Rational design of fluorescent probes for targeted in vivo nitroreductase visualization.,Organic & Biomolecular Chemistry

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Rational design of fluorescent probes for targeted in vivo nitroreductase visualization.
Organic & Biomolecular Chemistry ( IF 2.9 ) Pub Date : 2020-06-10 , DOI: 10.1039/d0ob00082e
Jie Gao ₁ , Xiaofan Yin ₁ , Mimi Li ₁ , Ji-An Chen ₁ , Jiahui Tan ₁ , Zhen Zhao ₁ , Xianfeng Gu ₁

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Nitroreductase (NTR) has been recognized as a biomarker for identifying the hypoxic status of cancers. Therefore, it is of high scientific interest to design effective fluorescent probes for tracking NTR activity. However, studies on elucidation of the structure−performance relationship of fluorescent probes and those providing valuable insight into optimized probe design have rarely been reported. Three BODIPY based fluorescent probes were made by conjugation of para-, ortho-, and meta-nitrobenzene to the BODIPY core via a thiolether bond, respectively. Our study revealed that the linkage and nitro substituent position significantly influence the capability of nitroreductase detection.

中文翻译：

荧光探针的合理设计，可用于靶向体内硝基还原酶的可视化。

硝基还原酶（NTR）已被认为是鉴定癌症低氧状态的生物标志物。因此，设计有效的追踪NTR活性的荧光探针具有很高的科学兴趣。但是，很少有研究阐明荧光探针的结构与性能之间的关系以及为优化探针设计提供有价值的见识的研究。三BODIPY系荧光探针由缀合制成段， -邻-和间位-硝基苯到BODIPY芯通过一个thiolether键分别。我们的研究表明，键和硝基取代基的位置会显着影响硝基还原酶的检测能力。

更新日期：2020-07-01

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