| |  Online-Ressource |
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| Verfasst von: | Lindner, Simon [VerfasserIn]  |
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| | Rudolf, Henning [VerfasserIn] |
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| | Palumbo, Giovanna [VerfasserIn] |
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| | Oos, Rosel [VerfasserIn] |
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| | Antons, Melissa Joy [VerfasserIn] |
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| | Hübner, Ralph [VerfasserIn] |
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| | Bartenstein, Peter [VerfasserIn] |
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| | Schirrmacher, Ralf [VerfasserIn] |
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| | Wängler, Björn [VerfasserIn] |
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| | Wängler, Carmen [VerfasserIn] |
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| Titel: | Are heterobivalent GRPR- and VPAC1R-bispecific radiopeptides suitable for efficient in vivo tumor imaging of prostate carcinomas? |
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| Verf.angabe: | Simon Lindner, Henning Rudolf, Giovanna Palumbo, Rosel Oos, Melissa Antons, Ralph Hübner, Peter Bartenstein, Ralf Schirrmacher, Björn Wängler, Carmen Wängler |
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| E-Jahr: | 2021 |
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| Jahr: | 15 September 2021 |
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| Umfang: | 7 S. |
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| Fussnoten: | Gesehen am 06.02.2023 |
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| Titel Quelle: | Enthalten in: Bioorganic & medicinal chemistry letters |
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| Ort Quelle: | Amsterdam [u.a.] : Elsevier Science, 1991 |
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| Jahr Quelle: | 2021 |
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| Band/Heft Quelle: | 48(2021) vom: Sept., Artikel-ID 128241, Seite 1-7 |
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| ISSN Quelle: | 1464-3405 |
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| Abstract: | Receptor-specific peptides labeled with positron emitters play an important role in the clinical imaging of several malignancies by positron emission tomography (PET). Radiolabeled heterobivalent bispecific peptidic ligands (HBPLs) can target more than one receptor type and by this - besides exhibiting other advantages - increase tumor imaging sensitivity. In the present study, we show the initial in vivo evaluation of the most potent heterobivalent gastrin-releasing peptide receptor (GRPR)- and vasoactive intestinal peptide receptor subtype 1 (VPAC1R)-bispecific radiotracer and determined its tumor visualization potential via PET/CT imaging. For this purpose, the most potent described HBPL was synthesized together with its partly scrambled heterobivalent monospecific homologs and its monovalent counterparts. The agents were efficiently labeled with 68Ga3+ and evaluated in an initial PET/CT tumor imaging study in a human prostate carcinoma (PCa) xenograft rat tumor model established for this purpose. None of the three 68Ga-HBPLs enabled a clear tumor visualization and a considerably higher involvement in receptor-mediated uptake was found for the GRPR-binding part of the molecule than for the VPAC1R-binding one. Of the monovalent radiotracers, only [68Ga]Ga-NODA-GA-PESIN could efficiently delineate the tumor, confirming the results. Thus, this work sets the direction for future developments in the field of GRPR- and VPAC1R-bispecific radioligands, which should be based on other VPAC1R-specific peptides than PACAP-27. |
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| DOI: | doi:10.1016/j.bmcl.2021.128241 |
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| URL: | Bitte beachten Sie: Dies ist ein Bibliographieeintrag. Ein Volltextzugriff für Mitglieder der Universität besteht hier nur, falls für die entsprechende Zeitschrift/den entsprechenden Sammelband ein Abonnement besteht oder es sich um einen OpenAccess-Titel handelt.
Volltext: https://doi.org/10.1016/j.bmcl.2021.128241 |
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| | Volltext: https://www.sciencedirect.com/science/article/pii/S0960894X21004686 |
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| | DOI: https://doi.org/10.1016/j.bmcl.2021.128241 |
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| Datenträger: | Online-Ressource |
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| Sprache: | eng |
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| Sach-SW: | Bispecific tumor targeting |
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| | GRPR |
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| | Heterobivalent peptidic ligands |
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| | Human prostate carcinoma |
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| | PACAP-27 |
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| | PESIN |
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| | VCaP tumor xenograft |
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| | VPACR |
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| K10plus-PPN: | 1833248260 |
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| Verknüpfungen: | → Zeitschrift |
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Are heterobivalent GRPR- and VPAC1R-bispecific radiopeptides suitable for efficient in vivo tumor imaging of prostate carcinomas? / Lindner, Simon [VerfasserIn]; 15 September 2021 (Online-Ressource)
