以<sup>18</sup>F-FDG为辅基的<sup>18</sup>F-氟标记方法研究进展

丁晖; 李阳; 李淼

doi:10.7538/hhx.2017.39.03.0193

以¹⁸F-FDG为辅基的¹⁸F-氟标记方法研究进展

西安交通大学第一附属医院医学影像科,陕西西安710061

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- 刊出日期: 2017-06-19

Methodological Progress of ¹⁸F-Fluoro-Labeling Employing ¹⁸F-FDG as Prosthetic Group

Department of Radiology, the First Affiliated Hospital, Xi’an Jiaotong University, Xi’an 710061, China

摘要

摘要: 在核医学分子影像领域用于正电子示踪剂的¹⁸F-氟标记方法中，基于含¹⁸F-氟中间体分子（即辅基）的方法其反应条件温和、化学选择性好，产物易纯化，是进行¹⁸F-氟标记的经典策略之一。2-¹⁸F-氟代-2-脱氧-D-葡萄糖（2-¹⁸F-fluoro-2-deoxy-D-glucose, ¹⁸F-FDG）是目前临床最常用的正电子示踪剂，其分子结构简单、亲水性强、易获得，是用于间接¹⁸F-氟标记的理想辅基。通过比较其方法学参数，并分析标记产物性能可知，以¹⁸F-FDG为辅基的间接¹⁸F-氟标记方法有酶法、成肟法、巯基连接法、“点击化学”法等，在小分子、肽、酶和纳米粒的¹⁸F-氟标记研究中均有报道。此外，微流控芯片等新技术在上述方法中也有应用。与¹⁸F-FDG连接可方便地同时实现被标记分子糖基化和¹⁸F-氟标记，显著改善标记产物的体内分布和消除特性，虽存在反应步骤多、被标记分子需修饰等局限，但以¹⁸F-FDG为辅基进行¹⁸F-氟标记仍是一种具有较高可行性和应用价值的间接¹⁸F-氟标记策略。
- ¹⁸F-氟代脱氧葡萄糖 /
- 辅基 /
- 间接标记 /
- ¹⁸F-氟标记 /
- 方法学
Abstract: In the field of nuclear medicine molecular imaging, ¹⁸F-fluoro-labeling methods based on intermediate molecule containing ¹⁸F-fluoro (i.e. prosthetic groups) has mild reaction condition, fine chemo-selectivity and simple purification for product. Therefore, the indirect ¹⁸F-fluoro-labeling via prosthetic group is a classical strategy in the development of tracers for positron emission tomography(PET). 2-¹⁸F-fluoro-2-deoxy-D-glucose (¹⁸F-FDG), which has simple scaffold, high hydrophilicity and easy accessibility, is the most popular tracer in PET practice and ideal prosthetic molecule for ¹⁸F-fluoro-labeling. In this paper, we review related methodological progress in literatures. The methodological parameters and product properties in these reports are compared and analyzed. Overall, several ¹⁸F-fluoro-labeling solutions employing ¹⁸F-FDG have emerged, including enzymic method, oxime formation, sulfydryl ligation and click chemistry. They were tried in the ¹⁸F-fluoro-labeling of small molecules, peptides, enzymes and nanoparticles. New technology such as microfluidic reactor was applied in some solutions aforementioned. Glycosylation and ¹⁸F-fluoro-labeling of precursor molecule can be achieved synchronically by the conjugation with ¹⁸F-FDG. Consequently, the in vivo bio-kinetics of labeling product are significantly improved. Although the ¹⁸F-fluoro-labeling employing ¹⁸F-FDG needs multi-step reaction and especial modification in precursor, it is generally a feasible and valuable indirect labeling strategy.
- ¹⁸F-FDG /
- prosthetic group /
- indirect labeling /
- ¹⁸F-fluoro-labeling /
- methodology

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参考文献(43)

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以18F-FDG为辅基的18F-氟标记方法研究进展

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出版历程

Methodological Progress of 18F-Fluoro-Labeling Employing 18F-FDG as Prosthetic Group

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出版历程

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以¹⁸F-FDG为辅基的¹⁸F-氟标记方法研究进展

Methodological Progress of ¹⁸F-Fluoro-Labeling Employing ¹⁸F-FDG as Prosthetic Group