RGD-based PET tracers for imaging receptor integrin αvβ3 expression

Positron emission tomography (PET) imaging of receptor integrin αvβ3 expression may play a key role in the early detection of cancer and cardiovascular diseases, monitoring disease progression, evaluating therapeutic response, and aiding anti‐angiogenic drugs discovery and development. The last decade has seen the development of new PET tracers for in vivo imaging of integrin αvβ3 expression along with advances in PET chemistry. In this review, we will focus on the radiochemistry development of PET tracers based on arginine–glycine–aspartic acid (RGD) peptide, present an overview of general strategies for preparing RGD‐based PET tracers, and review the recent advances in preparations of 18F‐labeled, 64Cu‐labeled, and 68Ga‐labeled RGD tracers, RGD‐based PET multivalent probes, and RGD‐based PET multimodality probes for imaging receptor integrin αvβ3 expression. The last decade has seen the development of new PET tracers for in vivo imaging of integrin αvβ3 expression along with advances in PET chemistry. In this review, we will focus on radiochemistry development of PET tracers based on arginine‐glycine‐aspartic acid (RGD) peptide, and present an overview of general strategies for preparing RGD based PET tracers, review the recent advances in preparations of 18F, 64Cu, and 68Ga labeled RGD tracers, RGD‐based PET multivalent probes, and RGD‐based PET multimodality probes for imaging receptor integrin αvβ3 expression.