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Evaluation of a Re-188-radiolabeled Arg-Gly-Asp peptide for tumor overexpressed alpha(v)beta(3) receptors
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)
2011
Source PublicationJOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
ISSN0362-4803
Volume54Issue:41162Pages:602
AbstractTo 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.
Indexed BySCI
Language英语
Funding Project应物所项目组
WOS IDWOS:000295901500004
Citation statistics
Cited Times:1[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.sinap.ac.cn/handle/331007/9508
Collection中科院上海应用物理研究所2011-2020年
Recommended Citation
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.
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