Strategic build-up of robust pipeline
  • Proteolysis-targeting chimera (PROTAC) is a new modality as a small molecule agent that induces ubiquitination and subsequent degradation of the target protein that involves a pathogenic process. PROTAC consists of three chemical elements: a ligand binding to a target protein, a ligand binding to E3 ubiquitin ligase, and a linker for conjugating these two ligands.
  • PROTAC induces the target protein and E3 ligase to form a ternary complex by utilizing a bifunctional small molecule, which can simultaneously bind the target protein and E3 ubiquitin ligase. The complex makes the target protein ubiquitinated by E3 ligase and then finally recognized and degraded by the proteasomes in the cellular system.
  • PROTAC has several major advantages:
    1. 1
      Overcome drug-resistant cancers
    2. 2
      Access traditionally “undruggable” protein targets
    3. 3
      Eliminate both enzymatic and nonenzymatic functions of target proteins
    4. 4
      Develop highly selective drugs for target proteins compared to small molecule inhibitors
  • In line with the commitment in oncology area, Therapex is in a research collaboration with Elgen Therapeutics to strengthen the R&D pipeline with PROTAC.
PROTAC Mechanism