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Potent Bombesin-like Peptides for GRP-Receptor Targeting of Tumors with 99mTc:  A Preclinical Study
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    Potent Bombesin-like Peptides for GRP-Receptor Targeting of Tumors with 99mTc:  A Preclinical Study
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    Institute of RadioisotopesRadiodiagnostic Products, National Center for Scientific Research “Demokritos”, 15310 Athens, Greece; Biomedica Life Sciences, S. A., 15451 Athens, Greece; Department of Pharmacy, University of Patras, 26500 Patras, Greece; and Institute of Pathology, University of Bern, CH-3010 Bern, Switzerland
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    Journal of Medicinal Chemistry

    Cite this: J. Med. Chem. 2005, 48, 1, 100–110
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    https://doi.org/10.1021/jm049437y
    Published December 4, 2004
    Copyright © 2005 American Chemical Society

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    Four open chain tetraamine-functionalized bombesin (BB) analogues were synthesized [parent tetradecapeptide-based Demobesin 3 and 4 and BB(7−14)-based Demobesin 5 and 6]. Labeling with 99mTc afforded high-purity and high specific activity radiotracers. Peptides showed high affinity for the human GRP-R (GRP-R = gastrin releasing peptide receptor) expressed in PC-3 cells. In human tumors preferentially expressing single bombesin receptor subtypes, they showed high affinity for the GRP-R, less affinity for the NMB−R (NMB-R = neuromedin B receptor) and no affinity for the orphan BB3-R (bombesin subtype 3 receptor). [99mTc]Demobesin 3−6 efficiently internalized in a time- and dose-dependent manner in PC-3 cells and showed a high and specific uptake in human PC-3 xenografts and the pancreas of nude mice. [99mTc]Demobesin 3 and 4 were rapidly excreted via the kidneys while the truncated analogues were predominantly processed by the hepatobiliary system. Patient studies are scheduled for validating the suitability of [99mTc]Demobesin 3 and 4 in the GRP-R-targeted imaging of tumors.

    Copyright © 2005 American Chemical Society

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     National Center for Scientific Research “Demokritos”.

     Biomedica Life Sciences.

    §

     University of Patras.

     University of Bern.

    *

     Corresponding author. Phone:  +30210-6503908. Fax:  +30210-6524480. E-mail:  [email protected].

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    Cite this: J. Med. Chem. 2005, 48, 1, 100–110
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    https://doi.org/10.1021/jm049437y
    Published December 4, 2004
    Copyright © 2005 American Chemical Society

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