Comparison of the binding and internalization properties of 12 DOTA-coupled and ¹¹¹In-labelled CCK2/gastrin receptor binding peptides: a collaborative project under COST Action BM0607

Aloj, Luigi; Aurilio, Michela; Rinaldi, Valentina; D'ambrosio, Laura; Tesauro, Diego; Peitl, Petra Kolenc; Maina, Theodosia; Mansi, Rosalba; von Guggenberg, Elisabeth; Joosten, Lieke; Sosabowski, Jane K; Breeman, Wouter A P; De Blois, Erik; Koelewijn, Stuart; Melis, Marleen; Waser, Beatrice; Beetschen, Karin; Reubi, Jean-Claude; de Jong, Marion (2011). Comparison of the binding and internalization properties of 12 DOTA-coupled and ¹¹¹In-labelled CCK2/gastrin receptor binding peptides: a collaborative project under COST Action BM0607. European journal of nuclear medicine and molecular imaging, 38(8), pp. 1417-25. Berlin: Springer 10.1007/s00259-011-1816-y

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Specific overexpression of cholecystokinin 2 (CCK2)/gastrin receptors has been demonstrated in several tumours of neuroendocrine origin. In some of these cancer types, such as medullary thyroid cancer (MTC), a sensitive diagnostic modality is still unavailable and therapeutic options for inoperable lesions are needed. Peptide receptor radionuclide therapy (PRRT) may be a viable therapeutic strategy in the management of these patients. Several CCK2R-targeted radiopharmaceuticals have been described in recent years. As part of the European Union COST Action BM0607 we studied the in vitro and in vivo characteristics of 12 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA)-conjugated CCK2R binding peptides. In the present study, we analysed binding and internalization characteristics. Stability, biodistribution and imaging studies have been performed in parallel by other centres involved in the project.

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