Protein Degrader Building Blocks

Targeted protein degradation (TPD) is a novel approach in drug discovery to effectively infiltrate the cell’s proteasomal degradation pathway and quickly eliminate target proteins from cells. This strategy has the potential to develop new therapeutics that differ considerably from classical inhibitors and is even viable for accessing “undruggable” protein targets and difficult-to-treat diseases.

Our diverse portfolio of protein degrader building blocks allows you to easily generate libraries of protein degraders that can be screened for effective degradation of your target proteins from cells. Our protein degraders, such as proteolysis targeting chimeras (PROTAC® molecules), are bifunctional molecules with three primary components: a ligand at one end that targets the protein of interest (POI); a second ligand at the opposite end that binds an E3 ligase; and a crosslinker in the middle that joins the two ends. The simultaneous degrader binding of two proteins brings the POI in close enough proximity for polyubiquitination by the E2 enzyme associated to the E3 ligase, which flags the POI for degradation through the proteasome.