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Microwave-assisted One-pot Synthesis of N-succinimidyl-4-[18F]fluorobenzoate [18F]SFB
Published on: June 28, 2011
Synthesis and Evaluation of Novel 99mTc-Labeled FGFR2-Targeting Peptides
Jingjing Yao1, Mingxuan Fan1, Jiaying Peng1
1Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, P. R. China.
Abstract:
To develop radiolabeled FGFR2-targeting probes for visualizing fibroblast growth factor receptor (FGFR) expression levels in the tumor microenvironment, four novel 99mTc-labeled FGFR2-targeting peptides ([99mTc]Tc-FGFR2-1, [99mTc]Tc-FGFR2-2, [99mTc]Tc-FGFR2-3, and [99mTc]Tc-FGFR2-4) with different amino acid linkers between the targeted peptide moiety and the 99mTc chelating group were designed and synthesized. The in vitro cellular inhibition, internalization, and efflux results demonstrated that the four 99mTc complexes exhibited FGFR2-specific binding and prolonged cellular retention in DU145 human prostate cancer cells, which indicated that modification from the glycine side (N-terminal) of CH02 was feasible. Among them, [99mTc]Tc-FGFR2-1 exhibited the highest in vitro cellular uptake and in vivo tumor uptake at 30 min postinjection, and tumor uptake could be significantly inhibited by the competitor CH02 (53% inhibited, p < 0.05), suggesting the tumor-specific targeting ability of [99mTc]Tc-FGFR2-1. The DU145-xenografted tumor lesions were clearly visualized by single photon emission computed tomography (SPECT)/CT at 30 min postinjection of [99mTc]Tc-FGFR2-1, highlighting its potential as a SPECT imaging probe for tumor FGFR2 detection.
Insights
Researchers developed novel technetium-99m (99mTc)-labeled peptides targeting fibroblast growth factor receptor 2 (FGFR2) for cancer imaging. The probe [99mTc]Tc-FGFR2-1 demonstrated high tumor uptake and specific visualization of FGFR2-expressing tumors in preclinical models.
Area of Science:
- Nuclear Medicine
- Radiochemistry
- Oncology
Background:
- Fibroblast growth factor receptor 2 (FGFR2) is implicated in tumor progression and is a target for cancer therapy.
- Developing targeted radiotracers is crucial for non-invasively assessing FGFR2 expression in the tumor microenvironment.
Purpose of the Study:
- To design and synthesize novel 99mTc-labeled peptides targeting FGFR2.
- To evaluate the *in vitro* and *in vivo* performance of these probes for SPECT imaging.
Main Methods:
- Synthesis of four 99mTc-labeled peptides with varying linkers.
- *In vitro* studies: cellular uptake, inhibition, and efflux assays in DU145 cells.
- *In vivo* studies: SPECT/CT imaging in DU145 xenograft models, including blocking studies.
Main Results:
- All four 99mTc complexes showed FGFR2-specific binding and good cellular retention.
- [99mTc]Tc-FGFR2-1 exhibited the highest *in vitro* uptake and *in vivo* tumor accumulation.
- Significant inhibition of tumor uptake by CH02 confirmed the specificity of [99mTc]Tc-FGFR2-1.
- Clear visualization of DU145 xenograft tumors was achieved using SPECT/CT with [99mTc]Tc-FGFR2-1.
Conclusions:
- Modification of the CH02 peptide linker is feasible for developing 99mTc-labeled FGFR2 probes.
- [99mTc]Tc-FGFR2-1 is a promising SPECT imaging agent for detecting FGFR2 expression in tumors.
- This probe has potential for guiding FGFR-targeted therapies.
