Novel FGFR4-Targeting Peptide for Single-Photon Emission Computed Tomography Imaging in Hepatocellular Carcinoma
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 99 m Tc via HYNIC, yielding 99 m Tc-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 99 m Tc-HYNIC-FYQ-8 is a promising peptide-based radiotracer for clinical imaging of FGFR4-overexpressing tumors.
Fields of Study & Subjects
Fibroblast Growth Factor Research
Bladder and Urothelial Cancer Treatments
Hepatocellular Carcinoma Treatment and Prognosis
Publication details
- Journal / source
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Volume
- 69
- Issue
- 3
- Pages
- 2703–2711
- Publication date
- 23 January 2026
- Language
- EN