Molecular Pharmaceutics· 2026Q1
Design, Synthesis, and Evaluation of 99mTc-Labeled Proline Isonitrile Derivatives with Optimized Linker Lengths for Tumor SPECT Imaging
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- 2026year
Short summary
[99mTc]Tc-CN7Pro, a novel technetium-99m-labeled proline derivative, demonstrates high tumor uptake (1.05 ± 0.09% ID/g in S180 mice, 2.47 ± 0.39% ID/g in U87MG models) and a tumor/muscle ratio of 5.03, making it a promising SPECT imaging agent.
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Key points
- Four l-proline isonitrile ligands (CN5Pro, CN6Pro, CN7Pro, CN8Pro) were synthesized and labeled with 99mTc, achieving >95% labeling yield and good stability.
- [99mTc]Tc-CN7Pro showed the highest tumor uptake (1.05 ± 0.09% ID/g in S180 mice, 2.47 ± 0.39% ID/g in U87MG models) and a tumor/muscle ratio of 5.03.
- SPECT/CT imaging clearly visualized tumors, with uptake inhibited by excess l-proline, suggesting proline transport as the mechanism.
- Cellular studies indicated uptake primarily via system A transporters, and the complex remained intact in vivo.
AI-generated from the title and abstract; the full text is not read.
Abstract
Abstract Amino acid metabolic imaging is among the important research directions in tumor molecular imaging. The highly active metabolism of proline in tumors, together with the abnormal expression of its key enzymes, makes it a promising target for tumor molecular imaging. To develop new proline transport-targeted tumor imaging agents, four l-proline isonitrile ligands (CN5Pro, CN6Pro, CN7Pro and CN8Pro) were synthesized and labeled with technetium-99m. All the complexes achieved >95% labeling yield with good stability. Biodistribution in S180 tumor-bearing mice revealed that [99mTc]Tc-CN7Pro exhibited the highest tumor uptake (1.05 ± 0.09% ID/g), a tumor/muscle ratio of 5.03, and predominant renal excretion. With respect to U87MG models, tumor uptake reached 2.47 ± 0.39% ID/g, confirming tumor imaging applicability. SPECT/CT imaging clearly revealed tumors, with uptake inhibited by excess l-proline. Cellular studies indicated uptake primarily via system A transporters, and the complex remained intact in vivo. Collectively, [99mTc]Tc-CN7Pro is convenient for labeling, achieves excellent targeting, and is very stable, making it a promising SPECT tumor imaging agent.
The authors' abstract, as published at the source. Molecular Pharmaceutics, 2026 · DOI ↗
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Field: Biochemistry (Biochemistry, Genetics and Molecular Biology)
BiochemistryBiochemistry, Genetics and Molecular Biology