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Development and Evaluation of 68Ga-Labeled TMTP1-Based Cyclic Peptide Probes for Targeting Hepatocellular Carcinoma
Yesen Li1, Yanjie Wang2, Yaoxuan Wang2
1Department of Nuclear Medicine, The First Affiliated Hospital of Xiamen University, School of Medicine, Xiamen University, Xiamen 361003, China.
Abstract:
This study focused on the development and evaluation of four [68Ga]-labeled cyclic TMTP1 peptide-based probes for targeting highly metastatic hepatocellular carcinoma (HCC). The probes─[68Ga]Ga-N-G-NVvRQ, [68Ga]Ga-c[K(N)NVvRQ], [68Ga]Ga-c[K(N)NVVRQ], and [68Ga]Ga-c[K(N)NVvRQ]2─were designed using a head-to-tail cyclization strategy to enhance their stability, improve tumor targeting, and reduce uptake in nontarget organs. The microPET imaging results showed that although tumor uptake for all four probes was similar at each time point, renal evaluation revealed that [68Ga]Ga-c[K(N)NVvRQ] had the lowest value at 15 min (1.90 ± 0.87%ID/g), significantly outperforming linear analog [68Ga]Ga-N-G-NVvRQ (2.87 ± 0.86%ID/g) and dimeric peptide, [68Ga]Ga-c[K(N)NVvRQ]2 (3.92 ± 0.68%ID/g), and the probe exhibited the lowest physiological uptake across major organs. At 30 min, the liver uptake of [68Ga]Ga-c[K(N)NVvRQ] was 0.29 ± 0.08%ID/g, with a tumor-to-liver (T/L) ratio of 2.45 ± 0.03. This low nonspecific uptake in normal organs contributed to high-contrast PET imaging, facilitating the diagnosis of small tumor lesions. In addition, the probe demonstrated sustained low renal radioactivity retention, which may offer potential benefits for minimizing additional radioactive damage to the kidneys. Overall, [68Ga]Ga-c[K(N)NVvRQ] achieved a good balance between strong tumor uptake and low nonspecific uptake in organs (especially in kidneys), making it an ideal candidate for further investigation in HCC imaging applications.
Insights
Researchers developed novel [68Ga]-labeled cyclic peptide probes for hepatocellular carcinoma (HCC) imaging. The probe [68Ga]Ga-c[K(N)NVvRQ] demonstrated optimal tumor targeting with reduced uptake in normal organs, showing promise for early HCC detection.
Area of Science:
- Nuclear Medicine
- Radiopharmaceutical Chemistry
- Oncology
Background:
- Hepatocellular carcinoma (HCC) is a highly metastatic cancer requiring effective diagnostic tools.
- Peptide-based radiotracers offer targeted imaging capabilities for various cancers.
- Cyclic peptides can enhance stability and improve pharmacokinetic profiles compared to linear analogs.
Purpose of the Study:
- To develop and evaluate novel [68Ga]-labeled cyclic TMTP1 peptide-based probes for targeting metastatic HCC.
- To assess the stability, tumor targeting, and biodistribution of these probes using microPET imaging.
- To identify a lead candidate probe with optimal characteristics for HCC diagnosis.
Main Methods:
- Synthesis and radiolabeling of four [68Ga]-labeled cyclic TMTP1 peptide analogs using a head-to-tail cyclization strategy.
- Evaluation of probe stability, tumor uptake, and biodistribution in vivo using microPET imaging.
- Comparison of the performance of cyclic probes against a linear analog and a dimeric peptide.
Main Results:
- All four probes showed similar tumor uptake, but [68Ga]Ga-c[K(N)NVvRQ] exhibited significantly lower renal uptake (1.90 ± 0.87%ID/g at 15 min) compared to linear and dimeric analogs.
- [68Ga]Ga-c[K(N)NVvRQ] demonstrated the lowest physiological uptake across major organs, including low liver uptake (0.29 ± 0.08%ID/g at 30 min) with a favorable tumor-to-liver ratio (2.45 ± 0.03).
- The probe displayed sustained low renal radioactivity retention and facilitated high-contrast PET imaging, enabling the detection of small tumor lesions.
Conclusions:
- The cyclic peptide probe [68Ga]Ga-c[K(N)NVvRQ] offers a favorable balance of strong tumor uptake and low non-specific uptake in critical organs, particularly the kidneys.
- This probe is a promising candidate for further investigation in positron emission tomography (PET) imaging applications for hepatocellular carcinoma.
- The optimized probe design may contribute to minimizing radiation dose to the kidneys, enhancing patient safety in diagnostic imaging.
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