Proximity-Induced Bioorthogonal Chemistry Using Inverse Electron Demand Diels-Alder Reaction

Möhler, Jasper S.; Werther, Philipp

doi:10.1007/978-1-4939-9537-0_12

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Tetrazine-triggered Cleavage From Vinyl Ether1

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2020

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“…But the second-order rate constants (k Table 1) [66] are several orders of magnitude lower than those of TCO or other strained alkenes. Although vinyl ethers may function well in proximity-induced reactions such as those involving nucleic acids [80], the sluggish kinetics could be the major obstacle to its application in vivo [80].…”

Section: Tetrazine-triggered Cleavage From Vinyl Ethermentioning

confidence: 99%

Activation and Delivery of Tetrazine-Responsive Bioorthogonal Prodrugs

Wang

Zhang

et al. 2020

Molecules

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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.

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Section: Tetrazine-triggered Cleavage From Vinyl Ethermentioning

confidence: 99%