(68)Ga-Labeling of RGD peptides and biodistribution

Elisabeth Blom, Irina Velikyan, Sergio Estrada, Håkan Hall, Taj Muhammad, Chenmin Ding, Manoj Nair, Bengt Långström

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Several peptides comprising Arg-Gly-Asp (RGD) domain and macrocyclic chelator were labeled with (68)Ga for the imaging of angiogenesis. The analogues varied in peptide constitution, linker and chelator type. The labeling efficiency did not vary with the peptide constitution and linker type, but depended on the chelator type. Four of the compounds containing 2,2',2'',2'''-(1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrayl)tetraacetic acid (DOTA) chelator were labeled at 90 ± 5°C using conventional or microwave heating reaching 90% of (68)Ga incorporation after 5 and 2 min respectively, when the concentration of the precursor was 2.5 μM. The compound having 2,2',2''-(1,4,7-triazonane-1,4,7-triyl)triacetic acid (NOTA) as the chelator could be labeled at room temperature within 5 min using 2.5 μM peptide precursor. Two of the compounds contained a poly (ethylene glycol) (PEG) linker to the chelator. The biodistribution of the analogues was studied in male rats.

Original languageEnglish
JournalInternational Journal of Clinical and Experimental Medicine
Issue number2
Pages (from-to)165-72
Number of pages8
Publication statusPublished - 2012
Externally publishedYes

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    Blom, E., Velikyan, I., Estrada, S., Hall, H., Muhammad, T., Ding, C., Nair, M., & Långström, B. (2012). (68)Ga-Labeling of RGD peptides and biodistribution. International Journal of Clinical and Experimental Medicine, 5(2), 165-72.