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Development of 18 F-Labeled Acridone Analogue for Tumor Imaging via Stimulator of Interferon Genes Targeting.
- Source :
-
Molecular pharmaceutics [Mol Pharm] 2023 Jul 03; Vol. 20 (7), pp. 3529-3538. Date of Electronic Publication: 2023 May 27. - Publication Year :
- 2023
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Abstract
- The stimulator of interferon genes (STING) is a pivotal protein in the production of STING-dependent type I interferon, which has the potential to enhance tumor rejection. The visualization of STING in the tumor microenvironment is valuable for STING-related treatments, but few STING imaging probes have been reported to date. In this study, we developed a novel <superscript>18</superscript> F-labeled agent ([ <superscript>18</superscript> F]F-CRI1) with an acridone core structure for the positron emission tomography (PET) imaging of STING in CT26 tumors. The probe was successfully prepared with a nanomolar STING binding affinity of K <subscript>d</subscript> = 40.62 nM. [ <superscript>18</superscript> F]F-CRI1 accumulated quickly in the tumor sites and its uptake reached a maximum of 3.02 ± 0.42% ID/g after 1 h i.v. injection. The specificity of [ <superscript>18</superscript> F]F-CRI1 was confirmed both in in vitro cell uptake and in vivo PET imaging by blocking studies. Our findings suggest that [ <superscript>18</superscript> F]F-CRI1 may be a potential agent for visualizing STING in the tumor microenvironment.
Details
- Language :
- English
- ISSN :
- 1543-8392
- Volume :
- 20
- Issue :
- 7
- Database :
- MEDLINE
- Journal :
- Molecular pharmaceutics
- Publication Type :
- Academic Journal
- Accession number :
- 37243620
- Full Text :
- https://doi.org/10.1021/acs.molpharmaceut.3c00137