Novel FGFR4-Targeting Peptide for Single-Photon Emission Computed Tomography Imaging in Hepatocellular Carcinoma
Qiurong Ju1, Xiaohui Wang1, Yutong Chen1
1State Key Laboratory of Natural Medicine, Department of Biomedical Engineering, School of Engineering, China Pharmaceutical University, No. 24 Tongjia Lane, Gulou District, Nanjing 211198, China.
Abstract:
Fibroblast growth factor receptor 4 (FGFR4) is overexpressed in various malignancies, making it a promising target for tumor diagnosis. In this study, we designed a series of FGFR4-targeted peptide-radionuclide conjugates (PRCs) based on a high-affinity peptide ligand derived from the binding epitope of the monoclonal antibody U3-1784. FYQ-8 showed the highest binding affinity for FGFR4-high-expressing HepG2 cells and was selected for radiolabeling with 99mTc via HYNIC, yielding 99mTc-HYNIC-FYQ-8. In xenograft models, this probe demonstrated high uptake (1.89 ± 0.35% ID/g) and produced high-contrast images specifically in high-FGFR4-expressing tumors. These results indicate that 99mTc-HYNIC-FYQ-8 is a promising peptide-based radiotracer for clinical imaging of FGFR4-overexpressing tumors.
Insights
A new radiotracer, 99mTc-HYNIC-FYQ-8, targets Fibroblast Growth Factor Receptor 4 (FGFR4). This peptide-based probe shows promise for imaging FGFR4-overexpressing tumors in preclinical models.
Area of Science:
- Oncology
- Radiochemistry
- Molecular Imaging
Background:
- Fibroblast Growth Factor Receptor 4 (FGFR4) overexpression is common in many cancers.
- FGFR4 presents a potential target for cancer diagnosis and therapy.
Purpose of the Study:
- To develop and evaluate a novel peptide-radionuclide conjugate (PRC) targeting FGFR4.
- To assess the diagnostic potential of the developed PRC for FGFR4-expressing tumors.
Main Methods:
- Design of FGFR4-targeted PRCs using a high-affinity peptide ligand (FYQ-8).
- Radiolabeling of FYQ-8 with technetium-99m (99mTc) using HYNIC conjugation.
- Evaluation of the radiotracer (99mTc-HYNIC-FYQ-8) in FGFR4-high-expressing cell lines and xenograft models.
Main Results:
- FYQ-8 exhibited high binding affinity to FGFR4-positive cells.
- The radiotracer 99mTc-HYNIC-FYQ-8 demonstrated specific uptake in high-FGFR4-expressing tumors in vivo.
- High-contrast imaging of tumors was achieved in xenograft models.
Conclusions:
- 99mTc-HYNIC-FYQ-8 is a specific and effective radiotracer for targeting FGFR4.
- This peptide-based radiotracer holds potential for clinical imaging of FGFR4-overexpressing malignancies.
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