Synthesis of Doxorubicin and miRNA Stimuli-Sensitive Conjugates for Combination Therapy.
Synthesis of Doxorubicin and miRNA Stimuli-Sensitive Conjugates for Combination Therapy.
复制标题
用于联合治疗的阿霉素和 miRNA 刺激敏感缀合物的合成。
DOI：
10.1007/978-1-4939-9220-1_8
复制
发表时间：
2019
期刊：
影响因子：
--
通讯作者：
Torchilin,VladimirP
中科院分区：
文献类型：
--
作者：
Costa,DanielF;Sarisozen,Can;Torchilin,VladimirP
通过使用化疗药物和小的非编码RNA的组合疗法的最新进展已经突出了优化这些药剂以允许它们在单一递送系统中运载的需要。该方案详细描述了多柔比星前药的合成，其中NHS偶联反应用于使药物对肿瘤微环境的蛋白水解活性敏感。还描述了通过S-S偶联反应设计脂质修饰的miRNA。多柔比星和miRNA两者的修饰促进了它们同时掺入混合胶束中以用于针对肿瘤细胞的联合治疗。
Recent advances in combination therapy by using chemotherapeutic drugs and small noncoding RNAs have highlighted the need for optimization of such agents to allow their carriage in a single delivery system. This protocol details the synthesis of a doxorubicin prodrug, where a NHS coupling reaction was used to sensitize the drug to the proteolytic activity of tumor microenvironments. The design of a lipid-modified miRNA by an S-S coupling reaction is also described. Modification of both, doxorubicin and miRNA, facilitated their simultaneous incorporation into mixed micelles for use in combination therapy against tumor cells.