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Verfasst von:Eder, Ann-Christin [VerfasserIn]   i
 Liolios, Christos [VerfasserIn]   i
 Mier, Walter [VerfasserIn]   i
 Haberkorn, Uwe [VerfasserIn]   i
 Eisenhut, Michael [VerfasserIn]   i
 Kopka, Klaus [VerfasserIn]   i
 Eder, Matthias [VerfasserIn]   i
Titel:Improving the imaging contrast of 68Ga-PSMA-11 by targeted linker design
Titelzusatz:charged spacer moieties enhance the pharmacokinetic properties
Verf.angabe:Ann-Christin Baranski, Martin Schäfer, Ulrike Bauder-Wüst, Anja Wacker, Jana Schmidt, Christos Liolios, Walter Mier, Uwe Haberkorn, Michael Eisenhut, Klaus Kopka, and Matthias Eder
E-Jahr:2017
Jahr:August 8, 2017
Umfang:8 S.
Teil:volume:28
 year:2017
 number:9
 pages:2485-2492
 extent:8
Fussnoten:Gesehen am 19.09.2018
Titel Quelle:Enthalten in: Bioconjugate chemistry
Ort Quelle:Columbus, Ohio : American Chemical Society, 1990
Jahr Quelle:2017
Band/Heft Quelle:28(2017), 9, Seite 2485-2492
ISSN Quelle:1520-4812
Abstract:68Ga-Glu-urea-Lys-(Ahx)-HBED-CC (68Ga-PSMA-11) represents a successful radiopharmaceutical for PET/CT imaging of prostate cancer. Further optimization of the tumor-to-background contrast might significantly enhance the sensitivity of PET/CT imaging and the probability of detecting recurrent prostate cancer at low PSA values. This study describes the advantage of histidine (H)/glutamic acid (E) and tryptophan (W)/glutamic acid (E) containing linkers on the pharmacokinetic properties of 68Ga-PSMA-11. The tracers were obtained by a combination of standard Fmoc-based solid-phase synthesis and copper(I)-catalyzed azide-alkyne cycloaddition. Their 68Ga complexes were compared to the clinical reference 68Ga-PSMA-11 with respect to cell binding, effective internalization, and tumor targeting properties in LNCaP-bearing balb/c nu/nu mice. The introduction of (HE)i (i = 1-3) or (WE)i (i = 1-3) into PSMA-11 resulted in a significantly changed biodistribution profile. The uptake values in kidneys, spleen, liver, and other background organs were reduced for (HE)3 while the tumor uptake was not affected. For (HE)1 the tumor uptake was significantly increased. The introduction of tryptophan-containing linkers also modulated the organ distribution profile. The results clearly indicate that histidine is of essential impact in order to improve the tumor-to-organ contrast. Hence, the histidine/glutamic acid linker modifications considerably improved the pharmacokinetic properties of 68Ga-PSMA-11 leading to a reduced uptake in dose limiting organs and a significantly enhanced tumor-to-background contrast. Glu-urea-Lys-(HE)3-HBED-CC represents a promising 68Ga complex ligand for PET/CT-imaging of prostate cancer.
DOI:doi:10.1021/acs.bioconjchem.7b00458
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 ; Verlag: http://dx.doi.org/10.1021/acs.bioconjchem.7b00458
 Volltext: https://doi.org/10.1021/acs.bioconjchem.7b00458
 DOI: https://doi.org/10.1021/acs.bioconjchem.7b00458
Datenträger:Online-Ressource
Sprache:eng
K10plus-PPN:1581098553
Verknüpfungen:→ Zeitschrift

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