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68Ga-Labeling of RGD peptides and biodistribution
Uppsala University, Disciplinary Domain of Science and Technology, Chemistry, Department of Biochemistry and Organic Chemistry.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Medicine, Department of Radiology, Oncology and Radiation Science, Radiology.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Preclinical PET Platform.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Preclinical PET Platform.
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2012 (English)In: International Journal of Clinical and Experimental Medicine, ISSN 1940-5901, E-ISSN 1940-5901, Vol. 5, no 2, 165-172 p.Article in journal (Refereed) Published
Abstract [en]

Several peptides comprising Arg-Gly-Asp (RGD) domain and macrocyclic chelator were labeled with 68Ga 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 68Ga 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.

Place, publisher, year, edition, pages
2012. Vol. 5, no 2, 165-172 p.
National Category
Basic Medicine Natural Sciences
Identifiers
URN: urn:nbn:se:uu:diva-188961PubMedID: 22567177OAI: oai:DiVA.org:uu-188961DiVA: diva2:580307
Available from: 2012-12-21 Created: 2012-12-21 Last updated: 2017-12-06Bibliographically approved

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PubMedhttp://www.ncbi.nlm.nih.gov/pmc/articles/PMC3342714/

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Velikyan, IrinaEstrada, SergioHall, HåkanLångström, Bengt

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