Methodological Progress of <sup>18</sup>F-Fluoro-Labeling Employing <sup>18</sup>F-FDG as Prosthetic Group

DING Hui; LI Yang; LI Miao

doi:10.7538/hhx.2017.39.03.0193

Journal of Nuclear and Radiochemistry > 2017 > 39(3): 193-207. > DOI: 10.7538/hhx.2017.39.03.0193

DING Hui, LI Yang, LI Miao. Methodological Progress of ¹⁸F-Fluoro-Labeling Employing ¹⁸F-FDG as Prosthetic Group[J]. Journal of Nuclear and Radiochemistry, 2017, 39(3): 193-207. DOI: 10.7538/hhx.2017.39.03.0193

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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

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

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