Radiolabeling and evaluation of ^(188)Re-RGD as an agent for α_vβ_3 receptor expression  

作　　者：Yufei MA Junfeng YU Cheng WANG Hua SHEN Hua WU 

机构地区：[1]Department of Nuclear Medicine,the First affiliataed Hospital,Xiamen University,55 Zhenhai Rd.,Xiamen 361003,China [2]Centre of Radiopharmaceutical Research,Shanghai Institute of Applied Physics,Chinese Academy of Science,Shanghai 201800,China

出　　处：《Nuclear Science and Techniques》2012年第1期47-51,共5页核技术（英文）

基　　金：Supported by Nature Science Foundation of China under Contract NO.81101066

摘　　要：Integrin αvβ3,a cell adhesion molecule,plays a key role in angiogenesis and tumor cell metastasis and is therefore an important target for new therapeutic and diagnostic strategies.Since RGD bind to αvβ3 particularly,a lot of RGD containing peptides were radiolabeled and evaluated as imaging or therapeutic agents.In this study,a new 188Re-RGD peptide analog was synthesized and characterized.Within 30min,the 188Re-H-E[c(RGDyK)]2 was obtained in radiochemical purity of better than 95%.The His-E[c(RGDyK)]2 had a good integrin-binding affinity (50% inhibitiory concentracer (IC50=46.5×10-9 nm) and exhibited active accumulation (7.20±1.06) in S180 tumor.Because of relatively fast washout in blood and normal tissues,the target/non-target ratio was high.Further experiments to improve the tumor targeting efficacy and in vivo kinetic profiles are in progress towards developing it into a promising radio agent.Integrin avβ3, a cell adhesion molecule, plays a key role in angiogenesis and tumor cell metastasis and is therefore an important target for new therapeutic and diagnostic strategies. Since RGD bind to avβ3 particularly, a lot of RGD containing peptides were radiolabeled and evaluated as imaging or therapeutic agents. In this study, a new 188Re-RGD peptide analog was synthesized and characterized. Within 30 min, the 188Re-H-E[c（RGDyK）]2 was obtained in radiochemical purity of better than 95%. The His-E[c（RGDyK）]2 had a good integrin-binding affinity （50% inhibitiory concentracer （IC50=46.5×10-9 nm） and exhibited active accumulation （7.20±1.06） in S180 tumor. Because of relatively fast washout in blood and normal tissues, the target/non-target ratio was high. Further experiments to improve the tumor targeting efficacy and in vivo kinetic profiles are in progress towards developing it into a promising radio agent.

关 键 词：放射性标记 AV RGD序列 评价 代理 受体 细胞粘附分子 肿瘤细胞 

分 类 号：Q516[生物学—生物化学] S859.84[农业科学—临床兽医学]