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Non-internalising antibody–drug conjugates
Chemical Society Reviews ( IF 40.4 ) Pub Date : 2022-11-02 , DOI: 10.1039/d2cs00446a Nicola Ashman 1 , Jonathan D Bargh 2 , David R Spring 1
Chemical Society Reviews ( IF 40.4 ) Pub Date : 2022-11-02 , DOI: 10.1039/d2cs00446a Nicola Ashman 1 , Jonathan D Bargh 2 , David R Spring 1
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Antibody–drug conjugates (ADCs) typically require internalisation into cancer cells to release their cytotoxic payload. However, this places stringent constraints on therapeutic development, requiring cancer targets that have high expression of internalising antigens and efficient intracellular processing. An alternative approach is emerging whereby the payloads can be released extracellularly from cleavable linkers upon binding to poorly-internalising antigens or other tumoral components. This removes the reliance on high antigen expression, avoids potentially inefficient internalisation, and can greatly expand the range of cancer targets to components of the extracellular tumour matrix. This review gives an overview of recent developments towards non-internalising ADCs, including emerging cancer-associated cell surface and extracellular proteins, cancer stromal targeting and the linking chemistry that enables extracellular payload release.
中文翻译：
非内化抗体-药物偶联物
抗体药物偶联物 (ADC) 通常需要内化到癌细胞中以释放其细胞毒性有效载荷。然而，这对治疗发展提出了严格的限制，需要具有高表达内化抗原和高效细胞内加工的癌症靶点。另一种方法正在出现，通过这种方法，有效载荷可以在与内化不良的抗原或其他肿瘤成分结合后从可裂解接头中释放到细胞外。这消除了对高抗原表达的依赖，避免了潜在的低效内化，并且可以极大地将癌症靶标的范围扩展到细胞外肿瘤基质的成分。这篇综述概述了非内化 ADC 的最新发展，包括新兴的癌症相关细胞表面和细胞外蛋白，
更新日期：2022-11-02
中文翻译：
非内化抗体-药物偶联物
抗体药物偶联物 (ADC) 通常需要内化到癌细胞中以释放其细胞毒性有效载荷。然而，这对治疗发展提出了严格的限制，需要具有高表达内化抗原和高效细胞内加工的癌症靶点。另一种方法正在出现，通过这种方法，有效载荷可以在与内化不良的抗原或其他肿瘤成分结合后从可裂解接头中释放到细胞外。这消除了对高抗原表达的依赖，避免了潜在的低效内化，并且可以极大地将癌症靶标的范围扩展到细胞外肿瘤基质的成分。这篇综述概述了非内化 ADC 的最新发展，包括新兴的癌症相关细胞表面和细胞外蛋白，
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