Chemically controlling the release of active molecules (e.g. drugs, fluorophores) in a biological environement will be applicable to a broad range of uses in chemical biology and drug delivery. We have designed new release molecules that rapidly react with tetrazines to efficiently liberate payload molecules. The design is compatible with different types of leaving groups, and the precursor molecules exhibit prolonged stability in serum. The release at physiological conditions was succesfully demonstrated by efficient tetrazine-mediated release of doxorubicin from a reactive prodrug inducing cytotoxicity in cancer cells. NMR-based studies provided preliminary mechanistic insights into this bioorthogonal dissociative reaction.<br/>

Tetrazine-induced release reactions

255th National Meeting (2018)

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