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Novel STING-targeted PET radiotracer for alert and therapeutic evaluation of acute lung injury

Duo Xu, Fan Yang, Jiayao Chen, Tianxing Zhu, Fen Wang, Yitai Xiao, Zibin Liang, Lei Bi, Guolong Huang, Zebo Jiang, Hong Shan, Dan Li

2022Acta Pharmaceutica Sinica B20 citationsDOIOpen Access PDF

Abstract

Acute lung injury (ALI), as a common clinical emergency, is pulmonary edema and diffuse lung infiltration caused by inflammation. The lack of non-invasive alert strategy, resulting in failure to carry out preventive treatment, means high mortality and poor prognosis. Stimulator of interferon genes (STING) is a key molecular biomarker of innate immunity in response to inflammation, but there is still a lack of STING-targeted strategy. In this study, a novel STING-targeted PET tracer, [18F]FBTA, was labeled with high radiochemical yield (79.7 ± 4.3%) and molar activity (32.5 ± 2.9 GBq/μmol). We confirmed that [18F]FBTA has a strong STING binding affinity (Kd = 26.86 ± 6.79 nmol/L) and can be used for PET imaging in ALI mice to alert early lung inflammation and to assess the efficacy of drug therapy. Our STING-targeted strategy also reveals that [18F]FBTA can trace ALI before reaching the computed tomography (CT) diagnostic criteria, and demonstrates its better specificity and distribution than [18F]fluorodeoxyglucose ([18F]FDG).

Topics & Concepts

StingMedicineLungInflammationPositron emission tomographyNuclear medicineInternal medicineEngineeringAerospace engineeringinterferon and immune responsesImmune Response and InflammationRespiratory Support and Mechanisms
Novel STING-targeted PET radiotracer for alert and therapeutic evaluation of acute lung injury | Litcius