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Published on: January 7, 2019
PET imaging with [68Ga]-labeled TGFβ-targeting peptide in a mouse PANC-1 tumor model
Yong Li1, Hong Zhao2, Shan Hu1
1Department of Nuclear Medicine, Shenzhen Hospital of Southern Medical University, Shenzhen, China.
Purpose:
Transforming growth factor β (TGFβ) is upregulated in many types of tumors and plays important roles in tumor microenvironment construction, immune escape, invasion, and metastasis. The therapeutic effect of antibodies and nuclide-conjugated drugs targeting TGFβ has not been ideal. Targeting TGFβ with small-molecule or peptide carriers labeled with diagnostic/therapeutic nuclides is a new development direction. This study aimed to explore and confirm the imaging diagnostic efficiency of TGFβ-targeting peptide P144 coupled with [68Ga] in a PANC-1 tumor model.
Procedures:
TGFβ-targeting inhibitory peptide P144 with stable activity was prepared through peptide synthesis and screening, and P144 was coupled with biological chelator DOTA and labeled with radionuclide [68Ga] to achieve a stable TGFβ-targeting tracer [68Ga]Ga-P144. This tracer was first used for positron emission tomography (PET) molecular imaging study of pancreatic cancer in a mouse PANC-1 tumor model.
Results:
[68Ga]Ga-P144 had a high targeted uptake and relatively long uptake retention time in tumors and lower uptakes in non-target organs and backgrounds. Target pre-blocking experiment with the cold drug P144-DOTA demonstrated that the radioactive uptake with [68Ga]Ga-P144 PET in vivo, especially in tumor tissue, had a high TGFβ-targeting specificity. [68Ga]Ga-P144 PET had ideal imaging efficiency in PANC-1 tumor-bearing mice, with high specificity in vivo and good tumor-targeting effect.
Conclusion:
[68Ga]Ga-P144 has relatively high specificity and tumor-targeted uptake and may be developed as a promising diagnostic tool for TGFβ-positive malignancies.
Insights
This study developed a novel Gallium-68 labeled peptide ([68Ga]Ga-P144) for imaging transforming growth factor β (TGFβ) in pancreatic cancer. The tracer demonstrated high specificity and tumor uptake, showing promise for diagnosing TGFβ-positive cancers.
Area of Science:
- Oncology
- Radiochemistry
- Molecular Imaging
Background:
- Transforming growth factor β (TGFβ) is crucial in tumor progression, immune evasion, and metastasis.
- Current therapies targeting TGFβ have limitations, necessitating novel diagnostic and therapeutic strategies.
- Targeting TGFβ with radiolabeled peptides offers a new avenue for molecular imaging and therapy.
Purpose of the Study:
- To evaluate the imaging diagnostic efficiency of a novel TGFβ-targeting peptide P144 labeled with Gallium-68 ([68Ga]Ga-P144).
- To assess the specificity and tumor-targeting capabilities of [68Ga]Ga-P144 in a PANC-1 pancreatic cancer mouse model.
- To explore the potential of [68Ga]Ga-P144 as a diagnostic tool for TGFβ-positive malignancies.
Main Methods:
- Peptide synthesis and screening of TGFβ-targeting peptide P144.
- Coupling of P144 with DOTA and subsequent labeling with radionuclide [68Ga].
- Positron emission tomography (PET) molecular imaging in a PANC-1 mouse model, including target pre-blocking experiments.
Main Results:
- [68Ga]Ga-P144 exhibited high targeted uptake and prolonged retention in tumors.
- Lower uptakes were observed in non-target organs, indicating good specificity.
- Pre-blocking studies confirmed high TGFβ-targeting specificity of [68Ga]Ga-P144 in vivo.
- [68Ga]Ga-P144 PET imaging demonstrated ideal efficiency, specificity, and tumor-targeting in PANC-1 bearing mice.
Conclusions:
- [68Ga]Ga-P144 possesses high specificity and tumor-targeted uptake.
- This tracer shows potential as a promising diagnostic tool for TGFβ-positive cancers.
- Further development could lead to improved molecular imaging for TGFβ-driven malignancies.
