A novel AlF-labelled NOTA-modified ubiquicidin 29-41 derivative as a bacterial infection PET imaging agent.
Eur J Med Chem
Key Laboratory of Radiopharmaceuticals of Ministry of Education, NMPA Key Laboratory for Research and Evaluation of Radiopharmaceuticals (National Medical Product Administration), College of Chemistry, Beijing Normal University, Beijing, 100875, China. Electronic address:
Published: March 2025
The antimicrobial peptide ubiquicidin 29-41 (TGRAKRRMQYNRR) is a potential target for detecting bacterial infection. A novel UBI 29-41 derivative modified with 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA) on the amino side of lysine was synthesized and radiolabelled with AlF, named [F]AlF-NOTA-UBI 29-41. The novel PET tracer maintained good in vitro stability in saline at room temperature and mouse serum at 37 °C. In vitro bacterial binding experiments indicated that the tracer specifically bound to Staphylococcus aureus. A significant difference in the uptake of [F]AlF-NOTA-UBI 29-41 between infected muscle and inflamed muscle was observed in biodistribution. A PET imaging study in mouse models with bacterial infection and sterile inflammation showed apparent accumulation at the infection site, suggesting that the complex is a potential PET tracer for distinguishing bacterial infection from sterile inflammation.
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