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首页> 外文期刊>Advanced Functional Materials >A Dual-FRET-Based Versatile Prodrug for Real-Time Drug Release Monitoring and In Situ Therapeutic Efficacy Evaluation
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A Dual-FRET-Based Versatile Prodrug for Real-Time Drug Release Monitoring and In Situ Therapeutic Efficacy Evaluation

机译：基于双FRET的多功能前药，用于实时药物释放监测和原位治疗效果评估

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摘要

A dual-Forster resonance energy transfer (FRET)-based versatile prodrug (V-prodrug), in which the fluorescence of both 5(6)-carboxylfluorescein (FAM) and doxorubicin (DOX) can be quenched by 4-(dimethylaminoazo)benzene-4-carboxylic acid (Dabcyl) with high quenching efficiency, is developed in this paper. The V-prodrug can selectively bind to the (v3) integrin overexpressed cancer cells through the Arg-Gly-Asp (RGD) targeting moiety. After that, the acid-mediated DOX release of the V-prodrug can be real-time monitored by the increase of the red fluorescence from DOX. Thereafter, DOX-induced cell apoptosis can also be in situ assessed by the fluorescence recovery of the FAM, due to the caspase-3-mediated Asp-Glu-Val-Asp (DEVD) peptide sequence cleavage. This novel prodrug provides a cascaded imaging of real-time drug release and subsequent cell apoptosis, which enables the in situ detection of the cancer response and the therapeutic efficacy evaluation of the prodrug.
机译：基于双福斯特共振能量转移（FRET）的多功能前药（V-prodrug），其中5（6）-羧基荧光素（FAM）和阿霉素（DOX）的荧光都可以被4-（二甲基氨基偶氮）苯淬灭本文开发了具有高淬灭效率的-4-羧酸（Dabcyl）。 V-前药可以通过Arg-Gly-Asp（RGD）靶向部分选择性地结合（v3）整联蛋白过表达的癌细胞。之后，可以通过增加DOX的红色荧光来实时监测V介导的酸介导的DOX释放。此后，由于caspase-3介导的Asp-Glu-Val-Asp（DEVD）肽序列的切割，DOX诱导的细胞凋亡也可以通过FAM的荧光恢复进行原位评估。这种新颖的前药提供了实时药物释放和随后的细胞凋亡的级联成像，从而能够原位检测癌症反应并评估前药的疗效。

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  • 来源
    《Advanced Functional Materials》 |2015年第47期|7317-7326|共10页
  • 作者

    Li Shi-Ying; Liu Li-Han; Rong Lei; Qiu Wen-Xiu; Jia Hui-Zhen; Li Bin; Li Fei; Zhang Xian-Zheng;

  • 作者单位

    Wuhan Univ, Key Lab Biomed Polymers, Minist Educ, Wuhan 430072, Peoples R China|Wuhan Univ, Dept Chem, Wuhan 430072, Peoples R China;

    Wuhan Univ, Key Lab Biomed Polymers, Minist Educ, Wuhan 430072, Peoples R China|Wuhan Univ, Dept Chem, Wuhan 430072, Peoples R China;

    Wuhan Univ, Key Lab Biomed Polymers, Minist Educ, Wuhan 430072, Peoples R China|Wuhan Univ, Dept Chem, Wuhan 430072, Peoples R China;

    Wuhan Univ, Key Lab Biomed Polymers, Minist Educ, Wuhan 430072, Peoples R China|Wuhan Univ, Dept Chem, Wuhan 430072, Peoples R China;

    Wuhan Univ, Key Lab Biomed Polymers, Minist Educ, Wuhan 430072, Peoples R China|Wuhan Univ, Dept Chem, Wuhan 430072, Peoples R China;

    Wuhan Univ, Key Lab Biomed Polymers, Minist Educ, Wuhan 430072, Peoples R China|Wuhan Univ, Dept Chem, Wuhan 430072, Peoples R China;

    Wuhan Univ, Key Lab Biomed Polymers, Minist Educ, Wuhan 430072, Peoples R China|Wuhan Univ, Dept Chem, Wuhan 430072, Peoples R China;

    Wuhan Univ, Key Lab Biomed Polymers, Minist Educ, Wuhan 430072, Peoples R China|Wuhan Univ, Dept Chem, Wuhan 430072, Peoples R China;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类
  • 关键词

    apoptosis imaging; drug release monitors; FRET; prodrugs; theranostics;

    机译：细胞凋亡成像;药物释放监测仪;FRET;前药;热疗;

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