Novel STING-targeted PET radiotracer for alert and therapeutic evaluation of acute lung injury.
10.1016/j.apsb.2022.12.017
- Author:
Duo XU
1
;
Fan YANG
2
;
Jiayao CHEN
1
;
Tianxing ZHU
2
;
Fen WANG
3
;
Yitai XIAO
2
;
Zibin LIANG
4
;
Lei BI
4
;
Guolong HUANG
4
;
Zebo JIANG
2
;
Hong SHAN
1
;
Dan LI
2
Author Information
1. Center for Interventional Medicine, the Fifth Affiliated Hospital, Sun Yat-sen University, Zhuhai 519000, China.
2. Department of Nuclear Medicine, the Fifth Affiliated Hospital, Sun Yat-sen University, Zhuhai 519000, China.
3. Department of Pathology, the First Affiliated Hospital, Sun Yat-sen University, Guangzhou 510080, China.
4. Guangdong Provincial Key Laboratory of Biomedical Imaging and Guangdong Provincial Engineering Research Center of Molecular Imaging, the Fifth Affiliated Hospital, Sun Yat-sen University, Zhuhai 519000, China.
- Publication Type:Journal Article
- Keywords:
Acute lung injury (ALI);
PET imaging;
Stimulator of interferon genes (STING);
[18F]FBTA
- From:
Acta Pharmaceutica Sinica B
2023;13(5):2124-2137
- CountryChina
- Language:English
-
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).