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| IJCEM Copyright © 2008-All rights reserved. Published by e-Century Publishing Corporation, Madison, WI 53711 |
Int J Clin Exp Med 2012;5(2):165-172
Original Article
68Ga-Labeling of RGD peptides and biodistribution
Elisabeth Blom, Irina Velikyan, Sergio Estrada, Håkan Hall, Taj Mahammad, Chenmin Ding, Manoj Nair, Bengt Långström
Department of Biochemistry and Organic Chemistry, Box 576, Husargatan 3, BMC, SE-751 23 Uppsala, Sweden; Unit of Radiology,
Department of Radiology, Oncology and Radiation Science, Uppsala University, SE-751 85 Uppsala, Sweden; PET Centre, Centre for
Medical Imaging, Uppsala University Hospital, SE-751 85, Uppsala, Sweden; Preclinical PET Platform, Department of Medicinal
Chemistry, Uppsala University; Imperial College, Centre for Pharmacology and Therapeutics, Division of Experimental Medicine,
London, UK; Odense University Hospital, PET & Cyclotron Unit, University of Southern Denmark, Odense, Denmark
Received February 12, 2012; accepted March 14, 2012; Epub April 6, 2012; Published April 30, 2012
Abstract: 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. (IJCEM1202010).
Keywords: 68Ga, RGD, biodistribution
Address all correspondence to:
Dr. Elisabeth Blom
Herlev University Hospital
Dept. Clinical Physiology
54 P1, Herlev Ringvej 75, DK-2730
Herlev, DENMARK.
Tel: +4538689961; Fax: +4544883411
E-mail: elisabeth.blom@heh.regionh.dk
Original Article
68Ga-Labeling of RGD peptides and biodistribution
Elisabeth Blom, Irina Velikyan, Sergio Estrada, Håkan Hall, Taj Mahammad, Chenmin Ding, Manoj Nair, Bengt Långström
Department of Biochemistry and Organic Chemistry, Box 576, Husargatan 3, BMC, SE-751 23 Uppsala, Sweden; Unit of Radiology,
Department of Radiology, Oncology and Radiation Science, Uppsala University, SE-751 85 Uppsala, Sweden; PET Centre, Centre for
Medical Imaging, Uppsala University Hospital, SE-751 85, Uppsala, Sweden; Preclinical PET Platform, Department of Medicinal
Chemistry, Uppsala University; Imperial College, Centre for Pharmacology and Therapeutics, Division of Experimental Medicine,
London, UK; Odense University Hospital, PET & Cyclotron Unit, University of Southern Denmark, Odense, Denmark
Received February 12, 2012; accepted March 14, 2012; Epub April 6, 2012; Published April 30, 2012
Abstract: 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. (IJCEM1202010).
Keywords: 68Ga, RGD, biodistribution
Address all correspondence to:
Dr. Elisabeth Blom
Herlev University Hospital
Dept. Clinical Physiology
54 P1, Herlev Ringvej 75, DK-2730
Herlev, DENMARK.
Tel: +4538689961; Fax: +4544883411
E-mail: elisabeth.blom@heh.regionh.dk
