Deng Shirui, Wen Xiaoan, Wang Jinzheng
School of China Pharmaceutical University, Nanjing, China.
Department of Lingang Laboratory, Shanghai, China.
Curr Med Chem. 2024 Sep 16. doi: 10.2174/0109298673320170240829110110.
Drug conjugates have emerged as a pivotal research focus in the field of targeted cancer therapy. They represent a widely explored prodrug strategy that significantly enhances the therapeutic index of drugs while minimizing side effects. The stability and selective cleavage of the linker within drug conjugates are critical for the therapeutic efficacy and targeted treatment achieved by these conjugates. In this review, we have categorized the linkers based on their cleavage mode and summarized the chemical properties, advantages, and limitations of various types of cleavable linkers. Particularly, examples have been provided to illustrate their specific potential for development.
药物偶联物已成为靶向癌症治疗领域的一个关键研究重点。它们代表了一种广泛探索的前药策略，能显著提高药物的治疗指数，同时将副作用降至最低。药物偶联物中连接子的稳定性和选择性裂解对于这些偶联物实现的治疗效果和靶向治疗至关重要。在本综述中，我们根据连接子的裂解模式对其进行了分类，并总结了各类可裂解连接子的化学性质、优点和局限性。特别提供了实例来说明它们的具体开发潜力。
