A Bioorthogonal TCO-Tetrazine-Based Pretargeted PET/NIRF Platform Enabling High-Contrast Tumor Imaging.

ABSTRACT: Objectives: Pretargeting strategies enhance the specificity and safety of radiopharmaceuticals by separating tumor targeting from radionuclide delivery. To address the rapid clearance and systemic exposure of directly labeled small-molecule agents, a DZ-1-based pretargeting system was developed, utilizing its broad-spectrum tumor-targeting characteristics. Methods: Three DZ-TCO precursors (DZ-1-TCO, DZ-Lys-TCO, and DZ-Lys-PEG₄-TCO) were synthesized and evaluated by near-infrared fluorescence imaging in HeLa and U87MG tumor-bearing mice. Two tetrazine probes (methyl-tetrazine and mono-substituted tetrazine) were labeled with ⁶⁸Ga to yield ⁶⁸Ga-DOTA-Me-Tz and ⁶⁸Ga-DOTA-H-Tz, whose stability was assessed in PBS and serum. Pretargeted P

SUBMITTER: Huang M 

PROVIDER: S-EPMC12735951 | biostudies-literature | 2025 Dec

REPOSITORIES: biostudies-literature