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Introduction of Protein Degraders

Compared with traditional pharmaceutical drug discovery focused on directly controlling protein activity, Protein Degraders utilizes the proteasome-mediated proteolysis via E3 ligase and engage the body's housekeeping protein degradation system to selectively degrade the pathogenic proteins to treat cancer or other difficult-to-treat diseases. Protein Degraders is a heterobifunctional small molecule that consists of a linker and two warheads - one binds to the target protein, and the other recruits the E3 ligase (see Fig.1). Empowered by this bifunctional characteristic, the disease-causing proteins can be ubiquitinated and degraded by the proteasome which will result in a return to normal physiological tissue. It's emerging as a novel approach with potential to offer therapeutic interventions beyond the limitations of current existing approaches.