PROTACs (PROteolysis TArgeting Chimeras) are heterobifunctional molecules with a distinct ligand that targets a specific E3 ligase which is tethered by another ligand specific for the target protein, using an optimized chemical linker. This allows to exploit cell’s own degradation machinery (Ubiquitin Proteasome System) to degrade target proteins.

The PROTAC approach has shown great promise at degrading proteins that were previously deemed extremely difficult to target. Expansion of this technology to the vast undruggable proteome remains elusive due to lack of efficient workflows to understand the structure-activity relationship to assist in rationally designing potent PROTACs.

LifeSensors offers a comprehensive evaluation of PROTAC mediated ubiquitination and degradation using traditional western blotting, reporter gene assays (fluorescent proteins, HiBiT) and LifeSensors’ high-throughput ubiquitination and degradation assays. Our targeted protein degradation team has a strong track record in developing preclinical PROTAC programs starting with identification of ligands for target, ligands for E3 ligases, designing model PROTACs, establishing ubiquitination, degradation, and lead optimization. During the optimization stage we offer collaboration with chemistry teams to rationally design a PROTAC that has superior ubiquitination and degradation profiles that can translate into reliable clinical candidates.