A5115907814- Signaling Pathways in Disease
- Protein Degradation and Inhibitors
- Computational Drug Discovery Methods
- Peptidase Inhibition and Analysis
Novartis (Switzerland)
2025
Many disease-relevant and functionally well-validated targets are difficult to drug. Their poorly defined 3D structure without deep hydrophobic pockets makes the development of ligands with low molecular weight high affinity almost impossible. For these targets, incorporation into a ternary complex may be viable alternative modulate in most cases inhibit their function. Therefore, we interested methods identify characterize glues. In protein array screen 50 different macrocyclic FKBP12...
The incorporation of disease-relevant targets in a compound-dependent manner into ternary complexes with an assisting chaperone protein has become common modality. Among the various types complex-forming compounds, molecular glues are particular interest because they do not require significant binary (independent) target affinity. Instead, formed by retrieve part their thermodynamic stability through newly induced chaperone-target or glue-target interactions that occur only complex. These...