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Chelator‐Free Radiolabeling of Nanographene: Breaking the Stereotype of Chelation
Author(s) -
Shi Sixiang,
Xu Cheng,
Yang Kai,
Goel Shreya,
Valdovinos Hector F.,
Luo Haiming,
Ehlerding Emily B.,
England Christopher G.,
Cheng Liang,
Chen Feng,
Nickles Robert J.,
Liu Zhuang,
Cai Weibo
Publication year - 2017
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201610649
Subject(s) - graphene , chelation , in vivo , nanoparticle , materials science , oxide , nanotechnology , positron emission tomography , combinatorial chemistry , chemistry , inorganic chemistry , medicine , microbiology and biotechnology , metallurgy , biology , radiology
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 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 abundant π 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.

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