(18)F-Based Pretargeted PET Imaging Based on Bioorthogonal Diels-Alder Click Chemistry.
(18)F-Based Pretargeted PET Imaging Based on Bioorthogonal Diels-Alder Click Chemistry.
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DOI：
10.1021/acs.bioconjchem.5b00504
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发表时间：
2016-02-17
影响因子：
4.7
通讯作者：
Lewis JS
中科院分区：
文献类型：
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作者：
Meyer JP;Houghton JL;Kozlowski P;Abdel-Atti D;Reiner T;Pillarsetty NV;Scholz WW;Zeglis BM;Lewis JS
提出了一种基于四嗪 (Tz) 和反式环辛烯 (TCO) 之间的生物正交逆电子需求狄尔斯-阿尔德 (IEDDA) 反应的首个 18F 预靶向 PET 成像方法。作为原理验证，利用抗 CA19.9 抗体 5B1 的 TCO 免疫缀合物和 Al[18F]NOTA 标记的四嗪放射性配体对表达 CA19.9 的 BxPC3 胰腺癌异种移植物进行可视化。生物分布和 18F-PET 成像数据清楚地表明，该方法有效地描绘了肿瘤块，注射放射性配体后 4 小时活性浓度高达 6.4%ID/g。
A first-of-its-kind 18F pretargeted PET imaging approach based on the bioorthogonal inverse electron demand Diels–Alder (IEDDA) reaction between tetrazine (Tz) and trans-cyclooctene (TCO) is presented. As proof-of-principle, a TCO-bearing immunoconjugate of the anti-CA19.9 antibody 5B1 and an Al[18F]NOTA-labeled tetrazine radioligand were harnessed for the visualization of CA19.9-expressing BxPC3 pancreatic cancer xenografts. Biodistribution and 18F-PET imaging data clearly demonstrate that this methodology effectively delineates tumor mass with activity concentrations up to 6.4 %ID/g at 4 h after injection of the radioligand.