Abstract: Integrin αvβ3, highly expressed in tumor cells and tumor vasculature endothelial cells but rarely expressed in mature vessels or normal tissues, and it can specifically recognize and combine with the peptides which containing tripeptide sequence Arg-Gly-Asp(RGD). Some stable RGD peptides and RGD-bombesin heterodimers are synthesized by structure modification and multimerization of RGD peptides. These RGD peptides labeled with gamma-emitting and positron-emitting nuclides have been reported as the target tumor imaging research hotspot, and clinical trials are under way. The PET/CT, SPECT/CT and PET/MRI multimode imaging are focused on the quantitative analysis of tumor integrin αvβ3 expression level and anti-angiogenesis patient screening, therapeutic effect evaluation and real time monitoring.