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Comparative biodistribution of 12 111In-labelled gastrin/CCK2 receptor-targeting peptidesLaverman, Peter ...PURPOSE: Cholecystokinin 2 (CCK-2) receptor overexpression has been demonstrated in various tumours such as medullary thyroid carcinomas and small-cell lung cancers. Due to this high expression, ... CCK-2 receptors might be suitable targets for radionuclide imaging and/or radionuclide therapy. Several CCK-2 receptor-binding radiopeptides have been developed and some have been tested in patients. Here we aimed to compare the in vivo tumour targeting properties of 12 (111)In-labelled 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA)-conjugated gastrin/CCK2 receptor-binding peptides. METHODS: Two CCK8-based peptides and ten gastrin-based peptide analogues were tested. All peptides were conjugated with DOTA and labelled with (111)In. Biodistribution studies were performed in mice with subcutaneous CCK2/gastrin receptor-expressing tumours and with receptor-negative tumours contralaterally. Biodistribution was studied by counting dissected tissues at 1 and 4 h after injection. RESULTS: Both the CCK analogues displayed relatively low tumour uptake (approximately 2.5%ID/g) as compared to minigastrin analogues. Two linear minigastrin peptides (MG0 and sargastrin) displayed moderate tumour uptake at both 1 and 4 h after injection, but also very high kidney uptake (both higher than 48%ID/g). The linear MG11, lacking the penta-Glu sequence, showed lower tumour uptake and also low kidney uptake. Varying the N-terminal Glu residues in the minigastrinanalogues led to improved tumour targeting properties, with PP-F11 displaying the optimal biodistribution. Besides the monomeric linear peptides,a cyclized peptide and a divalent peptide were tested. CONCLUSION: Based on these studies, optimal peptides for peptide receptor radionuclide targeting of CCK2/gastrin receptor-expressing tumours were the linear minigastrin analogue with six D-Glu residues (PP-F11), the divalent analogue MGD5 and the cyclic peptide cyclo-MG1. These peptides combined high tumour uptake with low kidney retention, and may therefore be good candidates for future clinical studies.Vir: European journal of nuclear medicine and molecular imaging. - ISSN 1619-7070 (Vol. 38, no. 8, 2011, str. 1410-1416)Vrsta gradiva - članek, sestavni delLeto - 2011Jezik - angleškiCOBISS.SI-ID - 3067505
Avtor
Laverman, Peter |
Joosten, Lieke |
Eek, Annemarie |
Roosenburg, Susan |
Kolenc, Petra, 1976- |
Maina, Theodosia |
Mäcke, Helmut |
Aloj, Luigi |
Guggenberg von, Elisabeth |
Sosabowski, Jane K. |
De Jong, Marion |
Reubi, Jean Claude |
Oyen, Wim J.G. |
Boerman, Otto C.
Teme
DOTA |
gastrin |
tumor |
holecistokinin
vir: European journal of nuclear medicine and molecular imaging. - ISSN 1619-7070 (Vol. 38, no. 8, 2011, str. 1410-1416)
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Laverman, Peter | |
Joosten, Lieke | |
Eek, Annemarie | |
Roosenburg, Susan | |
Kolenc, Petra, 1976- | 23364 |
Maina, Theodosia | |
Mäcke, Helmut | |
Aloj, Luigi | |
Guggenberg von, Elisabeth | |
Sosabowski, Jane K. | |
De Jong, Marion | |
Reubi, Jean Claude | |
Oyen, Wim J.G. | |
Boerman, Otto C. |
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