Development of a kit-like radiofluorinated biomolecule leading to a controlled self-assembly of 18F nanoparticles for a smart PET imaging application

• Published in: Chemical communications (Cambridge, England) Vol. 53; no. 48; pp. 6476 - 6479
• Main Authors: Lin, Jianguo, Wang, Wei, Li, Ke, Huang, Hongbo, Lv, Gaochao, Peng, Ying, Luo, Shineng, Qiu, Ling
• Format: Journal Article
• Language: English
• Published: 13.06.2017
• Subjects: chemical compounds; Condensation; condensation reactions; image analysis; Imaging; membrane permeability; Nanoparticles; neoplasms; Platforms; Positron emission; positron-emission tomography; Radiochemistry; Self assembly; Tomography; tracer techniques
• ISSN: 1364-548X; 1359-7345; 1364-548X
• DOI: 10.1039/c7cc03040a

A kit-like 18F-fluorination method has been successfully applied to prepare an activatable probe 1 with good radiochemical yield and high specific activity. The probe has good in vitro stability and favorable cell membrane permeability. A controlled condensation reaction was initiated, and self-assembly into nanoparticles occurred when the probe was in a reducing environment. Positron emission tomography (PET) imaging of the biothiol level in living subjects was conveniently and precisely realized using this probe. The present study may provide a new platform for the development of "smart" PET tracers for tumor imaging.A kit-like 18F-fluorination method has been successfully applied to prepare an activatable probe 1 with good radiochemical yield and high specific activity. The probe has good in vitro stability and favorable cell membrane permeability. A controlled condensation reaction was initiated, and self-assembly into nanoparticles occurred when the probe was in a reducing environment. Positron emission tomography (PET) imaging of the biothiol level in living subjects was conveniently and precisely realized using this probe. The present study may provide a new platform for the development of "smart" PET tracers for tumor imaging.