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European Journal of Nuclear Medicine and Molecular Imaging

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Open Access 01-08-2011 | Editorial Commentary

Evaluation of CCK2 receptor binding ligands: the inheritance of Thomas Behr

Authors: Otto C. Boerman, Luigi Aloj

Published in: European Journal of Nuclear Medicine and Molecular Imaging | Issue 8/2011

Excerpt

This issue of the European Journal of Nuclear Medicine and Molecular Imaging contains a series of studies comparing the in vitro and in vivo characteristics of a series of 12 cholecystokinin (CCK) receptor (CCKR) binding ligands [1‐3]. Nine European research groups from Athens, Basel, Freiburg, Innsbruck, Ljubljana, London, Naples, Nijmegen and Rotterdam supported by a COST Action (BM0607) of the European Union have cooperated to carry out these studies. The project aimed to evaluate the in vitro and in vivo properties of 12 DOTA-conjugated CCK2R ligands. The ligands were synthesized by the groups in Athens, Freiburg, Innsbruck, Nijmegen, London and Ljubljana and the following characteristics of the ligands were studied in standardized model systems:

The affinity (IC₅₀) of the ligands for the CCK2R was determined in Berne
The internalization kinetics of the ligands were determined in Naples and in Rotterdam
The stability of the ligands was evaluated in Innsbruck
The in vivo targeting properties of CCK2R-expressing tumours were evaluated in Nijmegen and in London

…

Laverman P, Joosten L, Eek A, Roosenburg S, Peitl PK, Maina T, et al. Comparative biodistribution of 12 (111)In-labelled gastrin/CCK2 receptor-targeting peptides. Eur J Nucl Med Mol Imaging, doi:10.1007/s00259-011-1806-0.

Aloj L, Aurilio M, Rinaldi V, D’ambrosio L, Tesauro D, Peitl PK, et al. Comparison of the binding and internalization properties of 12 DOTA-coupled and (111)In-labelled CCK2/gastrin receptor binding peptides: a collaborative project under COST Action BM0607. Eur J Nucl Med Mol Imaging, doi:10.1007/s00259-011-1816-y.

Ocak M, Helbok A, Rangger C, Peitl PK, Nock BA, 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, doi:10.1007/s00259-011-1818-9.

Behr TM, Jenner N, Radetzky S, Béhe M, Gratz S, Yücekent S, et al. Targeting of cholecystokinin-B/gastrin receptors in vivo: preclinical and initial clinical evaluation of the diagnostic and therapeutic potential of radiolabelled gastrin. Eur J Nucl Med 1998;25(4):424–30.PubMedCrossRef

Reubi JC, Schaer JC, Waser B. Cholecystokinin(CCK)-A and CCK-B/gastrin receptors in human tumors. Cancer Res 1997;57(7):1377–86.PubMed

Behr TM, Jenner N, Béhé M, Angerstein C, Gratz S, Raue F, et al. Radiolabeled peptides for targeting cholecystokinin-B/gastrin receptor-expressing tumors. J Nucl Med 1999;40(6):1029–44.PubMed

Title: Evaluation of CCK2 receptor binding ligands: the inheritance of Thomas Behr
Authors: Otto C. Boerman
Luigi Aloj
Publication date: 01-08-2011
Publisher: Springer-Verlag
Published in: European Journal of Nuclear Medicine and Molecular Imaging / Issue 8/2011
Print ISSN: 1619-7070
Electronic ISSN: 1619-7089
DOI: https://doi.org/10.1007/s00259-011-1848-3

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