Abstract
An increase of the click-to-release reaction rate between cleavable trans-cyclooctenes (TCO) and tetrazines would be beneficial for drug delivery applications. In this work, we developed a short and stereoselective synthesis route towards highly reactive sTCOs that serve as cleavable linkers, affording quantitative tetrazine-triggered payload release. In addition, the 5-fold more reactive sTCO exhibited the same in vivo stability as the parent TCO linker when used as antibody linker in circulation in mice.
Supplementary materials
Title
Supplementary Information
Description
Synthesis experimentals and methods for reactivity and release evaluations
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