title: Synthesis of a (68)ga-labeled peptoid-Peptide hybrid for imaging of neurotensin receptor expression in vivo.
abstract: The neurotensin receptor subtype 1 (NTS1) represents an attractive molecular target for imaging various tumors. Positron emission tomography (PET) gained widespread importance due to its sensitivity. We combined the design of a metabolically stable neurotensin analogue with a (68)Ga-radiolabeling approach. The (68)Ga-labeled peptoid-peptide hybrid [(68)Ga]3 revealed high stability, specific tumor uptake (0.7%ID/g, 65 min p.i.), and advantageous biokinetics in vivo using HT29 tumor-bearing nude mice. Because of the ability to internalize into NTS1-expressing tumor cells, [(68)Ga]3 proved to be highly suitable for a reliable and practical visualization of NTS1-expressing tumors in vivo by small animal PET.
authors.affiliation: Laboratory of Molecular Imaging, Clinic of Nuclear Medicine, Friedrich-Alexander University, Schwabachanlage 6, D-91054 Erlangen, Germany.
authors.forename: Simone
authors.initials: S
authors.lastname: Maschauer
authors.affiliation: Department of Chemisty and Pharmacy, Emil Fischer Center.
authors.forename: Jürgen
authors.initials: J
authors.lastname: Einsiedel
authors.affiliation: Laboratory of Molecular Imaging, Clinic of Nuclear Medicine, Friedrich-Alexander University, Schwabachanlage 6, D-91054 Erlangen, Germany.
authors.forename: Carsten
authors.initials: C
authors.lastname: Hocke
authors.affiliation: Department of Chemisty and Pharmacy, Emil Fischer Center.
authors.forename: Harald
authors.initials: H
authors.lastname: Hübner
authors.affiliation: Laboratory of Molecular Imaging, Clinic of Nuclear Medicine, Friedrich-Alexander University, Schwabachanlage 6, D-91054 Erlangen, Germany.
authors.forename: Torsten
authors.initials: T
authors.lastname: Kuwert
authors.affiliation: Department of Chemisty and Pharmacy, Emil Fischer Center.
authors.forename: Peter
authors.initials: P
authors.lastname: Gmeiner
authors.affiliation: Laboratory of Molecular Imaging, Clinic of Nuclear Medicine, Friedrich-Alexander University, Schwabachanlage 6, D-91054 Erlangen, Germany.
authors.forename: Olaf
authors.initials: O
authors.lastname: Prante
keywords: Neurotensin; gallium-68; neurotensin receptor; peptide; positron emission tomography (PET)