载荷。然而，它们与微管蛋白和微管的精确分子相互作用仍不清楚。我们确定了微管蛋白与三种超强肽基微管抑制剂 [MMAE、他托布林 （HTI-286） ...

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