⁶⁸Ga-Labeled TRAP-Based Glycoside Trimers for Imaging of the Functional Liver Reserve.

ABSTRACT: The exclusive asialoglycoprotein receptor (ASGR) expression on hepatocytes makes it an attractive target for imaging of the functional liver reserve. Here, we present a set of TRAP-based glycoside trimers and evaluate their imaging properties compared to the gold standard [^99mTc]Tc-GSA. The click-chemistry-based synthesis approach provided easy access to trimeric low-molecular-weight compounds. Labeling with ⁶⁸Ga was carried out in high radiochemical yields (>99%). Complexes showed high stability and hydrophilicity. Protein binding ranged between 10 and 25%. Highest binding affinity (IC₅₀) and best liver accumulation were found for [⁶⁸Ga]Ga-T3N3, followed by [⁶⁸Ga]Ga-T3G3 and [⁶⁸Ga]Ga-T0G3. Rapid elimina

SUBMITTER: Zierke MA 

PROVIDER: S-EPMC11571218 | biostudies-literature | 2024 Nov

REPOSITORIES: biostudies-literature