放射性核素标记RGD序列多肽与整合素αvβ3受体显像的研究进展

Study progress of malignant tumor imaging of integrin αvβ3 expression with radioisotope labelled RGD peptides

整合素主要介导细胞与细胞、细胞与细胞外基质（ECM）之间的相互黏附，对细胞的黏附、增殖、分化、转移、凋亡起到重要的调控作用，在肿瘤的侵袭转移中发挥重要作用。成熟血管内皮细胞和绝大多数正常器官系统中，整合素αvβ3受体表达缺乏或几乎不能被探及，但其在新生血管内皮细胞中有强烈表达，精氨酸-甘氨酸-天冬氨酸（RGD）肽是整合素αvβ3受体的特异性识别位点，因此，将放射性核素标记到含有RGD序列的肽类化合物上，用于整合素αvβ3受体显像，对于肿瘤早期和高特异性定位、定量诊断及治疗都具有重要意义。近年来国内外对RGD肽的标记方法和αvβ3受体显像进行了研究。

The malignant tumors must establish a neovasculature to grow, to invade, and to metastasize, in which αvβ3 integrin plays an important role. It is reported that the αvβ3 integrin made their effection mainly by binding triplet peptides RGD sequence in the proteins of the extracellular matrix. Because is reported to there is no or rare αvβ3 integrin in normal cells but more in activated endothelial cells, RGD is the special target point for αvβ3 Integrin. RGD antagonistic peptides radiolabelled by direct or indirect way could be used to display tumor αvβ3 Integrin by nuclear medicine image. It is of significance to locate and quantitate tumor Integrin high special in early diagnosis and therapy. This article reviews the marking method of RGD peptide and study about the image of αvβ3receptor.