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A Novel Peptide-Based PD-L1 PET Tracer: Design, Synthesis, and Preclinical Imaging Validation.

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ACS medicinal chemistry letters 📖 저널 OA 100% 2024: 2/2 OA 2025: 12/12 OA 2026: 16/16 OA 2024~2026 2026 Vol.17(1) p. 117-124 OA
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Zhang M, Dong Y, Mo C, Chen Z, Han Y, Wang M

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PD-L1 (programmed death ligand 1), the primary ligand of PD-1 (programmed death 1), is widely expressed across various tumor types.

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APA Zhang M, Dong Y, et al. (2026). A Novel Peptide-Based PD-L1 PET Tracer: Design, Synthesis, and Preclinical Imaging Validation.. ACS medicinal chemistry letters, 17(1), 117-124. https://doi.org/10.1021/acsmedchemlett.5c00448
MLA Zhang M, et al.. "A Novel Peptide-Based PD-L1 PET Tracer: Design, Synthesis, and Preclinical Imaging Validation.." ACS medicinal chemistry letters, vol. 17, no. 1, 2026, pp. 117-124.
PMID 41531950 ↗

Abstract

PD-L1 (programmed death ligand 1), the primary ligand of PD-1 (programmed death 1), is widely expressed across various tumor types. In this study, we developed a novel PET probe, [F]-AlF-Asp-TPP-1, for noninvasive imaging of PD-L1 expression. The probe was synthesized with a radiochemical yield of 13.7%, high radiochemical purity (>95%), and a molar activity exceeding 2.4 GBq/μmol. Stability assays confirmed excellent stability both and . Dynamic PET imaging over 90 min revealed rapid tracer accumulation in tumors and other organs within 15 min postinjection. Tumor uptake was 2.48 ± 0.05% ID/g, 1.81 ± 0.20% ID/g, and 0.96 ± 0.09% ID/g at 30, 60, and 90 min, respectively. Collectively, these results suggest that [F]-AlF-Asp-TPP-1 is a promising PET imaging agent for monitoring PD-L1 expression in tumors and may serve as a valuable tool for guiding PD-L1-targeted immunotherapy.

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