PET imaging with [68Ga]-labeled TGFβ-targeting peptide in a mouse PANC-1 tumor model

Purpose Transforming growth factor β (TGFβ) is upregulated in many types of tumors and plays important roles tumor microenvironment construction, immune escape, invasion, metastasis. The therapeutic effect antibodies nuclide-conjugated drugs targeting TGFβ has not been ideal. Targeting with small-molecule or peptide carriers labeled diagnostic/therapeutic nuclides a new development direction. This study aimed to explore confirm the imaging diagnostic efficiency TGFβ-targeting P144 coupled [ 68 Ga] PANC-1 model. Procedures inhibitory stable activity was prepared through synthesis screening, biological chelator DOTA radionuclide achieve tracer Ga]Ga-P144. first used for positron emission tomography (PET) molecular pancreatic cancer mouse Results Ga]Ga-P144 had high targeted uptake relatively long retention time lower uptakes non-target organs backgrounds. Target pre-blocking experiment cold drug P144-DOTA demonstrated that radioactive PET vivo , especially tissue, specificity. ideal tumor-bearing mice, specificity good tumor-targeting effect. Conclusion tumor-targeted may be developed as promising tool TGFβ-positive malignancies.