18F- and 68Ga-Labeled Neurotensin Peptides for PET Imaging of Neurotensin Receptor 1

Beitrag in einer Fachzeitschrift
(Originalarbeit)


Details zur Publikation

Autor(en): Maschauer S, Einsiedel J, Hübner H, Gmeiner P, Prante O
Zeitschrift: Journal of Medicinal Chemistry
Verlag: American Chemical Society
Jahr der Veröffentlichung: 2016
Band: 59
Seitenbereich: 6480-6492
ISSN: 0022-2623
Sprache: Englisch


Abstract


The neurotensin (NT) receptor-1 (NTS1) is overexpressed in a variety of carcinomas and is therefore an interesting target for imaging with positron emission tomography (PET). The aim of this study was the development of new NT derivatives based on the metabolically stable peptide sequence NLys-Lys-Pro-Tyr-Tle-Leu suitable for PET imaging. The NT peptides were synthesized by solid-phase supported peptide synthesis and elongated with respective chelators (NODA-GA, DOTA) for Ga-68-labeling or propargylglycine for F-18-labeling via copper-catalyzed azide-alkyne cycloaddition. Receptor affinities of the peptides for NTS1 were in the range of 19-110 nM. Biodistribution studies using HT29 tumor-bearing mice showed highest tumor uptake for [Ga-68]6 and [Ga-68]8 and specific binding in small-animal PET studies. The tumor uptake of Ga-68-labeled peptides in vivo significantly correlated with the in-vitro Ki values for NTS1. [Ga-68]8 displayed an excellent tumor-to-background ratio and could therefore be considered as an appropriate molecular probe for NTS1 imaging by PET.



FAU-Autoren / FAU-Herausgeber

Einsiedel, Jürgen Dr.
Hübner, Harald Dr.
Lehrstuhl für Pharmazeutische Chemie
Lehrstuhl für Pharmazeutische Chemie
Gmeiner, Peter Prof. Dr.
Lehrstuhl für Pharmazeutische Chemie
Maschauer, Simone PD Dr.
Professur für Molekulare Bildgebung und Radiochemie
Prante, Olaf Prof. Dr.
Professur für Molekulare Bildgebung und Radiochemie


Zusätzliche Organisationseinheit(en)
Emil-Fischer-Zentrum (Emil Fischer Center)


Zitierweisen

APA:
Maschauer, S., Einsiedel, J., Hübner, H., Gmeiner, P., & Prante, O. (2016). 18F- and 68Ga-Labeled Neurotensin Peptides for PET Imaging of Neurotensin Receptor 1. Journal of Medicinal Chemistry, 59, 6480-6492. https://dx.doi.org/10.1021/acs.jmedchem.6b00675

MLA:
Maschauer, Simone, et al. "18F- and 68Ga-Labeled Neurotensin Peptides for PET Imaging of Neurotensin Receptor 1." Journal of Medicinal Chemistry 59 (2016): 6480-6492.

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Zuletzt aktualisiert 2018-11-08 um 02:11