Preclinical Evaluation of ¹³¹I/¹⁸F-Labeled Covalent Small-Molecule Inhibitors for STING Status Imaging.

ABSTRACT: The stimulator of interferon genes (STING) is a vital protein to the immune surveillance of the tumor microenvironment. In this study, we develop novel inhibitor-based radioligands and evaluate their feasibility for noninvasive visualization of STING expression in tumor-bearing mice. Analogous compounds to STING inhibitors C170 and C176 were synthesized and labeled with ¹³¹I and ¹⁸F to attain [¹³¹I]I-NFIP and [¹⁸F]F-NFEP, respectively. The radiosynthesis was achieved with high radiochemical purity (>95%) and molar activity (28.56-48.89 GBq/μmol). The affinity and specificity of tracers were assessed through cell uptake and docking experiments, demonstrating that [¹³¹I]I-NFIP exhibited high specificity for STING, with a cell-based IC

SUBMITTER: Fang J 

PROVIDER: S-EPMC11184601 | biostudies-literature | 2024 Jun

REPOSITORIES: biostudies-literature