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Abstract #1130

Tumor-Specific Self-Assembly of DiaCEST Nanoparticles as Theranostic Agents

Yue Yuan1, Jia Zhang1, Xiaoliang Qi1, Shuoguo Li2, Guanshu Liu3, Xiaolei Song1, Michael McMahon3, and Jeff Bulte1

1Johns Hopkins University, Baltimore, MD, United States, 2Chinese Academy of Sciences, Beijing, China, 3Kennedy Krieger Institute, Baltimore, MD, United States

We employed a tumor-specific enzyme (furin)-mediated conversion of the anti-cancer and CEST MRI-visible drug olsalazine (Olsa), which resulted in the formation of self-assembled intracellular nanoparticles in tumor cells. In vivo studies using high-furin and low-furin expressing human xenografts showed that the OlsaCEST signal and anti-tumor therapeutic effect were 5 to 6-fold increased compared to single olsalazine molecules. An excellent “theranostic correlation” (R2 = 0.97) could be observed between the magnitude of the CEST MRI signal and therapeutic response (normalized tumor size).

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