放射性标记RGD肽行肿瘤αvβ3受体显像研究的进展

Study Progress of Malignant Tumor Imaging of Integrin αvβ3 Expression with Radiolabelled RGD Peptides

恶性肿瘤的持续生长、侵袭转移与肿瘤血管生成密切相关,在这个过程中整合素αvβ3起着重要的作用。αvβ3主要通过和细胞外基质(ECM)中的一些含RGD的三肽序列配体结合发挥作用,文献报道其在新生血管内皮细胞有强烈表达,而在正常细胞表达极少或缺乏,因此,放射性标记RGD肽作为高特异性的标记物对恶性肿瘤进行核医学显像,能够达到早期诊断和治疗目的。本文就近年来国内外RGD肽的标记方法和αvβ3受体显像研究进行了综述。

The malignant tumors must establish a neovaseulature to grow,to invade,and to metastasize,in which integrinsαvβ3 play an important role. It is found that the αvβ3 integrins produced its effect mainly by binding to triplet peptides BGD sequence in the proteins of the extracellular matrix. Because the expression of αvβ3 integrins is reported to be strong on activated endothelial cells but absent or rare on normal cells, so radiolabeled RGD antagonistic peptides could be used as high tumor specific markers to display tumor by nuclear medicine image and then we can success in early diagnosis and therapy. This article reviews the marking method of RGD peptide and study about the image ofαvβ3