Increasing Time on Target: Utilization of Inhibitors of Cysteine Cathepsins to Enhance the Tumor Retention of Receptor-Targeted Agents

摘要

We report a strategy of utilizing irreversible cysteine cathepsin inhibitor as trapping agent to increase the tumor residence time of receptor-targeted agents. The targeted constructs incorporating these cysteine cathepsin trapping agents were able to form high molecular weight adducts with intracellular cysteine cathepsins, thus achieving superior retention in tumor tissues.