Nuclear Science and Techniques

《核技术》(英文版) ISSN 1001-8042 CN 31-1559/TL     2019 Impact factor 1.556

Nuclear Science and Techniques ›› 2012, Vol. 23 ›› Issue (1): 47-51 doi: 10.13538/j.1001-8042/nst.23.47-51


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

MA Yufei1 YU Junfeng2 WANG Cheng2 SHEN Hua2 WU Hua1   

  1. 1Department of Nuclear Medicine,the First affiliataed Hospital,Xiamen University,55 Zhenhai Rd.,Xiamen 361003,China 2Centre of Radiopharmaceutical Research,Shanghai Institute of Applied Physics,Chinese Academy of Science,Shanghai 201800,China
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MA Yufei, YU Junfeng, WANG Cheng, SHEN Hua, WU Hua. Radiolabeling and evaluation of 188Re-RGD as an agent for α_vβ_3 receptor expression.Nuclear Science and Techniques, 2012, 23(1): 47-51     doi: 10.13538/j.1001-8042/nst.23.47-51


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.

Key words: fac-[188Re(H2O)3(CO)3]+, RGD peptide, Integrinαvβ3