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. Author manuscript; available in PMC: 2018 Dec 1.
Published in final edited form as: Bioorg Med Chem Lett. 2017 Oct 21;27(23):5089–5099. doi: 10.1016/j.bmcl.2017.10.051

Figure 8.

Figure 8

Use of a CXCR4-targeting cyclotide as a bioimaging tool for detecting CXCR4-overexpressing tumor cells in animal models.92 A. Distribution of [64Cu]MCo-CVX-6D (CXCR4-targetign cyclotide) and [64Cu]MCoTI-ID (a DOTA-labeled variant of native trypsin inhibitor cyclotide MCoTI-I) in NOD/SCID mice bearing U87 and U87-stb-CXCR4 tumors with PET-CT. Representative PET-CT volume rendered images of mice (n=3) injected with 250 µCi of [64Cu]MCo-CVX-6D or [64Cu]MCoTI-ID recorded 24 h post tracers injection demonstrating high accumulation of [64Cu]MCo-CVX-6D in the U87-stb-CXCR4 tumor and [64Cu]MCoTI-ID showed mostly kidney uptake, suggesting renal clearance for the non-CXCR4-targetign cyclotide. B. Ex vivo evaluation of [64Cu]MCo-CVX-6D and [64Cu]MCoTI-ID distribution and specificity in NOD/SCID mice bearing U87 and U87-stb-CXCR4 tumors. Ex vivo biodistribution analysis was performed at 90 min and 24 h after post tracers injection.