Integrins alpha v beta 3 are heterodimeric transmembrane glycoproteins,consisting of two noncovalently bound transmembrane subunits.Integrins alpha v beta 3 are usually expressed at low or undetectable levels in most adult epithelia but can be highly upregulated in some tumours and vascular endothelial cells,which make them an appealing targets for molecular imaging and therapy.Many different approaches for imaging ot integrins alpha v beta 3 expression have been studied in the recent years,including positron emission tomography,single photon emission tomography,magnetic resonance imaging,ultrasound and optical imaging.Integrin antagonists include function-blocking monoclonal antibodies,RGD peptide mimetics,targeted delivery of therapy.Preclinical studies and clinical trials of targeted therapy have great significance for exploring new therapy for tumor.