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. 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.

As a leading service provider in the field of biological research and drug discovery, Creative Biolabs is fully competent and dedicated to serving one-stop Proteolysis Targeting Chimeric (Protein Degraders) based molecular drug discovery which has become a promising strategy in the area of drug discovery. With the comprehensive advanced platform, Creative Biolabs provides global clients with Protein Degraders molecule discovery package service to meet the novel drug discovery goals. The package includes a variety of different services covering the whole process.

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.

Advantages of Protein Degraders

Protein Degraders has opened up a novel and exciting area of drug discovery because of the following advantages:

• Degrading pathogenic proteins rather than inhibiting them
• Low dosage
• Reduce toxicity
• Target undruggable proteins
• Prolonged pharmacodynamics effect