Print Email Facebook Twitter Tumor Targeting via Sialic Acid Title Tumor Targeting via Sialic Acid: [68Ga]DOTA-en-pba as a New Tool for Molecular Imaging of Cancer with PET Author Tsoukalas, Charalambos (National Centre for Scientific Research Demokritos) Geninatti-Crich, Simonetta (University of Turin) Gaitanis, Anastasios (Biomedical Research Foundation of the Academy of Athens) Tsotakos, Theodoros (National Centre for Scientific Research Demokritos) Paravatou-Petsotas, Maria (National Centre for Scientific Research Demokritos) Aime, Silvio (University of Turin) Jiménez-Juárez, R. (National Polytechnic Institute) Anagnostopoulos, Constantinos D. (Biomedical Research Foundation of the Academy of Athens) Djanashvili, K. (TU Delft BT/Biocatalysis) Bouziotis, Penelope (National Centre for Scientific Research Demokritos) Date 2018-02-20 Abstract Purpose: The aim of this study was to demonstrate the potential of Ga-68-labeled macrocycle (DOTA-en-pba) conjugated with phenylboronic vector for tumor recognition by positron emission tomography (PET), based on targeting of the overexpressed sialic acid (Sia). Procedures: The imaging reporter DOTA-en-pba was synthesized and labeled with Ga-68 at high efficiency. Cell binding assay on Mel-C and B16-F10 melanoma cells was used to evaluate melanin production and Sia overexpression to determine the best model for demonstrating the capability of [68Ga]DOTA-en-pba to recognize tumors. The in vivo PET imaging was done with B16-F10 tumor-bearing SCID mice injected with [68Ga]DOTA-en-pba intravenously. Tumor, blood, and urine metabolites were assessed to evaluate the presence of a targeting agent. Results: The affinity of [68Ga]DOTA-en-pba to Sia was demonstrated on B16-F10 melanoma cells, after the production of melanin as well as Sia overexpression was proved to be up to four times higher in this cell line compared to that in Mel-C cells. Biodistribution studies in B16-F10 tumor-bearing SCID mice showed blood clearance at the time points studied, while uptake in the tumor peaked at 60 min post-injection (6.36 ± 2.41 % ID/g). The acquired PET images were in accordance with the ex vivo biodistribution results. Metabolite assessment on tumor, blood, and urine samples showed that [68Ga]DOTA-en-pba remains unmetabolized up to at least 60 min post-injection. Conclusions: Our work is the first attempt for in vivo imaging of cancer by targeting overexpression of sialic acid on cancer cells with a radiotracer in PET. To reference this document use: http://resolver.tudelft.nl/uuid:81843603-230d-4806-9573-f271b6b83a3f DOI https://doi.org/10.1007/s11307-018-1176-0 Embargo date 2019-02-20 ISSN 1536-1632 Source Molecular Imaging and Biology, 1-10 Part of collection Institutional Repository Document type journal article Rights © 2018 Charalambos Tsoukalas, Simonetta Geninatti-Crich, Anastasios Gaitanis, Theodoros Tsotakos, Maria Paravatou-Petsotas, Silvio Aime, R. Jiménez-Juárez, Constantinos D. Anagnostopoulos, K. Djanashvili, Penelope Bouziotis Files PDF MolImagBiol_2018_peer_reviewd.pdf 1.19 MB Close viewer /islandora/object/uuid:81843603-230d-4806-9573-f271b6b83a3f/datastream/OBJ/view