摘要
微管蛋白结合剂的疗效和耐受性受到其对癌细胞的低特异性的阻碍,就像大多数临床上使用的抗癌剂一样。为了提高特异性,微管蛋白结合剂已与靶向癌细胞的药物共价偶联,以提供主动靶向药物偶联物。这些偶联物旨在增加癌细胞对药物的摄取,同时具有正常细胞有限的摄取,从而提高疗效和耐受性。使用的方法包括附着在小分子,多糖,肽,蛋白质和抗体上,这些抗体利用这些物质的受体的过表达。迄今为止,抗体靶向策略是最成功的,其中六个这样的例子已经获得了临床批准。许多其他偶联物类型,特别是那些靶向叶酸受体的结合物类型,在临床前模型和早期临床研究中显示出有希望的疗效和毒性特征。本文介绍了用于形成这些主动靶向偶联物的最新策略的成功与否的讨论。
关键词: 微管蛋白结合剂的疗效和耐受性受到其对癌细胞的低特异性的阻碍,就像大多数临床上使用的抗癌剂一样。为了提高特异性,微管蛋白结合剂已与靶向癌细胞的药物共价偶联,以提供主动靶向药物偶联物。这些偶联物旨在增加癌细胞对药物的摄取,同时具有正常细胞有限的摄取,从而提高疗效和耐受性。使用的方法包括附着在小分子,多糖,肽,蛋白质和抗体上,这些抗体利用这些物质的受体的过表达。迄今为止,抗体靶向策略是最成功的,其中六个这样的例子已经获得了临床批准。许多其他偶联物类型,特别是那些靶向叶酸受体的结合物类型,在临床前模型和早期临床研究中显示出有希望的疗效和毒性特征。本文介绍了用于形成这些主动靶向偶联物的最新策略的成功与否的讨论。
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