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Marine Antibody–Drug Conjugates: Design Strategies and Research Progress

机译:海洋抗体-药物共轭物:设计策略和研究进展

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摘要

Antibody–drug conjugates (ADCs), constructed with monoclonal antibodies (mAbs), linkers, and natural cytotoxins, are innovative drugs developed for oncotherapy. Owing to the distinctive advantages of both chemotherapy drugs and antibody drugs, ADCs have obtained enormous success during the past several years. The development of highly specific antibodies, novel marine toxins’ applications, and innovative linker technologies all accelerate the rapid R&D of ADCs. Meanwhile, some challenges remain to be solved for future ADCs. For instance, varieties of site-specific conjugation have been proposed for solving the inhomogeneity of DARs (Drug Antibody Ratios). In this review, the usages of various natural toxins, especially marine cytotoxins, and the development strategies for ADCs in the past decade are summarized. Representative ADCs with marine cytotoxins in the pipeline are introduced and characterized with their new features, while perspective comments for future ADCs are proposed.
机译:用单克隆抗体(mAb),接头和天然细胞毒素构建的抗体-药物偶联物(ADC)是为肿瘤疗法开发的创新药物。由于化学疗法药物和抗体药物的独特优势,ADC在过去几年中获得了巨大的成功。高特异性抗体的开发,新型海洋毒素的应用以及创新的接头技术,都加速了ADC的快速研发。同时,未来的ADC还面临一些挑战。例如,针对解决DARs(药物抗体比率)的不均一性,已经提出了多种针对特定部位的共轭形式。在这篇综述中,总结了过去十年中各种天然毒素(尤其是海洋细胞毒素)的用途以及ADC的发展策略。介绍了管线中具有海洋细胞毒素的代表性ADC,并介绍了它们的新功能,同时提出了有关未来ADC的观点评论。

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