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Article Abstract
Immunotherapy has brought great benefits to cancer patients, but only some patients benefit from it. Noninvasive, real-time and dynamic monitoring of the effectiveness of immunotherapy through PET imaging may provide assistance for the treatment plan of immunotherapy. In this study, we designed and synthesized a new targeted PD-L1 peptide NOTA-PEG-Asp-PDL1P, which was labeled with nuclide F to obtain a new imaging agent [F]AlF-NOTA-PEG-Asp-PDL1P. The total radiochemical yield of [F]AlF-NOTA-PEG-Asp-PDL1P was 13.7 % (Uncorrected radiochemical yield, n > 5). [F]AlF-NOTA-PEG-Asp-PDL1P achieved high radiochemical purity (>95 %) with a molar activity more than 51.2 GBq/μmol. [F]AlF-NOTA-PEG-Asp-PDL1P exhibited good hydrophilicity and had good stability both in vivo and in vitro, it can specifically targets B16F10 tumor with PD-L1 expression, and had a relatively high retention in tumor, a relatively fast clearance in vivo and a higher tumor-to-non-target ratio, all of which could make [F]AlF-NOTA-PEG-Asp-PDL1P a potential tracer for PD-L1 prediction before clinical immunotherapy.
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| http://dx.doi.org/10.1016/j.bioorg.2024.107193 | DOI Listing |
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