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TPE-Based Peptide Micelles for Targeted Tumor Therapy and Apoptosis Monitoring
ACS Applied Bio Materials ( IF 4.6 ) Pub Date : 2021-01-07 , DOI: 10.1021/acsabm.0c01493
Wenjun Qin 1 , Yu Wu 1 , Yunhong Hu 2 , Yanming Dong 2 , Tonghui Hao 1 , Cheng Zhang 2
ACS Applied Bio Materials ( IF 4.6 ) Pub Date : 2021-01-07 , DOI: 10.1021/acsabm.0c01493
Wenjun Qin 1 , Yu Wu 1 , Yunhong Hu 2 , Yanming Dong 2 , Tonghui Hao 1 , Cheng Zhang 2
Affiliation
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A targeted drug delivery system with lessened side effects and real-time monitoring of tumor cell apoptosis is highly desirable for precision therapy. Herein, we developed a traceable self-assembled micelle (TPR@DOX) by grafting Arg-Gly-Asp (RGD) peptide and tetraphenylethene (TPE) fluorophore on both axial positions of amphiphilic polymers. The aggregation-induced emission (AIE) characteristics of TPE makes the micelle visible for high-quality imaging, indicating the loading and release of doxorubicin (DOX) during the delivery process. RGD peptide can specifically bind to αvβ3 integrin on tumor cell surfaces to facilitate cellular uptake. Furthermore, TPE fluorophore was linked by a caspase-responsive Asp-Glu-Val-Asp (DEVD) peptide, which could be cleaved and generated a hydrophobic TPE residue, resulting in aggregation and fluorescence recovery to indicate apoptosis. In vitro experiments, such as smart nanoplatform, showed remarkable tumor cell killing ability, opening an avenue in precise tumor therapy.
中文翻译：
基于TPE的肽胶束用于靶向肿瘤治疗和细胞凋亡监测
精确治疗迫切需要具有减少的副作用和实时监测肿瘤细胞凋亡的靶向药物输送系统。在这里，我们通过在两亲性聚合物的两个轴向位置上接枝Arg-Gly-Asp（RGD）肽和四苯基乙烯（TPE）荧光团，开发了可追溯的自组装胶束（TPR @ DOX）。TPE的聚集诱导发射（AIE）特性使胶束对于高质量成像可见，表明在递送过程中阿霉素（DOX）的负载和释放。RGD肽可以特异性结合于α v β 3肿瘤细胞表面的整合素有助于细胞摄取。此外，TPE荧光团通过半胱天冬酶响应的Asp-Glu-Val-Asp（DEVD）肽连接，该肽可被切割并产生疏水性TPE残基，从而导致聚集和荧光恢复，表明细胞凋亡。诸如智能纳米平台之类的体外实验显示出卓越的肿瘤细胞杀伤能力，为精确的肿瘤治疗开辟了道路。
更新日期：2021-01-18
中文翻译：
基于TPE的肽胶束用于靶向肿瘤治疗和细胞凋亡监测
精确治疗迫切需要具有减少的副作用和实时监测肿瘤细胞凋亡的靶向药物输送系统。在这里，我们通过在两亲性聚合物的两个轴向位置上接枝Arg-Gly-Asp（RGD）肽和四苯基乙烯（TPE）荧光团，开发了可追溯的自组装胶束（TPR @ DOX）。TPE的聚集诱导发射（AIE）特性使胶束对于高质量成像可见，表明在递送过程中阿霉素（DOX）的负载和释放。RGD肽可以特异性结合于α v β 3肿瘤细胞表面的整合素有助于细胞摄取。此外，TPE荧光团通过半胱天冬酶响应的Asp-Glu-Val-Asp（DEVD）肽连接，该肽可被切割并产生疏水性TPE残基，从而导致聚集和荧光恢复，表明细胞凋亡。诸如智能纳米平台之类的体外实验显示出卓越的肿瘤细胞杀伤能力，为精确的肿瘤治疗开辟了道路。
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