The Legumain Protease‐Activated Auristatin Prodrugs Suppress Tumor Growth and Metastasis without Toxicity

Tumor exploitation: Novel monomethylauristatin E and didesmethylauristatin E prodrugs were prepared, and in vitro and in vivo evaluations of the prodrugs using human and mouse cancer cell lines showed that they are less toxic and more efficacious than the parent cytotoxins, as their activation was catalyzed selectively by the cysteine protease, legumain, which is overexpressed in the active form in tumor microenvironments.