 The Alphavbeta3 integrin, one of the most prominent members of integrin superfamily, is trans-membrane heterodimeric proteins which mediate cell-cell and cell-extracellular matrix adhesion. Integrin alphavbeta3 receptor plays an pivotal role in promoting, sustaining and regulating the angiogenesis and was identified as a marker of angiogenic vascular tissue. Cyclic arginine-glycine-aspartic acid RGD peptides was identified as a key integrin recognition motif which could strongly bind to integrin alphavbeta3 and inhibit new blood vessel formation. Animal study in antigen induced arthritis demonstrated that intra-articular administration of a cyclic RGD antagonist of alphavbeta3 leading to inhibition of cell infiltrate, synovial angiogenesis, pannus formation, cartilage erosions and even diminishing arthritis severity. For these properties, RGD peptide-based multimodality molecular probes have been developed for noninvasive imaging by targeting integrin alphavbeta3. And compared with 18F-FDG PETCT, radiolabeled RGD imaging is a promising approach to visualize angiogenesis and provide a therapeutic target for anti-angiogenetic and anti-integrin therapy. 