Evaluation of a Re-188-radiolabeled Arg-Gly-Asp peptide for tumor overexpressed alpha(v)beta(3) receptors
文献类型:期刊论文
作者 | Ma, Yufei ; Yu, Junfeng(于俊峰) ; Han, Yanjiang ; Wang, Cheng ; Li, Jianbo(李剑波) ; Shen, Hua ; Wang, Ni ; Yin, Duanzhi(尹端沚) |
刊名 | JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
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出版日期 | 2011 |
卷号 | 54期号:41162页码:602 |
ISSN号 | 0362-4803 |
英文摘要 | To develop a peptide-based radiopharmaceutical for the therapy of alpha(v)beta(3) receptors overexpressed tumors, we have prepared a novel Arg-Gly-Asp (RGD) peptide (HCRGDCF(D)CRGDC, P12) radiolabeled with Re-188. 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 Re-188-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 5180 tumor. Fast clearance of Re-188-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 Re-188-labeling RGD as a radiotherapeutic agent. |
收录类别 | SCI |
语种 | 英语 |
WOS记录号 | WOS:000295901500004 |
公开日期 | 2012-07-04 |
源URL | [http://ir.sinap.ac.cn/handle/331007/9508] ![]() |
专题 | 上海应用物理研究所_中科院上海应用物理研究所2011-2017年 |
推荐引用方式 GB/T 7714 | Ma, Yufei,Yu, Junfeng,Han, Yanjiang,et al. Evaluation of a Re-188-radiolabeled Arg-Gly-Asp peptide for tumor overexpressed alpha(v)beta(3) receptors[J]. JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS,2011,54(41162):602. |
APA | Ma, Yufei.,Yu, Junfeng.,Han, Yanjiang.,Wang, Cheng.,Li, Jianbo.,...&Yin, Duanzhi.(2011).Evaluation of a Re-188-radiolabeled Arg-Gly-Asp peptide for tumor overexpressed alpha(v)beta(3) receptors.JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS,54(41162),602. |
MLA | Ma, Yufei,et al."Evaluation of a Re-188-radiolabeled Arg-Gly-Asp peptide for tumor overexpressed alpha(v)beta(3) receptors".JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS 54.41162(2011):602. |
入库方式: OAI收割
来源:上海应用物理研究所
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