Radiolabeling RGD-Peptide Using fac-¹⁸⁸Re(CO)₃(H₂O)₃⁺

Integrin α_vβ₃ is a member of the integrin family, which plays an important role in angiogenesis and tumour metastasis. The peptides containing arginine-glycine-aspartic acid(RGD) sequence can bind to integrin α_vβ₃ selectively. In the present study, we labeled two RGD-peptides via fac-¹⁸⁸Re(CO)₃(H₂O)₃⁺. The results show that the labeling yields are more than 90% for both of radiolabeled compounds, and they are all stable in phosphate buffered saline and new-born calf serum, even challenged in histidine or cysteine solution. We will evaluate their biological properties to develop radiolabeled agents for tumor therapy.