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KMID : 1145520220080020077
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Journal of Radiopharmaceuticals and Molecular Probes
2022 Volume.8 No. 2 p.77 ~ p.85
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Development & Assessment of Alkyl Chain Modified Aptamers as Potential PET Radiotracers for Lymphoma Diagnosis
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Lee Ji-Woong
Shin Un-Chol
Bae Seok-U
Kim Ji-Yoon
Cho Hae-Joon
Park Ji-Ae
Lee Kyo-Chul
Kim Jung-Young
Kim Suhng-Wook
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Abstract
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The Td05 and Sgc8c, DNA-based aptamers, are well-known to target internalized surface markers (IGHM and PTK7) of Burkitt’s lymphoma and acute lymphoblastic leukemia (ALL). Thus, Td05 and Sgc8c labeled with metallic radioisotope 64Cu can be evaluated as potential diagnostic PET imaging agents. In this study, we modified the carbon chain length of the last adenosine of aptamer (n = 3, 6, 12) to increase tumor cell uptake and select the best candidate among six types of aptamer analogues and one adenosine of aptamer. After labeling of 64Cu, [64Cu]Cu-DOTA-aptamer analogues were evaluated in vitro studies (serum stability, Log P values, cell uptake, biodistribution). Then, we evaluate in vivo PET imaging study for two candidates (64Cu-DOTA-C12-Sgc8c, 64Cu-DOTA-C6-Td05). PET images clearly visualize tumors at 24 h post-injection rather than at an early time point and the tumor-to-background ratio also increases at the delay time point. 64Cu-DOTA-C12-Sgc8c and 64Cu-DOTA-C6-Td05 could be used as potential radiotracers for lymphoma.
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KEYWORD
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Td05, Sgc8c, Burkitt’s lymphoma, Acute lymphoblastic leukemia, 64Cu-DOTA-C12-Sgc8c, 64Cu-DOTA-C6-Td05
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