Stimuli-responsive prodrugs with self-immolative linker for improved cancer therapy

IF 6 2区医学 Q1 CHEMISTRY, MEDICINAL

European Journal of Medicinal Chemistry Pub Date : 2024-09-30 DOI:10.1016/j.ejmech.2024.116928

Wenting Xu , Ang Jia , Zhixian Lei , Jianing Wang , Hongfei Jiang , Shuai Wang , Qi Wang

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Abstract

Self-immolative prodrugs have gained significant attention as an innovative approach for targeted cancer therapy. These prodrugs are engineered to release the active anticancer agents in response to specific triggers within the tumor microenvironment, thereby improving therapeutic precision while reducing systemic toxicity. This review focuses on the molecular architecture and design principles of self-immolative prodrugs, emphasizing the role of stimuli-responsive linkers and activation mechanisms that enable controlled drug release. Recent advancements in this field include the development of prodrugs that incorporate targeting moieties for enhanced site-specificity. Moreover, the review discusses the incorporation of targeting moieties to achieve site-specific drug delivery, thereby improving the selectivity of treatment. By summarizing key research from the past five years, this review highlights the potential of self-immolative prodrugs to revolutionize cancer treatment strategies and pave the way for their integration into clinical practice.

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带有自巯基连接体的刺激响应原药，用于改善癌症治疗

作为癌症靶向治疗的一种创新方法，自凋亡原药受到了广泛关注。这些原药可根据肿瘤微环境中的特定触发因素释放活性抗癌药物，从而提高治疗的精确性，同时降低全身毒性。本综述重点介绍自惰性原药的分子结构和设计原理，强调刺激响应连接体和激活机制的作用，从而实现药物的可控释放。该领域的最新进展包括开发出了含有靶向分子的原药，从而增强了靶点特异性。此外，本综述还讨论了如何通过加入靶向分子来实现特定部位给药，从而提高治疗的选择性。通过总结过去五年的主要研究，本综述强调了自凋亡原药彻底改变癌症治疗策略的潜力，并为其融入临床实践铺平了道路。

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来源期刊

European Journal of Medicinal Chemistry 化学-医药化学

CiteScore

11.70

自引率

9.00%

发文量

863

审稿时长

29 days

期刊介绍： The European Journal of Medicinal Chemistry is a global journal that publishes studies on all aspects of medicinal chemistry. It provides a medium for publication of original papers and also welcomes critical review papers. A typical paper would report on the organic synthesis, characterization and pharmacological evaluation of compounds. Other topics of interest are drug design, QSAR, molecular modeling, drug-receptor interactions, molecular aspects of drug metabolism, prodrug synthesis and drug targeting. The journal expects manuscripts to present the rational for a study, provide insight into the design of compounds or understanding of mechanism, or clarify the targets.