The cell adhesion molecule integrin αvβ3 is an important player in the process of angiogenesis. In
the last decades, a series of radiolabeled Arg-Gly-Asp (RGD) peptides targeting integrin αvβ3 has been
prepared and optimized for positron emission tomography (PET) and single-photon-emission computed
tomography (SPECT) imaging of integrin αvβ3 expression. Several promising radiotracers have been tested in
clinical trials. In this review, we will introduce strategies that have been used to optimize and accelerate RGD
radiotracers towards clinical translation; illustrate RGD-based radiotracers that have been investigated in
clinical trials; and discuss the other applications of RGD radiotracers aside from tumor detection.
Keywords: Arg-Gly-Asp (RGD), integrin αvβ3, molecular imaging, radionuclide therapy, radiotracer, tumor.
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