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Cyclic peptides containing the Arg-Gly-Asp (RGD) sequence have been shown to specifically bind the angiogenesis biomarker  α    V    β   3  integrin. We report the synthesis, chemical characterization, and biological evaluation of two novel dimeric cyclic RGD-based molecular probes for the targeted imaging of  α    V    β   3  activity (a radiolabeled version,  64 Cu-NOTA-PEG 4 -cRGD 2 , for PET imaging, and a fluorescent version, FITC-PEG 4 -cRGD 2 , for  in vitro  work). We investigated the performance of this probe at the receptor, cell, organ, and whole-body levels, including its use to detect diabetes associated impairment of ischemia-induced myocardial angiogenesis. Both versions of the probe were found to be stable, demonstrated fast receptor association constants, and showed high specificity for  α    V    β   3  in HUVECs ( K    d   ~ 35 nM). Dynamic PET-CT imaging indicated rapid blood clearance via kidney filtration, and accumulation within  α    V    β   3 -positive infarcted myocardium.  64 Cu-NOTA-PEG 4 -cRGD 2  demonstrated a favorable biodistribution, slow washout, and excellent performance with respect to the quality of the PET-CT images obtained. Importantly, the ratio of probe uptake in infarcted heart tissue compared to normal tissue was significantly higher in non-diabetic rats than in diabetic ones. Overall, our probes are promising agents for non-invasive quantitative imaging of  α    V    β   3  expression, both  in vitro  and  in vivo .

Synthesis, Chemical Characterization and Multiscale Biological Evaluation of a Dimeric-cRGD Peptide for Targeted Imaging of α V β 3 Integrin Activity