Antibody-drug conjugates: Recent advances in linker chemistry.
Antibody-drug conjugates: Recent advances in linker chemistry.
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抗体-药物偶联物：连接化学的最新进展
DOI：
10.1016/j.apsb.2021.03.042
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发表时间：
2021-12
期刊：
影响因子：
--
通讯作者：
Li S
中科院分区：
文献类型：
--
作者：
Su Z;Xiao D;Xie F;Liu L;Wang Y;Fan S;Zhou X;Li S
抗体-药物偶联物（ADC）正在逐渐改变临床癌症治疗。抗体-药物缀合物接头分子决定功效和副作用两者，并且因此对ADC的命运具有主要影响。理想的接头应该在循环系统中稳定，并在肿瘤中特异性释放细胞毒性有效载荷。然而，现有的接头通常非特异性地释放有效载荷，并且不可避免地导致脱靶毒性。这一缺陷正成为制约ADC发展的一个越来越重要的因素。对具有最佳治疗窗的ADC的追求已经在新型接头的发现和开发方面取得了显著进展。本文综述了近5年来ADC的化学触发剂、连接体-抗体连接和连接体-有效负载连接的研究进展，并介绍了ADC的ADMET特性。这项工作也有助于阐明未来的发展方向的连接器。抗体药物缀合物（ADC）正在彻底改变癌症治疗。决定功效和脱靶毒性的接头是ADC的核心组分。综述了近5年来连接体的研究进展。
Antibody–drug conjugates (ADCs) are gradually revolutionizing clinical cancer therapy. The antibody–drug conjugate linker molecule determines both the efficacy and the adverse effects, and so has a major influence on the fate of ADCs. An ideal linker should be stable in the circulatory system and release the cytotoxic payload specifically in the tumor. However, existing linkers often release payloads nonspecifically and inevitably lead to off-target toxicity. This defect is becoming an increasingly important factor that restricts the development of ADCs. The pursuit of ADCs with optimal therapeutic windows has resulted in remarkable progress in the discovery and development of novel linkers. The present review summarizes the advance of the chemical trigger, linker‒antibody attachment and linker‒payload attachment over the last 5 years, and describes the ADMET properties of ADCs. This work also helps clarify future developmental directions for the linkers. Antibody–drug conjugates (ADCs) are revolutionizing cancer therapy. Linkers, determining both efficacy and off-target toxicity, are the core components of ADCs. The advances of linkers over the past 5 years are reviewed.
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