PROteolysis TArgeting Chimeras(English)
- artificially hijack the components of the UPS (Ubiquitin Proteasome System) to degrade a target protein, founding the concept of PROTAC Drug Discovery. PROTAC drugs are hetero-bifunctional small molecules that contain two functional ligands connected via a linker; one ligand binds to a target protein and the other ligand binds to an E3 ligase. Bringing these two entities into proximity theoretically leads to polyubiquitylation and proteasomal degradation of the target protein. However, given the complexity this scenario does not always play out, and the PROTAC discovery platform faces several challenges
- E3, UPS
- Pharmacology / pharmaceutics
- https://doi.org…medchem.1c00037
- https://lifesen…drug-discovery/