Abstract
Eliminated without a trace: The fastest click reaction, the highly selective inverse-electron-demand Diels-Alder reaction, has been modified to enable selective bioorthogonal release. Thus, the click reaction of a tetrazine with a drug-bound trans-cyclooctene caused the instantaneous release of the drug and CO2 (see scheme). One possible application is the chemically triggered release, and thereby activation, of a drug from a tumor-bound antibody-drug conjugate.
Original language | English |
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Pages (from-to) | 14112-14116 |
Number of pages | 5 |
Journal | Angewandte Chemie - International Edition |
Volume | 52 |
Issue number | 52 |
DOIs | |
Publication status | Published - 23 Dec 2013 |
Keywords
- cycloaddition
- elimination
- pyridazines
- tetrazines
- trans-cyclooctene