Department of Radiology, Memorial Sloan Kettering Cancer Center, New York, New York.
QOPNA and LAQV-REQUIMTE, Department of Chemistry, University of Aveiro, Aveiro, Portugal.
J Nucl Med. 2020 Sep;61(9):1369-1375. doi: 10.2967/jnumed.119.236430. Epub 2020 Jan 31.
Galectins are carbohydrate-binding proteins overexpressed in bladder cancer (BCa) cells. Dendritic galactose moieties have a high affinity for galectin-expressing tumor cells. We radiolabeled a dendritic galactose carbohydrate with F (F-labeled galactodendritic unit ) and examined its potential in imaging urothelial malignancies. The F-labeled first-generation galactodendritic unit was obtained from its tosylate precursor. We conducted studies in a galectin-expressing UMUC3 orthotopic BCa model to determine the ability of F-labeled galactodendritic unit to image BCa. Intravesical administration of F-labeled galactodendritic unit allowed specific accumulation of the carbohydrate radiotracer in galectin-1-overexpressing UMUC3 orthotopic tumors when imaged with PET. The F-labeled galactodendritic unit was not found to accumulate in nontumor murine bladders. The F-labeled galactodendritic unit and similar analogs may be clinically relevant and exploitable for PET imaging of galectin-1-overexpressing bladder tumors.
半乳糖凝集素是膀胱癌（BCa）细胞中过表达的碳水化合物结合蛋白。树突状半乳糖部分与表达半乳糖凝集素的肿瘤细胞具有高亲和力。我们用 F（F 标记的半乳糖树突状单元）标记了树突状半乳糖碳水化合物，并研究了其在成像尿路上皮恶性肿瘤中的潜力。F 标记的第一代半乳糖树突状单元是从其甲苯磺酸酯前体获得的。我们在表达半乳糖凝集素的 UMUC3 原位 BCa 模型中进行了研究，以确定 F 标记的半乳糖树突状单元成像 BCa 的能力。当用 PET 成像时，膀胱内给予 F 标记的半乳糖树突状单元允许碳水化合物放射性示踪剂特异性地在过表达半乳糖凝集素-1 的 UMUC3 原位肿瘤中积累。未发现 F 标记的半乳糖树突状单元在非肿瘤小鼠膀胱中积累。F 标记的半乳糖树突状单元和类似的类似物可能具有临床相关性，并可用于过表达半乳糖凝集素-1 的膀胱癌的 PET 成像。
