Abstract

The cell adhesion molecule integrin α_vβ₃ is an important player in the process of angiogenesis. In the last decades, a series of radiolabeled Arg-Gly-Asp (RGD) peptides targeting integrin α_vβ₃ has been prepared and optimized for positron emission tomography (PET) and single-photon-emission computed tomography (SPECT) imaging of integrin α_vβ₃ 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 α_vβ₃, molecular imaging, radionuclide therapy, radiotracer, tumor.