Degrader-antibody conjugates,Chemical Society Reviews

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Degrader-antibody conjugates
Chemical Society Reviews ( IF 40.4 ) Pub Date : 2022-05-04 , DOI: 10.1039/d2cs00141a
Peter S Dragovich ₁

Affiliation

Degrader-antibody conjugates (DACs) are novel entities that combine a proteolysis targeting chimera (PROTAC) payload with a monoclonal antibody via some type of chemical linker. This review provides a current summary of the DAC field. Many general aspects associated with the creation and biological performance of traditional cytotoxic antibody-drug conjugates (ADCs) are initially presented. These characteristics are subsequently compared and contrasted with related parameters that impact DAC generation and biological activity. Several examples of DACs assembled from both the scientific and the patent literature are utilized to highlight differing strategies for DAC creation, and specific challenges associated with DAC construction are documented. Collectively, the assembled examples demonstrate that biologically-active DACs can be successfully prepared using a variety of PROTAC payloads which employ diverse E3 ligases to degrade multiple protein targets.

中文翻译：

降解抗体偶联物

降解抗体偶联物 (DAC) 是一种新型实体，它将蛋白水解靶向嵌合体 (PROTAC) 有效载荷与单克隆抗体相结合，通过某种类型的化学接头。这篇评论提供了 DAC 领域的当前摘要。最初介绍了与传统细胞毒性抗体-药物偶联物 (ADC) 的产生和生物学性能相关的许多一般方面。随后将这些特征与影响 DAC 生成和生物活性的相关参数进行比较和对比。从科学和专利文献中收集的几个 DAC 示例用于突出 DAC 创建的不同策略，并记录了与 DAC 构建相关的具体挑战。总的来说，组装的示例表明，可以使用各种 PROTAC 有效负载成功制备具有生物活性的 DAC，这些有效负载采用多种 E3 连接酶来降解多个蛋白质靶标。

更新日期：2022-05-04

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