Abstract
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.
Highlights
The efficacy of a pharmacotherapy usually depends on whether the drug would achieve its optimal concentration at the specific lesions
[31], providing an opportunity release1B). These strategies about tetrazine-responsive prodrug activation mainly focus on the cytotoxic groups for selective activation of proteins [42,43], fluorogenic probes [44,45] and prodrugs [2,27,46]
Phase I clinical based on a Click combination targeted systems, the inactive prodrugs can betrial selectively released this review, we summarized several without causing toxicity to normal, healthy tissue
Summary
The efficacy of a pharmacotherapy usually depends on whether the drug would achieve its optimal concentration at the specific lesions. Prodrugs [2,27,46] to (Figure in living the cleavage of carbamates, esters and ethers [31], providing an opportunity release1B) These strategies about tetrazine-responsive prodrug activation mainly focus on the cytotoxic groups for selective activation of proteins [42,43], fluorogenic probes [44,45] and prodrugs [2,27,46]. Chemotherapeutics usually associated therapeutic window and severe systemic (Figure 1B) in livingwhich systems These strategieswith aboutnarrow tetrazine-responsive prodrug activation mainly adverse effects. One of the two bioorthogonal reactants acts as a pro-moiety in the prodrug, and the focus on the cytotoxic chemotherapeutics which usually associated with narrow therapeutic window partner acting as a trigger releases the active drug upon reaction. This review, we prodrug-activation chemistries based on tetrazine bioorthogonal cleavage reaction and their further applications for in vivo drug delivery
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