Linkers

The properties of each linker (length, composition of atoms and rigidity) may significantly impact the spatial orientation and alignment of the two functional elements of PROTACs. We have assembled a collection of 100+ linkers which include the most popular flexible polyethylene glycol (PEG) chains as well as more rigid heterocycle-containing linkers (piperidine-based and piperazine-based). The terminal functionality of our linkers represents a diverse selection of functional groups: diamines, amino acids, amino alcohols, amino alkynes, and amino epoxides.
The potential therapeutic application of bifunctional molecules goes far beyond protein degraders (e.g. selective RNA degradation with ribonuclease targeting chimeras RIBOTAC or protein stabilization with DUPTAC) making the connection of two functional ligands with a proper linker a versatile approach for the design of new therapeutic modalities with superior properties. All our linker building blocks conform to the highest quality standards for HPLC purity and structural LC-MS and 1H NMR characterization.