Evaluation of a 188Re-radiolabeled Arg-Gly-Asp peptide for tumor overexpressed αvβ3 receptors
✍ Scribed by Yufei Ma; Junfeng Yu; Yanjiang Han; Cheng Wang; Jianbo Li; Hua Shen; Ni Wang; Duanzhi Yin
- Publisher
- John Wiley and Sons
- Year
- 2011
- Tongue
- French
- Weight
- 346 KB
- Volume
- 54
- Category
- Article
- ISSN
- 0022-2135
No coin nor oath required. For personal study only.
✦ Synopsis
To develop a peptide‐based radiopharmaceutical for the therapy of α~v~β~3~ receptors overexpressed tumors, we have prepared a novel Arg‐Gly‐Asp (RGD) peptide (HCRGDCF(D)CRGDC, P12) radiolabeled with ^188^Re. 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 [IC~50~ = 86.3 nm]. The stability of ^188^Re‐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 ^188^Re‐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 ^188^Re‐labeling RGD as a radiotherapeutic agent.