An atom-economical design of PET tracer for imaging α v β 3 integrin via utilizing the three-in-one function of 64 Copper.

In this study, alpha(v)beta(3) integrin in U87 tumor cells was imaged with a Cu-64-peptidic probe, in which the linear peptide GHRGDHG is used as a pre-ligand, while Cu-64 bears three functional roles that include generation of the PET signal, coordination with two GH moieties of the pre-ligand, and cyclizing the linear pre-ligand into an active cyclic-RGD form (termed as Cu-64-Cyclo-RGD) for alpha(v)beta(3) integrin.