Based on a biocompatible condensation reaction caused by tumor-related proprotein convertase furin, we developed a novel probe RRVR-Olsa for tumor-targeted CEST MR imaging and chemotherapy to accomplish theranostics. Our preliminary studies indicated that, RRVR-Olsa elicited an obvious increase in CEST signal and higher cytotoxicity on furin-overexpressing HCT116 cancer cells than on furin-deficient LoVo cells and on furin inhibitor-treated HCT116 cancer cells. In vivo CEST MRI with the use of RRVR-Olsa could readily distinguish the difference of furin expression in HCT116 tumor and LoVo tumor, which we attributed to the furin-directed intracellular self-assembly of RRVR-Olsa to olsalazine nanoparticles with enhanced accumulation.
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