Figure 12.

(a) Schematic illustrations of furin-guided Ga nanoparticles formation. After reduction and furin cleavage, CBT-Ga is subjected to the CBT-Cys click condensation reaction to yield the cyclized oligomers, which self-assemble into Ga nanoparticles CBT-Ga-NPs. Schematic illustrations are also present of furin-controlled condensation of CBT-⁶⁸Ga and CBT-Ga to yield hybrid oligomers, which self-assemble into radioactive nanoparticles CBT-⁶⁸Ga-NPs in furin-overexpressing cancer cells. (b) Representative whole body coronal microPET images of MDA-MB-468 tumor-bearing mice at different time points postintravenous injections of 100 μL of 5–12 MBq of CBT-⁶⁸Ga and 20 mg kg^–1 of CBT-Ga (top) or 5–12 MBq of CBT-⁶⁸Ga (bottom) via tail veins. White dashed ellipses indicate the tumors. (c) Time course uptake of CBT-⁶⁸Ga in heart, liver, lung, kidney, brain, muscle, and MDA-MB-468 tumor. The data were derived from PET quantification [% injected dose (ID)/g, n = 4 for each group]. (d) Time course bar graphs of the tumor/liver ratios in part (c). Reproduced with permission from ref (96). Copyright 2019 American Chemical Society.