Expertise of the month: PROTACS and Molecular Glues

Targeted Protein Degradation (TPD) is a hot topic in drug discovery today. PROteolysis Targeting Chimeras (PROTACs) and molecular glues provide an approach for the targeted degradation of a protein of interest (POI) with a small molecule.

SpiroChem discovery team has identified leads across several projects.

On PROTACs and molecular glues projects, SpiroChem chemists bring support for:

• Developing efficient synthesis of E3 ligase recruiters such as Thalidomide, Lenalidomide, VHL, ….
• Introducing diversified handles on E3 ligase recruiters
• Connecting various warheads

For PROTACs projects, SpiroChem chemists use their expertise for escaping from usual PEG linkers.

PEG Linker

• High risk of hydrophobic collapse
• Low solubility
• Limited IP space

SpiroChem linkers

SpiroChem designs novel linkers containing 3D constrained modules to:

• Minimize hydrophobic collapse and reduce the risk of aggregation of the complex
• Improve PhysChem properties of the complex
• Generate novel IP space

We will be happy to support your projects.

For more information, please contact Laurence Jung at laurence.jung@spirochem.com.