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铜标记的丹磺酰化合物作为用于凋亡成像的荧光和正电子发射断层显像探针。

Cu-labeled dansyl compounds as fluorescent and PET probes for imaging apoptosis.

作者信息

Han Junyan, Wang Xukui, Yu MeiXiang

机构信息

Cyclotron & Radiopharmaceutical Core, Houston Methodist Hospital, Weill Cornell Medical College of Cornell University, 6565 Fannin Street, Houston, TX 77030, USA.

Cyclotron & Radiopharmaceutical Core, Houston Methodist Hospital, Weill Cornell Medical College of Cornell University, 6565 Fannin Street, Houston, TX 77030, USA.

出版信息

Bioorg Med Chem Lett. 2016 Nov 15;26(22):5594-5596. doi: 10.1016/j.bmcl.2016.09.057. Epub 2016 Sep 29.

Abstract

Compound DNSTT-Cu, a novel chelate of Cu with DOTA conjugated to a fluorescent dansyl fragment, is developed for imaging cell apoptosis. Apoptotic U-87MG cells could be selectively visualized by the fluorescence of DNSTT-Cu from cytoplasm of cells, confirmed by the fluorescence of apoptosis cells co-labeled with Alexa Fluor 568-labeled annexin V, a conventional probe for selectively labeling membranes of apoptosis cells. A radioactive Cu analog, DNSTT-Cu, was easily synthesized, providing a potential PET probe for imaging apoptosis in vivo.

摘要

化合物DNSTT-Cu是一种新型的铜螯合物,它将与荧光丹磺酰片段共轭的DOTA与铜结合,用于细胞凋亡成像。凋亡的U-87MG细胞可以通过细胞胞质中DNSTT-Cu的荧光被选择性地可视化,这通过与Alexa Fluor 568标记的膜联蛋白V(一种用于选择性标记凋亡细胞膜的传统探针)共标记的凋亡细胞的荧光得到证实。一种放射性铜类似物DNSTT-Cu易于合成,为体内凋亡成像提供了一种潜在的正电子发射断层扫描(PET)探针。

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