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Published on: February 3, 2015
The Synthesis and Initial Evaluation of MerTK Targeted PET Agents
Li Wang1, Yubai Zhou2, Xuedan Wu1
1Biomedical Research Imaging Center, Department of Radiology, and UNC Lineberger Comprehensive Cancer Center, The University of North Carolina at Chapel Hill, Chapel Hill, NC 27514, USA.
Abstract:
MerTK (Mer tyrosine kinase), a receptor tyrosine kinase, is ectopically or aberrantly expressed in numerous human hematologic and solid malignancies. Although a variety of MerTK targeting therapies are being developed to enhance outcomes for patients with various cancers, the sensitivity of tumors to MerTK suppression may not be uniform due to the heterogeneity of solid tumors and different tumor stages. In this report, we develop a series of radiolabeled agents as potential MerTK PET (positron emission tomography) agents. In our initial in vivo evaluation, [18F]-MerTK-6 showed prominent uptake rate (4.79 ± 0.24%ID/g) in B16F10 tumor-bearing mice. The tumor to muscle ratio reached 1.86 and 3.09 at 0.5 and 2 h post-injection, respectively. In summary, [18F]-MerTK-6 is a promising PET agent for MerTK imaging and is worth further evaluation in future studies.
Insights
Researchers developed a novel positron emission tomography (PET) agent, [¹⁸F]-MerTK-6, for imaging MerTK (Mer tyrosine kinase). This agent shows promising tumor uptake in preclinical models, suggesting its potential for cancer diagnostics.
Area of Science:
- Oncology
- Radiochemistry
- Molecular Imaging
Background:
- MerTK (Mer tyrosine kinase) is aberrantly expressed in various human cancers, making it a therapeutic target.
- Tumor sensitivity to MerTK suppression varies due to tumor heterogeneity and stage.
- Developing targeted therapies requires accurate methods to assess MerTK expression.
Purpose of the Study:
- To develop novel radiolabeled agents for MerTK-targeted positron emission tomography (PET) imaging.
- To evaluate the in vivo performance of these agents for potential cancer imaging applications.
Main Methods:
- Synthesis and radiolabeling of potential MerTK PET agents.
- In vivo evaluation of radiolabeled agents in B16F10 tumor-bearing mice.
- Assessment of tumor uptake and tumor-to-muscle ratios at various time points post-injection.
Main Results:
- [¹⁸F]-MerTK-6 demonstrated significant uptake in B16F10 tumors (4.79 ± 0.24%ID/g).
- Tumor-to-muscle ratios of 1.86 and 3.09 were achieved at 0.5 and 2 hours post-injection, respectively.
- These results indicate favorable biodistribution and tumor targeting.
Conclusions:
- [¹⁸F]-MerTK-6 is a promising PET imaging agent for MerTK.
- The agent warrants further investigation for its utility in imaging MerTK-positive cancers.
- This tool could aid in patient stratification for MerTK-targeted therapies.
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