A fluorinated azine as a versatile scaffold for the development of Cu (II)-specific multi-functional imaging probes
A fluorinated azine as a versatile scaffold for the development of Cu (II)-specific multi-functional imaging probes
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氟化吖嗪作为多功能支架，用于开发 Cu (II) 特异性多功能成像探针
DOI：
10.1016/j.snb.2021.130106
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发表时间：
2021
影响因子：
8.4
通讯作者：
Xu Hao
中科院分区：
文献类型：
--
作者：
Ye Weijian;Xie Mengting;Wei Junjie;Li Guocong;Tang Yongjin;Hou Lu;Wang Lu;Yu Huijuan;Lee Chi-Sing;Xu Hao
铜对许多生理活动至关重要，其稳态异常与癌症以及神经退行性疾病有关。具有单一成像模式的铜靶向探针已被广泛报道并在特定方面应用。在此，我们描绘了基于氟化azineFN的Cu（II）特异性多功能成像探针的发展。吖嗪选择性地与Cu 2+离子结合，形成1：1FN-Cu 2+络合物，并诱导显著的荧光猝灭，这可以在加入H2S（Na 2S作为H2S的来源）后恢复。顺磁性Cu ~（2+）离子的结合也导致了FN-Cu ~（2+）复合物中19 F核的弛豫增强，提高了体模图像的信噪比。首次合成了18F-放射性标记的类似物[18F]FN，并将其用于食蟹猴PET/CT成像，以进行初步的药代动力学研究。
Copper is vital to many physiological activities, and its dyshomeostasis is related to cancers as well as neurodegenerative diseases. Copper targeting probes with single imaging modality have been extensively reported and employed in specific aspects. Herein, we delineate the development of Cu(II)-specific multi-functional imaging probes based on a fluorinated azineFN. The azine selectively binds to a Cu2+ion, forming a 1:1FN-Cu2+complex, and induces a substantial fluorescence quenching, which can be resumed upon addition of H2S (Na2S as the source of H2S). The binding of the paramagnetic Cu2+ions also leads to the relaxation enhancement of the19F nuclei in theFN-Cu2+complex and improve the signal-to-noise ratio of the phantom images. The18F-radiolabeled analogue, [18F]FN, is synthesized for the first time and used in PET/CT imaging on cynomolgus for a preliminary study of pharmacokinetics.