ChemPartner’s in vitro biology team has developed a series of assays for protein ubiquitin-proteasome system, including deubiquitination enzyme activity, E1 activating enzyme activity, E2 conjugating enzyme activity, and the E3 ligase activity assays, which can be used to identify inhibitors or activators in the system.
Assay Platform for Ubiquitin System
Meanwhile, the research on the ubiquitin-protease system also gave birth to a new drug discovery approach, PROTAC (Proteolysis Targeting Chimera), which utilizes the unbiquitin-proteasome system to directly degrade the protein of interest (POI). PROTACs recruit the POI to the E3 ligase then trigger the proteasome-mediated degradation. Due to the “event-driven” nature of PROTACs, it is different from traditional drugs which inhibit the functional activity of the target protein through long-term and high affinity binding, thus it became an emerging technique for “undruggable targets” drug discovery. ChemPartner has developed a series of corresponding assays which can detect the degree of ubiquitination on the POI at the biochemical level to evaluate the PROTAC activity.