A link to the drug: Self-eliminating linkers in drug delivery and bioorthogonal chemistry

Self-eliminating linkers enable chemists and biologists to mask a chemical group required for function, with the added benefit of being able to control the removal of the group on demand. However, there are still some issues with these types of linkers including: (1) non-optimal release kinetics and (2) generation of reactive by-products.

Our investigations into improved stimuli-responsive self-eliminating linkers will be presented. For example, we have developed a method for bioorthogonal activation of prodrugs, whereby the structure of the linker dictates the release rate of the drug.

Also discussed will be our work investigating the potential to generate bioactive heterocycles in situ from reactive linker by-products following activation and self-elimination of the prodrug.