Evaluation of a 188Re‐radiolabeled Arg‐Gly‐Asp peptide for tumor overexpressed αvβ3 receptors |
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Authors: | Yufei Ma Junfeng Yu Yanjiang Han Cheng Wang Jianbo Li Hua Shen Ni Wang Duanzhi Yin |
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Affiliation: | The Centre of Radiopharmaceutical Research, Shanghai Institute of Applied Physics, Chinese Academy of Sciences, , Shanghai, 201800 China |
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Abstract: | To develop a peptide‐based radiopharmaceutical for the therapy of αvβ3 receptors overexpressed tumors, we have prepared a novel Arg‐Gly‐Asp (RGD) peptide (HCRGDCF(D)CRGDC, P12) radiolabeled with 188Re. With His acid at the end of the peptide containing RGD, the label efficiency was more than 95% within 30 min. The peptide binds to human glioblastoma U87MG cells with high affinity [IC50 = 86.3 nm]. The stability of 188Re‐P12 in vitro was also investigated. More than 80% of radioactivity was kept in the peptide after 4 h incubation in phosphate buffer solution (pH = 7.4) or calf serum under physiological conditions. Biodistribution of this radiocompound was carried out in mice bearing S180 tumor. Fast clearance of 188Re‐peptide from blood and specific uptakes by tumors realized higher tumor‐to‐blood ratio (1.80) 4 h post‐injection. Obvious difference was observed between the blocking and unblocking experiments in whole body autoradiography imaging. These results have demonstrated the potential of 188Re‐labeling RGD as a radiotherapeutic agent. |
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Keywords: | 188Re S180 tumor radiolabeling RGD peptide α vβ 3 |
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