Promising potential of a 18F-labelled small-molecular radiotracer to evaluate PD-L1 expression in tumors by PET imaging.
Bioorg Chem
; 115: 105294, 2021 10.
Article
em En
| MEDLINE
| ID: mdl-34426150
ABSTRACT
Programmed death ligand 1 (PD-L1) expression level is a reproducible biomarker for guiding stratification of patients to immunotherapy. However, the most widely used immunohistochemistry method is incompetent to fully understand the PD-L1 expression level in the whole body because of the highly complex PD-L1 expression in the tumor microenvironment. In this work, a novel small-molecular radiotracer [18F]LG-1 based on the biphenyl active structure was developed to evaluate PD-L1 expression in tumors. [18F]LG-1 was obtained by conjugating and radiolabeling with [18F]FDG with high radiochemical purity (>98.0%) and high molar activity (37.2 ± 2.9 MBq/nmol). In vitro experimental results showed that [18F]LG-1 could target PD-L1 in tumor cells and the cellular uptake in A375-hPD-L1 cells (PD-L1 + ) was clearly higher than that in A375 cells (PD-L1-). In vivo dynamic PET images of [18F]LG-1 provided clear visualization of A375-hPD-L1 tumor with high tumor-to-background contrast, and the tumor uptake was determined to be 3.98 ± 0.21 %ID/g at 60 min, which was 2.6-fold higher than that of A375 tumor. These results suggested that [18F]LG-1 had great potential as a promising PD-L1 radiotracer.
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Base de dados:
MEDLINE
Assunto principal:
Compostos Radiofarmacêuticos
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Tomografia por Emissão de Pósitrons
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Bibliotecas de Moléculas Pequenas
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Antígeno B7-H1
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Melanoma
Limite:
Animals
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Female
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Humans
Idioma:
En
Ano de publicação:
2021
Tipo de documento:
Article