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. 2022 Jan 17;82(7):1409–1422. doi: 10.1158/0008-5472.CAN-21-2897

Figure 1.

Figure 1. Bdd shows remarkable urinary disposing properties. A, A table showing the components and the net charges of BDD as well as its D-configuration (Bdd), neutrally charged (BKD), positively charged (BKK), and pegylated (PEG3DD) counterparts. B, A synthetic scheme showing radiolabeling of the peptides with 89Zr for comparative PK and biodistribution studies. C, Representative μPET/CT images of BALB/cJ mice acquired 1, 4, and 24 hours after administration of different 89Zr-radiolabeled peptides (20 μCi, 20 μg, in 100 μL PBS) via tail-vein injections (n = 4/group). The whole body images were acquired with or without emptying the animal's bladders. D, Bar chart showing the amount of radioactivity in urine samples (20 μL) collected from animals (n = 5) at different time intervals after administration of 89Zr-Bdd. E, Comparing the renal clearance of the radiolabeled peptides. Plots showing the percentage of injected dose (%ID) in kidneys of the animals over time. The percentage of ID was calculated according to the radioactivity measured at the ROI of the acquired PET images. F, Comparing the PK profiles of the radiolabeled peptides (n = 4/analogue). Blood samples (20 μL) were collected at various time intervals after injection of the peptides or free 89Zr to the animals. The results (radioactivity measured in blood samples) were fit into a two-compartmental model for determining the t1/2α (half-life of distribution phase) and t1/2β (half-life of elimination phase). The other PK parameters are available in Supplementary Fig. S1A. G, Endpoint biodistribution study of 89Zr-Bdd. The animals were euthanized at different time intervals (n = 4/time point) after administration of the peptide (20 μCi, 20 μg, in 100 μL PBS). The amount of peptide (radioactivity) in the harvested organs was determined. The results (corrected from decay) were expressed as %ID. Student t test; **, P < 0.01; ***, P < 0.001.

Bdd shows remarkable urinary disposing properties. A, A table showing the components and the net charges of BDD as well as its D-configuration (Bdd), neutrally charged (BKD), positively charged (BKK), and pegylated (PEG3DD) counterparts. B, A synthetic scheme showing radiolabeling of the peptides with 89Zr for comparative PK and biodistribution studies. C, Representative μPET/CT images of BALB/cJ mice acquired 1, 4, and 24 hours after administration of different 89Zr-radiolabeled peptides (20 μCi, 20 μg, in 100 μL PBS) via tail-vein injections (n = 4/group). The whole body images were acquired with or without emptying the animal's bladders. D, Bar chart showing the amount of radioactivity in urine samples (20 μL) collected from animals (n = 5) at different time intervals after administration of 89Zr-Bdd. E, Comparing the renal clearance of the radiolabeled peptides. Plots showing the percentage of injected dose (%ID) in kidneys of the animals over time. The percentage of ID was calculated according to the radioactivity measured at the ROI of the acquired PET images. F, Comparing the PK profiles of the radiolabeled peptides (n = 4/analogue). Blood samples (20 μL) were collected at various time intervals after injection of the peptides or free 89Zr to the animals. The results (radioactivity measured in blood samples) were fit into a two-compartmental model for determining the t1/2α (half-life of distribution phase) and t1/2β (half-life of elimination phase). The other PK parameters are available in Supplementary Fig. S1A. G, Endpoint biodistribution study of 89Zr-Bdd. The animals were euthanized at different time intervals (n = 4/time point) after administration of the peptide (20 μCi, 20 μg, in 100 μL PBS). The amount of peptide (radioactivity) in the harvested organs was determined. The results (corrected from decay) were expressed as %ID. Student t test; **, P < 0.01; ***, P < 0.001.