PET/CT Imaging with an <sup>18</sup>F-Labeled Galactodendritic Unit in a Galectin-1-Overexpressing Orthotopic Bladder Cancer Model.

Pereira, Patricia M R; Roberts, Sheryl; Figueira, Flávio; Tomé, João P C; Reiner, Thomas; Lewis, Jason S · J Nucl Med · 2020

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Abstract

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 <sup>18</sup>F (<sup>18</sup>F-labeled galactodendritic unit <b>4</b>) and examined its potential in imaging urothelial malignancies. <b>Methods:</b> The <sup>18</sup>F-labeled first-generation galactodendritic unit <b>4</b> was obtained from its tosylate precursor. We conducted <i>in vivo</i> studies in a galectin-expressing UMUC3 orthotopic BCa model to determine the ability of <sup>18</sup>F-labeled galactodendritic unit <b>4</b> to image BCa. <b>Results:</b> Intravesical administration of <sup>18</sup>F-labeled galactodendritic unit <b>4</b> allowed specific accumulation of the carbohydrate radiotracer in galectin-1-overexpressing UMUC3 orthotopic tumors when imaged with PET. The <sup>18</sup>F-labeled galactodendritic unit <b>4</b> was not found to accumulate in nontumor murine bladders. <b>Conclusion:</b> The <sup>18</sup>F-labeled galactodendritic unit <b>4</b> and similar analogs may be clinically relevant and exploitable for PET imaging of galectin-1-overexpressing bladder tumors.

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