Synthesis and evaluation of a novel (68)Ga-labeled DOTA-benzamide derivative for malignant melanoma imaging |
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Authors: | Hee-Jung Kim Dong-Yeon Kim Jeong-Hoon Park Seung-Dae Yang Min-Goo Hur Jung-Joon Min Kook-Hyun Yu |
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Affiliation: | Radiation Instrumentation Research Division, Korea Atomic Energy Research Institute, Jeongeup, Republic of Korea; Department of Chemistry, Dongguk University-seoul, Seoul, Republic of Korea. |
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Abstract: | Malignant melanoma displays a highly aggressive metastasis. Thus, early diagnosis of malignant melanoma is important for patient survival. We designed and synthesized a novel (68)Ga-labeled benzamide derivative that specifically binds to melanoma as demonstrated by its ability to bind to melanin. (68)Ga-SCN-DOTA-PCA was synthesized with a radiochemical yield of ~80% and a radiochemical purity of >97% by analytical HPLC. The in vitro binding of (68)Ga-SCN-DOTA-PCA to melanin and its cellular uptake demonstrated the selective uptake in melanin. In addition, the biodistribution and micro-PET imaging of (68)Ga-SCN-DOTA-PCA in B16F10 tumor models showed the specific accumulation in melanoma. These results suggest that (68)Ga-SCN-DOTA-PCA would be a promising agent for melanoma diagnosis. |
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