Radiation Instrumentation Research Division, Korea Atomic Energy Research Institute, Jeongeup, Republic of Korea.
Bioorg Med Chem Lett. 2012 Aug 15;22(16):5288-92. doi: 10.1016/j.bmcl.2012.06.043. Epub 2012 Jun 19.
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.
恶性黑色素瘤表现出高度侵袭性的转移。因此，恶性黑色素瘤的早期诊断对患者的生存至关重要。我们设计并合成了一种新型的（68）Ga 标记的苯甲酰胺衍生物，通过其与黑色素结合的能力证明其能特异性结合黑色素。（68）Ga-SCN-DOTA-PCA 的放射化学产率约为 80%，放射化学纯度大于 97%，通过分析 HPLC 得到。（68）Ga-SCN-DOTA-PCA 与黑色素的体外结合及其细胞摄取表明其对黑色素具有选择性摄取。此外，（68）Ga-SCN-DOTA-PCA 在 B16F10 肿瘤模型中的生物分布和 micro-PET 成像显示其在黑色素瘤中的特异性积累。这些结果表明，（68）Ga-SCN-DOTA-PCA 可能成为一种有前途的黑色素瘤诊断剂。
