Activation and Delivery of Tetrazine-Responsive Bioorthogonal Prodrugs
Yayue Wang,
Chang Zhang,
Haoxing Wu,
Ping Feng
Affiliations
Yayue Wang
Huaxi MR Research Center, Department of Nuclear Medicine, Frontiers Science Center for Disease-Related Molecular Network, West China Hospital, Sichuan University, Chengdu 610041, China
Chang Zhang
Huaxi MR Research Center, Department of Nuclear Medicine, Frontiers Science Center for Disease-Related Molecular Network, West China Hospital, Sichuan University, Chengdu 610041, China
Haoxing Wu
Huaxi MR Research Center, Department of Nuclear Medicine, Frontiers Science Center for Disease-Related Molecular Network, West China Hospital, Sichuan University, Chengdu 610041, China
Ping Feng
Institute of Clinical Trials, West China Hospital, Sichuan University, Chengdu 610041, China
Prodrugs, which remain inert until they are activated under appropriate conditions at the target site, have emerged as an attractive alternative to drugs that lack selectivity and show off-target effects. Prodrugs have traditionally been activated by enzymes, pH or other trigger factors associated with the disease. In recent years, bioorthogonal chemistry has allowed the creation of prodrugs that can be chemically activated with spatio-temporal precision. In particular, tetrazine-responsive bioorthogonal reactions can rapidly activate prodrugs with excellent biocompatibility. This review summarized the recent development of tetrazine bioorthogonal cleavage reaction and great promise for prodrug systems.
