Bombesin receptor antagonists may be preferable to agonists for tumor targeting

Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine
Renzo CescatoJean Claude Reubi

Abstract

Two bombesin analogs, Demobesin 4 and Demobesin 1, were characterized in vitro as gastrin-releasing peptide (GRP) receptor agonist and antagonist, respectively, and were compared as (99m)Tc-labeled ligands for their in vitro and in vivo tumor-targeting properties. N(4)-[Pro(1),Tyr(4),Nle(14)]Bombesin (Demobesin 4) and N(4)-[d-Phe(6),Leu-NHEt(13),des-Met(14)]bombesin(6-14) (Demobesin 1) were characterized in vitro for their binding properties with GRP receptor autoradiography using GRP receptor-transfected HEK293 cells, PC3 cells, and human prostate cancer specimens. Their ability to modulate calcium mobilization in PC3 and transfected HEK293 cells was analyzed as well as their ability to trigger internalization of the GRP receptor in transfected HEK293 cells, as determined qualitatively by immunofluorescence microscopy and quantitatively by enzyme-linked immunosorbent assay (ELISA). Further, their internalization properties as (99m)Tc-labeled radioligands were tested in vitro in both cell lines. Finally, their biodistribution was analyzed in PC3 tumor-bearing mice. A comparable binding affinity with the 50% inhibitory concentration (IC(50)) in the nanomolar range was measured for Demobesin 4 and Demobesin 1 in all tested tissue...Continue Reading

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Citations

Apr 17, 2010·European Journal of Nuclear Medicine and Molecular Imaging·Jean Claude ReubiJean E Rivier
Aug 19, 2010·European Journal of Nuclear Medicine and Molecular Imaging·Rosalba MansiHelmut R Maecke
Jan 7, 2011·European Journal of Nuclear Medicine and Molecular Imaging·Beatrice Waser, Jean Claude Reubi
Mar 6, 2012·European Journal of Nuclear Medicine and Molecular Imaging·Melpomeni Fani, Helmut R Maecke
Mar 6, 2012·European Journal of Nuclear Medicine and Molecular Imaging·K P Koopmans, A W J M Glaudemans
Dec 1, 2009·Amino Acids·Hao HongWeibo Cai
Sep 24, 2008·Bioconjugate Chemistry·Wael R Abd-ElgalielSusan Z Lever
Jan 28, 2010·Biochemistry·Seulki LeeXiaoyuan Chen
Mar 17, 2010·Chemical Reviews·Seulki LeeXiaoyuan Chen
Oct 14, 2009·Molecular BioSystems·Raphael AlfordHisataka Kobayashi
Mar 7, 2013·Cancer Biotherapy & Radiopharmaceuticals·Clément MorgatPhilippe Fernandez
Jan 15, 2013·Journal of Amino Acids·Jyothi Thundimadathil
Oct 2, 2012·PloS One·Hanwen ZhangHelmut R Maecke
Feb 16, 2011·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Kimberly A LearsBuck E Rogers
Feb 13, 2014·European Journal of Nuclear Medicine and Molecular Imaging·Beatrice Waser, Jean Claude Reubi
Feb 26, 2010·European Journal of Nuclear Medicine and Molecular Imaging·Rogier P J SchroederMarion de Jong
Jul 23, 2014·European Journal of Nuclear Medicine and Molecular Imaging·Lisa BodeiIrvin M Modlin
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Nov 4, 2010·Wiley Interdisciplinary Reviews. Nanomedicine and Nanobiotechnology·Sumita RahaGayle Woloschak
Oct 24, 2013·The Prostate·Meike KörnerJean Claude Reubi

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