Department of Molecular Sciences and Nanosystems, Università Ca' Foscari Campus Scientifico, Via Torino 155, 30174 Venezia-Mestre, Italy.
Pathology Unit, Department of Molecular Biology and Translational Research, Centro di Riferimento Oncologico di Aviano (CRO) IRCCS, Via Franco Gallini 2, 33081 Aviano, Italy.
Int J Mol Sci. 2024 Aug 8;25(16):8651. doi: 10.3390/ijms25168651.
This review highlights significant advancements in antibody-drug conjugates (ADCs) equipped with metal-based and nature-inspired payloads, focusing on synthetic strategies for antibody conjugation. Traditional methods such us maleimide and succinimide conjugation and classical condensation reactions are prevalent for metallodrugs and natural compounds. However, emerging non-conventional strategies such as photoconjugation are gaining traction due to their milder conditions and, in an aspect which minimizes side reactions, selective formation of ADC. The review also summarizes the therapeutic and diagnostic properties of these ADCs, highlighting their enhanced selectivity and reduced side effects in cancer treatment compared to non-conjugated payloads. ADCs combine the specificity of monoclonal antibodies with the cytotoxicity of chemotherapy drugs, offering a targeted approach to the elimination of cancer cells while sparing healthy tissues. This targeted mechanism has demonstrated impressive clinical efficacy in various malignancies. Key future advancements include improved linker technology for enhanced stability and controlled release of cytotoxic agents, incorporation of novel, more potent, cytotoxic agents, and the identification of new cancer-specific antigens through genomic and proteomic technologies. ADCs are also expected to play a crucial role in combination therapies with immune checkpoint inhibitors, CAR-T cells, and small molecule inhibitors, leading to more durable and potentially curative outcomes. Ongoing research and clinical trials are expanding their capabilities, paving the way for more effective, safer, and personalized treatments, positioning ADCs as a cornerstone of modern medicine and offering new hope to patients.
这篇综述重点介绍了配备基于金属和受自然启发的有效载荷的抗体药物偶联物(ADC)的重大进展,重点介绍了抗体缀合的合成策略。用于金属药物和天然化合物的传统方法,如马来酰亚胺和琥珀酰亚胺缀合以及经典缩合反应,仍然很常见。但是,由于条件较为温和,并且在一定程度上可以最小化副反应,从而选择性地形成 ADC,新兴的非传统策略(如光偶联)正在受到关注。该综述还总结了这些 ADC 的治疗和诊断特性,强调了它们在癌症治疗中与非缀合有效载荷相比,具有增强的选择性和降低的副作用。ADC 将单克隆抗体的特异性与化疗药物的细胞毒性结合在一起,为消除癌细胞提供了靶向方法,同时保护了健康组织。这种靶向机制在各种恶性肿瘤中显示出了令人印象深刻的临床疗效。未来的关键进展包括改进连接子技术,以增强稳定性和控制细胞毒性剂的释放,将新型、更有效、细胞毒性剂纳入其中,并通过基因组和蛋白质组技术鉴定新的癌症特异性抗原。ADC 还预计将在与免疫检查点抑制剂、CAR-T 细胞和小分子抑制剂的联合治疗中发挥关键作用,从而产生更持久和潜在的治愈效果。正在进行的研究和临床试验正在扩展它们的能力,为更有效、更安全和个性化的治疗铺平道路,使 ADC 成为现代医学的基石,并为患者带来新的希望。