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Chelator-Free Radiolabeling of Nanographene: Breaking the Stereotype of Chelation.


ABSTRACT: Macrocyclic chelators have been widely employed in the realm of nanoparticle-based positron emission tomography (PET) imaging, whereas its accuracy remains questionable. Here, we found that 64 Cu can be intrinsically labeled onto nanographene based on interactions between Cu and the ??electrons of graphene without the need of chelator conjugation, providing a promising alternative radiolabeling approach that maintains the native in?vivo pharmacokinetics of the nanoparticles. Due to abundant ??bonds, reduced graphene oxide (RGO) exhibited significantly higher labeling efficiency in comparison with graphene oxide (GO) and exhibited excellent radiostability in?vivo. More importantly, nonspecific attachment of 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA) on nanographene was observed, which revealed that chelator-mediated nanoparticle-based PET imaging has its inherent drawbacks and can possibly lead to erroneous imaging results in?vivo.

SUBMITTER: Shi S 

PROVIDER: S-EPMC5345346 | biostudies-literature | 2017 Mar

REPOSITORIES: biostudies-literature

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Chelator-Free Radiolabeling of Nanographene: Breaking the Stereotype of Chelation.

Shi Sixiang S   Xu Cheng C   Yang Kai K   Goel Shreya S   Valdovinos Hector F HF   Luo Haiming H   Ehlerding Emily B EB   England Christopher G CG   Cheng Liang L   Chen Feng F   Nickles Robert J RJ   Liu Zhuang Z   Cai Weibo W  

Angewandte Chemie (International ed. in English) 20170207 11


Macrocyclic chelators have been widely employed in the realm of nanoparticle-based positron emission tomography (PET) imaging, whereas its accuracy remains questionable. Here, we found that <sup>64</sup> Cu can be intrinsically labeled onto nanographene based on interactions between Cu and the π electrons of graphene without the need of chelator conjugation, providing a promising alternative radiolabeling approach that maintains the native in vivo pharmacokinetics of the nanoparticles. Due to ab  ...[more]

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