[Cu]Cu-NOTA-PEG-H-Tz 用于 LS174T 异种移植体的靶向前成像评估 - 与 [In]In-DOTA-PEG-BisPy-Tz 的比较。
Evaluation of [Cu]Cu-NOTA-PEG-H-Tz for Pretargeted Imaging in LS174T Xenografts-Comparison to [In]In-DOTA-PEG-BisPy-Tz.
机构信息
Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Jagtvej 160, 2100 Copenhagen, Denmark.
Department of Clinical Physiology, Nuclear Medicine & PET, Rigshospitalet, Blegdamsvej 9, 2100 Copenhagen, Denmark.
出版信息
Molecules. 2021 Jan 21;26(3):544. doi: 10.3390/molecules26030544.
Pretargeted nuclear imaging for the diagnosis of various cancers is an emerging and fast developing field. The tetrazine ligation is currently considered the most promising reaction in this respect. Monoclonal antibodies are often the preferred choice as pretargeting vector due to their outstanding targeting properties. In this work, we evaluated the performance of [Cu]Cu-NOTA-PEG-H-Tz using a setup we previously used for [In]In-DOTA-PEG-BisPy-Tz, thereby allowing for comparison of the performance of these two promising pretargeting imaging agents. The evaluation included a comparison of the physicochemical properties of the compounds and their performance in an ex vivo blocking assay. Finally, [Cu]Cu-NOTA-PEG-H-Tz was evaluated in a pretargeted imaging study and compared to [In]In-DOTA-PEG-BisPy-Tz. Despite minor differences, this study indicated that both evaluated tetrazines are equally suited for pretargeted imaging.
用于各种癌症诊断的靶向核医学成像技术是一个新兴且快速发展的领域。在这方面，四嗪连接目前被认为是最有前途的反应。由于其出色的靶向特性，单克隆抗体通常是首选的靶向载体。在这项工作中，我们使用之前用于[In]In-DOTA-PEG-BisPy-Tz 的设置评估了[Cu]Cu-NOTA-PEG-H-Tz 的性能，从而可以比较这两种有前途的靶向成像剂的性能。评估包括比较化合物的物理化学性质及其在体外阻断测定中的性能。最后，在靶向成像研究中评估了[Cu]Cu-NOTA-PEG-H-Tz，并与[In]In-DOTA-PEG-BisPy-Tz 进行了比较。尽管存在细微差异，但这项研究表明，两种评估的四嗪都同样适合靶向成像。
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