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用于便捷构建多价和多模态成像探针的通用分子支架

Universal Molecular Scaffold for Facile Construction of Multivalent and Multimodal Imaging Probes.

作者信息

Gai Yongkang, Xiang Guangya, Ma Xiang, Hui Wenqi, Ouyang Qin, Sun Lingyi, Ding Jiule, Sheng Jing, Zeng Dexing

机构信息

School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology , Wuhan 430030, China.

Department of Radiology, University of Pittsburgh , 100 Technology Drive, Suite 452D, Pittsburgh, Pennsylvania 15219, United States.

出版信息

Bioconjug Chem. 2016 Mar 16;27(3):515-20. doi: 10.1021/acs.bioconjchem.6b00034. Epub 2016 Feb 24.

Abstract

Multivalent and multimodal imaging probes are rapidly emerging as powerful chemical tools for visualizing various biochemical processes. Herein, we described a bifunctional chelator (BFC)-based scaffold that can be used to construct such promising probes concisely. Compared to other reported similar scaffolds, this new BFC scaffold demonstrated two major advantages: (1) significantly simplified synthesis due to the use of this new BFC that can serve as chelator and linker simultaneously; (2) highly efficient synthesis rendered by using either click chemistry and/or total solid-phase synthesis. In addition, the versatile utility of this molecular scaffold has been demonstrated by constructing several multivalent/multimodal imaging probes labeled with various radioisotopes, and the resulting radiotracers demonstrated substantially improved in vivo performance compared to the two individual monomeric counterparts.

摘要

多价和多模态成像探针正迅速成为用于可视化各种生化过程的强大化学工具。在此,我们描述了一种基于双功能螯合剂(BFC)的支架,它可用于简洁地构建此类有前景的探针。与其他报道的类似支架相比,这种新型BFC支架具有两个主要优点:(1)由于使用了这种可同时作为螯合剂和连接体的新型BFC,合成过程显著简化;(2)通过使用点击化学和/或全固相合成实现了高效合成。此外,通过构建几种用各种放射性同位素标记的多价/多模态成像探针,证明了这种分子支架的多功能性,并且与两种单独的单体对应物相比,所得放射性示踪剂在体内的性能有了显著改善。

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