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| Verfasst von: | Liolios, Christos [VerfasserIn]  |
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| | Buchmuller, Benjamin C. [VerfasserIn] |
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| | Bauder-Wüst, Ulrike [VerfasserIn] |
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| | Schäfer, Martin [VerfasserIn] |
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| | Leotta, Karin [VerfasserIn] |
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| | Haberkorn, Uwe [VerfasserIn] |
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| | Eder, Matthias [VerfasserIn] |
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| | Kopka, Klaus [VerfasserIn] |
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| Titel: | Monomeric and dimeric 68Ga-labeled bombesin Analogues for Positron Emission Tomography (PET) imaging of tumors expressing Gastrin-Releasing Peptide Receptors (GRPrs) |
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| Verf.angabe: | Christos Liolios, Benjamin Buchmuller, Ulrike Bauder-Wüst, Martin Schäfer, Karin Leotta, Uwe Haberkorn, Matthias Eder, and Klaus Kopka |
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| E-Jahr: | 2018 |
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| Jahr: | February 12, 2018 |
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| Umfang: | 13 S. |
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| Teil: | volume:61 |
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| | year:2018 |
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| | number:5 |
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| | pages:2062-2074 |
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| | extent:13 |
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| Fussnoten: | Im Titel ist "68" in 68Ga-labeled hochgestellt ; Gesehen am 25.02.2020 |
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| Titel Quelle: | Enthalten in: Journal of medicinal chemistry |
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| Ort Quelle: | Washington, DC : ACS, 1959 |
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| Jahr Quelle: | 2018 |
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| Band/Heft Quelle: | 61(2018), 5, Seite 2062-2074 |
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| ISSN Quelle: | 1520-4804 |
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| Abstract: | The GRPr, highly expressed in prostate PCa and breast cancer BCa, is a promising target for the development of new PET radiotracers. The chelator HBED-CC (N,N′-bis[2-hydroxy-5-(carboxyethyl)benzyl]ethylenediamine-N,N′-diacetic acid) was coupled to the bombesin peptides: HBED-C-BN(2-14) 1, HBED-CC-PEG2-[d-Tyr6,β-Ala11,Thi13,Nle14]-BN(6-14) 2, HBED-CC-Y-[d-Phe6,Sta13,Leu14]-BN(6-14) (Y = 4-amino-1-carboxymethylpiperidine) 3, and HBED-CC-{PEG2-Y-[d-Phe6,Sta13,Leu14]-BN(6-14)}2 4 (homodimer). Compounds 1-4 presented high binding affinities for GRPr (T47D, 0.56-3.51 nM; PC-3, 2.12-4.68 nM). In PC-3 and T47D cells, agonists [68Ga]1 and [68Ga]2 were mainly internalized while antagonists [68Ga]3 and [68Ga]4 were surface bound. Cell-related radioactivity reached a maximum after 45 min, while tracer levels followed GRPr expression (PC-3 > T47D > LNCaP > MDA-MB-231). [68Ga]4 showed the highest cell-bound radioactivity (PC-3 and T47D). In vivo, tumor (PC-3) targeting for [68Ga]3 and [68Ga]4 increased over time, with dynamic μPET showing clearer tumors images at later time points. [68Ga]3 and [68Ga]4 can be considered suitable PET tracers for imaging PCa and BCa expressing GRPr. |
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| DOI: | doi:10.1021/acs.jmedchem.7b01856 |
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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/10.1021/acs.jmedchem.7b01856 |
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| | Verlag: https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01856 |
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| | DOI: https://doi.org/10.1021/acs.jmedchem.7b01856 |
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| Datenträger: | Online-Ressource |
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| Sprache: | eng |
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| K10plus-PPN: | 1690920491 |
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| Verknüpfungen: | → Zeitschrift |
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Monomeric and dimeric 68Ga-labeled bombesin Analogues for Positron Emission Tomography (PET) imaging of tumors expressing Gastrin-Releasing Peptide Receptors (GRPrs) / Liolios, Christos [VerfasserIn]; February 12, 2018 (Online-Ressource)
