Comparison of biological stability and metabolism of CCK2 receptor targeting peptides, a collaborative project under COST BM0607(708 views) Ocak M, Helbok A, Rangger C, Peitl PK, Nock BA, Morelli G, Eek A, Sosabowskijk, Breeman WA, Reubi JC, Decristoforo C
Keywords: 177lu, Cck, Cholecystokinin Receptor, Gastrin, In Vitro Stability, In Vivo Stability, Metabolism, 10 Tetraazacyclododecane 1, 10 Tetraacetic Acid, Cholecystokinin B Receptor, Gastrin Derivative, Peptide, Radioligand, Animal Tissue, Article, Controlled Study, Female, High Performance Liquid Chromatography, Human, Human Tissue, In Vitro Study, Isotope Labeling, Lung Small Cell Cancer, Matrix Assisted Laser Desorption Ionization Time Of Flight Mass Spectrometry, Mouse, Nonhuman, Protein Binding, Protein Cleavage, Protein Metabolism, Thyroid Medullary Carcinoma, Urinalysis, Amino Acid Sequence, Binding Sites, Cooperative Behavior, Methionine, Molecular Sequence Data, Oxidation-Reduction, Protein Stability,
Affiliations: *** IBB - CNR ***
Clinical Department of Nuclear Medicine, Innsbruck Medical University, Anichstrasse 35, 6020 Innsbruck, Austria
Department of Pharmaceutical Technology, Pharmacy Faculty, Istanbul University, Istanbul, Turkey
Department for Nuclear Medicine, University Medical Centre Ljubljana, Ljubljana, Slovenia
Molecular Radiopharmacy, Institute of Radioisotopes-Radiodiagnostic Products, National Center for Scientific Research Demokritos, Athens, Greece
Department of Biological Sciences, CIRPeB, University of Naples Federico II and IBB-CN, Naples, Italy
Centre for Molecular Oncology and Imaging, Institute of Cancer, Barts and the London Queen Mary's School of Medicine and Dentistry, London, United Kingdom
Division of Cell Biology, Experimental Cancer Research Institute of Pathology, University of Berne, Berne, Switzerland
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Reubi, J. C., Maecke, H. R., Peptide-based probes for cancer imaging (2008) J Nucl Med, 49 (11), pp. 1735-1738
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Behr, T. M., Behe, M. P., Cholecystokinin-B/gastrin receptor-targeting peptides for staging and therapy of medullary thyroid cancer and other cholecystokinin-B receptor-expressing malignancies (2002) Seminars in Nuclear Medicine, 32 (2), pp. 97-109
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Mather, S. J., McKenzie, A. J., Sosabowski, J. K., Morris, T. M., Ellison, D., Watson, S. A., Selection of radiolabeled gastrin analogs for peptide receptor-targeted radionuclide therapy (2007) Journal of Nuclear Medicine, 48 (4), pp. 615-622. , http: //jnm. snmjournals. org/cgi/reprint/48/4/615, DOI 10. 2967/jnumed. 106. 037085
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Comparison of biological stability and metabolism of CCK2 receptor targeting peptides, a collaborative project under COST BM0607
Stability of radiolabelled cholecystokinin 2 (CCK2) receptor targeting peptides has been a major limitation in the use of such radiopharmaceuticals especially for targeted radionuclide therapy applications, e.g. for treatment of medullary thyroid carcinoma (MTC). The purpose of this study was to compare the in vitro stability of a series of peptides binding to the CCK2 receptor [selected as part of the COST Action on Targeted Radionuclide Therapy (BM0607)] and to identify major cleavage sites. Twelve different 1,4,7,10-tetraazacyclododecane-N,N',N'',N'''-tetraacetic acid (DOTA)-minigastrin/CCK conjugates were provided within an European COST Action (BM0607) by different laboratories and radiolabelled with (177)Lu. Their in vitro stabilities were tested in fresh human serum. Radiochemical yields (RCY) and intact radioligands for half-life calculations were determined by radio-HPLC. Matrix-assisted laser desorption/ionisation time-of-flight mass spectrometry (MALDI-TOF MS) analysis of metabolites was performed to identify cleavage products using conjugates labelled with excess stable (nat)Lu, incubated in serum at 37A degrees C. Urine metabolite analysis after injection in normal mice was performed by radio-HPLC analysis. Variable stability in human serum was found for the different peptides with calculated half-lives between 4.5 +/- 0.1 h and 198 +/- 0.1 h (n = 2). In urine of normal mice only metabolised peptide fragments were detected even at short times after injection for all peptides. MALDI-TOF MS revealed a major cleavage site of all minigastrin derivatives between Asp and Phe-NH(2) at the C-terminal end. Development of CCK2 receptor ligands especially for therapeutic purposes in patients with MTC or small cell lung cancer (SCLC) is still ongoing in different laboratories. This comparative study provided valuable insight into the importance of biological stability especially in the context of other results of this comparative trial within the COST Action BM0607.
Comparison of biological stability and metabolism of CCK2 receptor targeting peptides, a collaborative project under COST BM0607
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