Immunotoxins and anticancer drug conjugate assemblies: the role of the linkage between components.
Immunotoxins and anticancer drug conjugate assemblies: the role of the linkage between components.
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DOI：
10.3390/toxins3070848
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发表时间：
2011-07
期刊：
影响因子：
4.2
通讯作者：
Cattel L
中科院分区：
文献类型：
--
作者：
Dosio F;Brusa P;Cattel L
免疫毒素和抗体-药物结合物是以蛋白质为基础的药物，结合了靶标特异的结合域和细胞毒域。这些化合物对包括癌症在内的疾病具有潜在的治疗作用，几项临床试验显示出令人鼓舞的结果。尽管靶向消除恶性细胞是一个优雅的概念，但仍有许多实际挑战限制了结合物的治疗应用，包括低效率的细胞摄取、低细胞毒性和非靶向效应。在化学合成法制备免疫结合物的过程中，连接两个构件的铰链组件的选择是至关重要的：结合物必须在体内保持稳定，但当达到目标时必须能够有效地释放有毒部分。已经做出了巨大的努力，本文综述了开发免疫结合物所采用的策略，重点是化学连接物的进化。
Immunotoxins and antibody-drug conjugates are protein-based drugs combining a target-specific binding domain with a cytotoxic domain. Such compounds are potentially therapeutic against diseases including cancer, and several clinical trials have shown encouraging results. Although the targeted elimination of malignant cells is an elegant concept, there are numerous practical challenges that limit conjugates’ therapeutic use, including inefficient cellular uptake, low cytotoxicity, and off-target effects. During the preparation of immunoconjugates by chemical synthesis, the choice of the hinge component joining the two building blocks is of paramount importance: the conjugate must remain stable in vivo but must afford efficient release of the toxic moiety when the target is reached. Vast efforts have been made, and the present article reviews strategies employed in developing immunoconjugates, focusing on the evolution of chemical linkers.
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影响因子：
4.2
作者：
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通讯作者：
Fabbrini MS
影响因子：
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