Development of survivin imaging agents for the realization of tumor specific nuclear medicine diagnosis

在本研究中，我们旨在开发靶向Survivin的放射性药物，以实现肿瘤特异性核医学诊断。由于4，6-二芳基吡啶酮类化合物对Survivin蛋白的二聚体具有很高的亲和力，因此我们合成了几种新的衍生物，并对其进行了评价。在高表达Survivin的癌细胞的结合实验中，这些4，6-二芳基吡啶酮类化合物表现出高的膜通透性和与Survivin表达部位相似的蓄积模式。此外，体内生物分布研究表明，4，6-二芳基吡啶酮具有中等的血液滞留和正常组织的快速清除。本研究结果表明，这些4，6-二芳基吡啶酮类化合物可能是很有前途的Survivin肿瘤显像剂。

In the present study, we aimed to develop survivin targeting radiopharmaceuticals for the realization of tumor specific nuclear medicine diagnosis. Because 4, 6-diaryl pyridinones have been reported to possess high affinity for dimer site of survivin protein, several derivatives were synthesized and evaluated. In the binding assay using the cancer cells with high expression of survivin, these 4, 6-diaryl pyridinone derivatives showed high membrane permeability and similar accumulation pattern with survivin expression site. Furthermore in vivo biodistribution study revealed that[^<125> I] 4, 6-diaryl pyridinones showed moderate blood retention and rapid clearance by normal tissues. The results of this study illustrate that these 4, 6-diaryl pyridinones might be promising tumor imaging agents for survivin.