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. Author manuscript; available in PMC: 2021 Jul 28.
Published in final edited form as: J Am Chem Soc. 2021 Mar 19;143(12):4714–4724. doi: 10.1021/jacs.1c00312

Figure 4. Phenyl ester traceless linker editing for optimized T-API release.

Figure 4.

a, Drug release mechanism via 1,6-elimination from triazolopyridazinium salts conjugates in T-series brush prodrugs. b, Modulation of release kinetics of the T-API via linker chemistry. c, Release of T-API inhibitor in vitro (saline buffer, 37 °C). d, Released T-API in tumors 72 h after the last dose in 60 mg/kg × 4 treatment groups (n=5). Concentration of released T-API at the tumor site is finely tuned via linker chemistry; error bars represent SD. e, Ratios of released T-API in the tumor relative to whole blood. Brush prodrugs offer favorable accumulation and differential release in the tumor. a: below limit of quantification.