开发用于癌症治疗的刺激响应小分子前药的策略。
Strategies for the development of stimuli-responsive small molecule prodrugs for cancer treatment.
发表日期:2024
作者:
Yuxuan Tu, Jianbao Gong, Jing Mou, Hongfei Jiang, Haibo Zhao, Jiake Gao
来源:
Frontiers in Pharmacology
摘要:
已批准的抗癌药物通常因其治疗窗口狭窄而面临挑战,这主要是因为高全身毒性和对肿瘤的选择性有限。前药最初是设计用于进行特定化学修饰的无活性药物分子。这些修饰使药物失去活性,直到它们在体内遇到特定条件或生物标志物,此时它们被转化为活性药物分子。这种深思熟虑的设计通过增强肿瘤特异性并最大限度地减少脱靶效应,显着提高了抗癌药物输送的功效。前药设计的最新进展集中于将这些策略与脂质体、胶束和聚合物体等递送系统相结合,以进一步改善靶向性并减少副作用。这篇综述概述了设计专注于癌症治疗的刺激响应小分子前药的策略,强调了它们的化学结构和控制药物释放的机制。通过提供全面的概述,我们旨在强调这些创新方法彻底改变癌症治疗的潜力。版权所有 © 2024 Tu、Gong、Mou、Jiang、Zhao 和 Gau。
Approved anticancer drugs typically face challenges due to their narrow therapeutic window, primarily because of high systemic toxicity and limited selectivity for tumors. Prodrugs are initially inactive drug molecules designed to undergo specific chemical modifications. These modifications render the drugs inactive until they encounter specific conditions or biomarkers in vivo, at which point they are converted into active drug molecules. This thoughtful design significantly improves the efficacy of anticancer drug delivery by enhancing tumor specificity and minimizing off-target effects. Recent advancements in prodrug design have focused on integrating these strategies with delivery systems like liposomes, micelles, and polymerosomes to further improve targeting and reduce side effects. This review outlines strategies for designing stimuli-responsive small molecule prodrugs focused on cancer treatment, emphasizing their chemical structures and the mechanisms controlling drug release. By providing a comprehensive overview, we aim to highlight the potential of these innovative approaches to revolutionize cancer therapy.Copyright © 2024 Tu, Gong, Mou, Jiang, Zhao and Gao.