Proteolysis Targeting Chimeras (PROTACs)

Proteolysis Targeting Chimeras (PROTACs) 

Targeted protein degradation (TPD) is an emerging technology with the potential to tackle disease-causing proteins that were previously considered as “undruggable”. PROTACs are heterobifunctional molecules comprising of a ligand for a target protein and an E3 ligase joined by a linker. In PROTACs, one ligand binds to the protein of interest, and another ligand binds to E3 ubiquitin ligase to induce ubiquitylation of the protein of interest and its subsequent degradation by the ubiquitin-proteasome system (UPS), after which the PROTAC is recycled to target another copy of the protein of interest. Currently, PROTACs have successfully degraded diverse proteins, such as BTK, BRD4, AR, ER, STAT3, IRAK4, tau, etc. 

PROTAC technology

Team Glycomindsynth is dedicated to offer:

  • A library of non-classical PEG linkers to support structure-activity studies of PROTAC molecules.
  • Custom synthesis of various ligands for proteins of interest, including BTK, BRD4, AR, ER, STAT3, IRAK4 etc.
  • Custom synthesis of E3 ubiquitin ligase ligands (e.g. VHL, CRBN) with the desired linker and handle.