利用放射性核素标志物靶向示踪肿瘤并显像已成为肿瘤早期诊断的一种重要方法。精氨酸-甘氨酸-天冬氨酸(RGD)多肽可与肿瘤新生血管内皮细胞表达的整合素αⅤβ3特异性结合,用放射性核素标记RGD肽,利用分子影像技术可示踪肿瘤新生血管,从而在早期确立诊断。文章就近年来国内外RGD肽的修饰、标记方法、纳米技术应用进行阐述,并就利用αⅤβ3受体,综述了RGD肽介导的PET/SPECT显像、磁共振显像、超声显像、光学显像临床应用进展。 Targeted tracking of tumors using radionuclide markers and imaging has become an important method of early diagnosis of tumors. The arginine-glycine-aspartic acid (RGD) polypeptide can specifically bind with integrin αVβ3 expressed by tumor neovascular endothelial cells. The radionuclide-labeled RGD peptide can be used to detect tumor neovascularization by using molecular imaging technique Early diagnosis. In this paper, we describe the modification, labeling and application of RGD peptides at home and abroad in recent years. In the light of the use of αVβ3 receptor, we reviewed the effects of RGD peptide-mediated PET / SPECT imaging, magnetic resonance imaging, Like clinical application progress.