铼羰基化合物标记含RGD的多肽

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

摘要: α_vβ^₃是一种在包括肿瘤引起的血管增生及肿瘤转移中起重要作用的细胞黏附受体，含RGD序列的肽及其类似物可以作为拮抗剂与α_vβ₃正常配体进行竞争结合。本工作以三羰基铼为前体标记了2个含有RGD序列的多肽，实验结果表明，2个多肽的标记率和放化纯度均大于90%，体外稳定性良好。将进一步对其进行生物评价，以判别其是否有潜力发展成为肿瘤治疗剂。

Abstract: Integrin α_vβ₃is 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.