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

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• 作者：Luigi Aloj (1) l.aloj@istitutotumori.na.it r>Michela Aurilio (1) r>Valentina Rinaldi (1) r>Laura D’ambrosio (1) r>Diego Tesauro (2) r>Petra Kolenc Peitl (3) r>Theodosia Maina (4) r>Rosalba Mansi (5) r>Elisabeth von Guggenberg (6) r>Lieke Joosten (7) r>Jane K. Sosabowski (8) r>Wouter A. P. Breeman (9) r>Erik De Blois (9) r>Stuart Koelewijn (9) r>Marleen Melis (9) r>Beatrice Waser (10) r>Karin Beetschen (10) r>Jean Claude Reubi (10) r>Marion de Jong (9)
• 关键词：Gastrin – Cholecystokinin – Tumour – DOTA
• 刊名：European Journal of Nuclear Medicine and Molecular Imaging
• 出版年：2011
• 出版时间：August 2011
• 年：2011
• 卷：38
• 期：8
• 页码：1417-1425
• 全文大小：316.2 KB
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Macrocyclic chelator-coupled gastrin-based radiopharmaceuticals for targeting of gastrin receptor-expressing tumours. Eur J Nucl Med Mol Imaging 2008;35:1868–77. doi: r>7. Aloj L, Caracò C, Panico M, Zannetti A, Del Vecchio S, Tesauro D, et al. In vitro and in vivo evaluation of 111In-DTPAGlu-G-CCK8 for cholecystokinin-B receptor imaging. J Nucl Med 2004;45:485–94. r>8. Reubi JC, Waser B, Schaer JC, Laederach U, Erion J, Srinivasan A, et al. Unsulfated DTPA- and DOTA-CCK analogs as specific high-affinity ligands for CCK-B receptor-expressing human and rat tissues in vitro and in vivo. Eur J Nucl Med 1998;25:481–90. r>9. von Guggenberg E, Sallegger W, Helbok A, Ocak M, King R, Mather SJ, et al. Cyclic minigastrin analogues for gastrin receptor scintigraphy with technetium-99m: preclinical evaluation. J Med Chem 2009;52:4786–93. doi: r>10. Roosenburg S, Laverman P, Joosten L, Eek A, Oyen WJ, de Jong M, et al. Stabilized (111)In-labeled sCCK8 analogues for targeting CCK2-receptor positive tumors: synthesis and evaluation. Bioconjug Chem 2010;21:663–70. doi: r>11. Mather SJ, McKenzie AJ, Sosabowski JK, Morris TM, Ellison D, Watson SA. Selection of radiolabeled gastrin analogs for peptide receptor-targeted radionuclide therapy. J Nucl Med 2007;48:615–22. r>12. Sosabowski JK, Matzow T, Foster JM, Finucane C, Ellison D, Watson SA, et al. Targeting of CCK-2 receptor-expressing tumors using a radiolabeled divalent gastrin peptide. J Nucl Med 2009;50:2082–9. doi: r>13. Nock BA, Maina T, Béhé M, Nikolopoulou A, Gotthardt M, Schmitt JS, et al. CCK-2/gastrin receptor-targeted tumor imaging with (99m)Tc-labeled minigastrin analogs. J Nucl Med 2005;46:1727–36. r>14. Fr?berg AC, de Jong M, Nock BA, Breeman WA, Erion JL, Maina T, et al. Comparison of three radiolabelled peptide analogues for CCK-2 receptor scintigraphy in medullary thyroid carcinoma. Eur J Nucl Med Mol Imaging 2009;36:1265–72. doi: r>15. Béhé M, Behr TM. Cholecystokinin-B (CCK-B)/gastrin receptor targeting peptides for staging and therapy of medullary thyroid cancer and other CCK-B receptor expressing malignancies. Biopolymers 2002;66:399–418. doi: r>16. Béhé M, Kluge G, Becker W, Gotthardt M, Behr TM. Use of polyglutamic acids to reduce uptake of radiometal-labeled minigastrin in the kidneys. J Nucl Med 2005;46:1012–5. r>17. Laverman P, Roosenburg S, Gotthardt M, Park J, Oyen WJ, de Jong M, et al. Targeting of a CCK(2) receptor splice variant with (111)In-labelled cholecystokinin-8 (CCK8) and (111)In-labelled minigastrin. Eur J Nucl Med Mol Imaging 2008;35:386–92. doi: r>18. von Guggenberg E, Dietrich H, Skvortsova I, Gabriel M, Virgolini IJ, Decristoforo C. 99mTc-labelled HYNIC-minigastrin with reduced kidney uptake for targeting of CCK-2 receptor-positive tumours. Eur J Nucl Med Mol Imaging 2007;34:1209–18. doi: r>19. Ocak M, Helbok A, Rangger C, Peitl PK, Nock B, Morelli G, et al. Comparison of biological stability and metabolism of CCK2-receptor targeting peptides, a collaborative project under COST BM0607. Eur J Nucl Med Mol Imaging 2011, in press. r>20. Laverman P, Joosten L, Eek A, Roosenburg S, Peitl PK, Maina T, et al. Comparative biodistribution of twelve gastrin/CCK2 receptor targeting peptides. Eur J Nucl Med Mol Imaging 2011, in press. r>21. Sosabowski JK, Finucane C, Foster JM, Ellison D, Burnet J, Laverman P, et al. Comparison of 111In-labelled CCK2-receptor targeting peptides using NanoSPECT/CT imaging. Submitted for publication 2011. r>22. Giragossian C, Mierke DF. Intermolecular interactions between cholecystokinin-8 and the third extracellular loop of the cholecystokinin-2 receptor. Biochemistry 2002;41:4560–6. r>23. Roosenburg S, Laverman P, van Delft FL, Boerman OC. Radiolabeled CCK/gastrin peptides for imaging and therapy of CCK2 receptor-expressing tumors. Amino Acids 2010. doi:10.1007/s00726-010-0501-y. r>24. D’Andrea LD, Testa I, Panico M, Di Stasi R, Caracò C, Tarallo L, et al. In vivo and in vitro characterization of CCK8 bearing a histidine-based chelator labeled with 99mTc-tricarbonyl. Biopolymers 2008;90:707–12. doi: r>25. Tornesello AL, Aurilio M, Accardo A, Tarallo L, Barbieri A, Arra C, et al. Gastrin and cholecystokinin peptide-based radiopharmaceuticals: an in vivo and in vitro comparison. J Pept Sci 2011;17:405–12. doi: r>26. Marsouvanidis PJ, Tatsi A, Nock BA, Krenning EP, Maina T, de Jong M. [111In]Sargastrin, a Gastrin I-based radioligand targeting CCK2-R-positive tumors in vivo. Eur J Nucl Med Mol Imaging 2009;36:S259. r>27. Kolenc-Peitl P, Mansi R, Tamma ML, Gmeiner-Stopar T, Sollner-Dolenc M, Waser B, et al. Highly improved metabolic stability and pharmacokinetics of indium-111-DOTA-gastrin conjugates for targeting of the gastrin receptor. J Med Chem. In press 2011.
• 作者单位：1. AF Medicina Nucleare, Istituto Nazionale Tumori, Fondazione “G. Pascale- Via M. Semmola, 80131 Naples, Italy2. CIRPeB, Università “Federico II- Naples, Italy3. Department of Nuclear Medicine, University Medical Centre Ljubljana, Ljubljana, Slovenia4. Molecular Radiopharmacy, Institute of Radioisotopes-Radiodiagnostic Products, National Center for Scientific Research Demokritos, Athens, Greece5. Department of Nuclear Medicine, University Hospital Freiburg, Freiburg, Germany6. Department of Nuclear Medicine, Innsbruck Medical University, Innsbruck, Austria7. Department of Nuclear Medicine, Radboud University Nijmegen Medical Centre, Nijmegen, The Netherlands8. Centre for Molecular Oncology and Imaging, Institute of Cancer, Barts and the London Queen Mary’s School of Medicine and Dentistry, London, UK9. Department of Nuclear Medicine, Erasmus MC, Rotterdam, The Netherlands10. University of Berne, Berne, Switzerland
• 刊物类别：Medicine
• 刊物主题：Medicine & Public Healthr>Nuclear Mediciner>Imaging and Radiologyr>Orthopedicsr>Cardiologyr>Oncologyr>
• 出版者：Springer Berlin / Heidelberg
• ISSN：1619-7089

文摘

Purpose 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.