Molecular pharmaceutics
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Molecular pharmaceutics · Mar 2019
Detecting Vulnerable Atherosclerotic Plaques by 68Ga-Labeled Divalent Cystine Knot Peptide.
Integrin αvβ3 has been considered as a promising biomarker for vulnerable atherosclerotic plaques, and it is highly expressed by those instability-associated factors, such as macrophages, vessel endothelial cells, and smooth muscle cells. Our previous study successfully showed that the 64Cu-labeled divalent (containing two RGD motifs) cystine knot peptide, 64Cu-NOTA-3-4A, had high binding affinity and specificity in targeting vulnerable carotid atherosclerotic plaques with increased αvβ3 levels. Therefore, considering that 68Ga has excellent nuclear physical properties for positron emission tomography (PET), this study aimed to investigate the feasibility of using 68Ga-NOTA-3-4A for PET study of vulnerable atherosclerotic plaques. ⋯ Furthermore, the plaque accumulation of 68Ga-NOTA-3-4A was significantly inhibited via coinjection of c(RGDyK). Finally, immunostaining identified integrin αvβ3 expressed by macrophages, vessel endothelial cells, and smooth muscle cells. In summary, 68Ga-NOTA-3-4A has high potential to be a promising PET tracer for imaging vulnerable atherosclerotic plaques.