X-ray Crystallography

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PROTAC

PROTACs (proteolysis-targeting chimeras) are a class of small molecule that induces targeted protein degradation via the ubiquitin-proteasome system.

PROTACs are hybrid bifunctional small molecule or peptide compound that links a ligand for the target protein and a ligand for the E3 ubiquitin ligase via a linker, these two ligands specifically bind to their respective receptors (the target protein and the E3 ligase). The proximity of these receptors triggers the transfer of ubiquitin molecules from the E2 ligase to the target protein, once sufficiently ubiquitinated, the target protein is recognized by the 26S proteasome, which then enters and degrades the target protein.

Case Presentation

SMARCA2+PROTAC+VCB

Molecular Glue

Molecular glue are a class of small chemical molecules that target the protein-protein interaction interfaces. Together with PROTACs, they are part of the targeted protein degradation (TPD) technology. The main difference between molecular glues and PROTACs lies in their functional design: molecular glues are monofunctional small molecules, while PROTACs are bifunctional molecules. Molecular glues modify the surface of ubiquitin ligases, particularly E3 ligases, to enable the recognition and degradation of novel substrates.

Case Presentation

CRBNmidi+MG+IKZF1

MEK1+MG+BRAF

Service Content

Service Content