Exploiting the Concept of Multivalency with ⁶⁸Ga- and ⁸⁹Zr-Labelled Fusarinine C-Minigastrin Bioconjugates for Targeting CCK2R Expression.

ABSTRACT: Cholecystokinin-2 receptors (CCK2R) are overexpressed in a variety of malignant diseases and therefore have gained certain attention for peptide receptor radionuclide imaging. Among extensive approaches to improve pharmacokinetics and metabolic stability of minigastrin (MG) based radioligands, the concept of multivalency for enhanced tumour targeting has not been investigated extensively. We therefore utilized fusarinine C (FSC) as chelating scaffold for novel mono-, di-, and trimeric bioconjugates for targeting CCK2R expression. FSC-based imaging probes were radiolabelled with positron emitting radionuclides (gallium-68 and zirconium-89) and characterized in vitro (log⁡D, IC₅₀, and cell uptake) and in vivo (metabolic stability in BALB/c mice, biodistributio

SUBMITTER: Summer D 

PROVIDER: S-EPMC5914118 | biostudies-literature | 2018

REPOSITORIES: biostudies-literature