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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