Advance of ¹⁸FLabeled RGD Peptide as Integrin α_Ⅴβ₃ Receptor Imaging Agents

Angiogenesis is vital for tumor growth and metastasis. Integrin α_Ⅴβ₃ receptor has been shown to play a key role in tumor angiogenesis and metastasis. The highly expression of integrin α_Ⅴβ₃ receptor in endothelial cells and tumor cells presents an interesting molecular target for diagnosis and treatment of the rapidly growing and metastatic tumors. Arginineglycine-aspartic acid (Arg-Gly-Asp, RGD) peptide can specifically target to integrin α_Ⅴβ₃ receptor. ¹⁸F labeled RGD peptides can be used to non-invasively visualize and quantify α_Ⅴβ₃ integrin expression levels, and play a key role in early diagnosis of tumor, monitoring and evaluation of anti-angiogenesis. In recent years, there has been a great acceleration in the development of radiolabeled receptor-binding peptides for single photon emission computed tomography (SPECT) and positron emission tomography (PET) imaging in nuclear oncology. Integrin α_Ⅴβ₃ receptor is expected to become the new target spot of radioactive substance, while the radioactive nuclide labeled RGD peptides will be a potential tumor imaging agent in clinical. This article reviews the recent development of ¹⁸F labeled RGD peptide and its application in tumor integrin α_Ⅴβ₃ receptor imaging.