Furin‐Mediated Self‐Assembly of Olsalazine Nanoparticles for Targeted Raman Imaging of Tumors,Angewandte Chemie International Edition

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Furin‐Mediated Self‐Assembly of Olsalazine Nanoparticles for Targeted Raman Imaging of Tumors
Angewandte Chemie International Edition ( IF 16.1 ) Pub Date : 2020-12-15 , DOI: 10.1002/anie.202014839
Yue Yuan ₁ , Piyush Raj ₂ , Jia Zhang ₃ , Soumik Siddhanta ₂ , Ishan Barman ₂ , Jeff W. M. Bulte ₄

Affiliation

Olsalazine (Olsa) is a broad‐spectrum anti‐cancer agent acting as a DNA‐methylation inhibitor. When conjugated to 2‐cyano‐6‐aminobenzothiazole and a peptide substrate specific for the tumor‐overexpressed enzyme furin, it can self‐assemble into nanoparticles that can be detected by chemical‐exchange saturation‐transfer magnetic‐resonance imaging (CEST MRI). We report here that these nano‐assemblies can also be detected with high specificity in furin‐overexpressing tumor cells by Raman spectroscopy with a distinct scattering signature and demonstrate the utility of this sensing mechanism in vitro and in vivo. Our findings suggest that Raman spectroscopy could be used for high‐resolution image‐guided surgery to precisely delineate tumor margins during and after resection in real‐time as well as to determine microscopic tumor invasion and multifocal locoregional tumor spread, which are currently impossible to visualize with available imaging technologies, including CEST MRI.

中文翻译：

奥林嗪纳米颗粒的弗林蛋白酶介导的自组装，用于肿瘤靶向拉曼成像

Olsalazine（Olsa）是一种广谱抗癌药，可作为DNA甲基化抑制剂。与2-氰基-6-氨基苯并噻唑和特异性表达于肿瘤过度表达的酶弗林蛋白酶的肽底物偶联后，它可以自组装成纳米颗粒，可以通过化学交换饱和转移磁共振成像（CEST MRI）进行检测。我们在这里报告，这些纳米组装件还可以通过具有独特散射特征的拉曼光谱法在弗林蛋白酶过表达的肿瘤细胞中以高特异性检测出来，并证明了这种传感机制在体外和体内的实用性。

更新日期：2021-02-12

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