Background: RGD peptides are small peptides containing arginine-glycine-aspartic (Arg-
Gly-Asp) acid triple-peptide motif and can specifically bind to integrin receptor on the cell surface.
Discussion: The integrin receptors, especially alpha(v) beta(3), are highly expressed on the surface
of activated endothelial cells and tumor cells while displaying low expression on mature endothelial
cells. Molecular imaging can achieve the imaging of the biological processes at cellular and
molecular levels in vivo and help in qualitative and quantitative research, making the evaluation of
the expression levels of integrin possible in vivo.
Conclusion: Therefore, RGD peptides show great potential in the study of specific imaging of tumor-
induced angiogenesis. This study reviewed the recent research progress of RGD peptide–
mediated imaging of tumor-induced angiogenesis, which can benefit the RGD peptide–targeted
molecular imaging researches.