Novel Strategy for Preparing Dual-Modality Optical/PET Imaging Probes via Photo-Click Chemistry

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• 作者：Lingyi Sun ; Jiule Ding ; Wei Xing ; Yongkang Gai ; Jing Sheng ; Dexing Zeng
• 刊名：Bioconjugate Chemistry
• 出版年：2016
• 出版时间：May 18, 2016
• 年：2016
• 卷：27
• 期：5
• 页码：1200-1204
• 全文大小：333K
• 年卷期：0
• ISSN：1520-4812

文摘

Preparation of small molecule based dual-modality probes remains a challenging task due to the complicated synthetic procedure. In this study, a novel concise and generic strategy for preparing dual-modality optical/PET imaging probes via photo-click chemistry was developed, in which the diazole photo-click linker functioned not only as a bridge between the targeting-ligand and the PET imaging moiety, but also as the fluorophore for optical imaging. A dual-modality AE105 peptidic probe was successfully generated via this strategy and subsequently applied in the fluorescent staining of U87MG cells and the ⁶⁸Ga based PET imaging of mice bearing U87MG xenograft. In addition, dual-modality monoclonal antibody cetuximab has also been generated via this strategy and labeled with ⁶⁴Cu for PET imaging studies, broadening the application of this strategy to include the preparation of macromolecule based imaging probes.