Drug Optimization
Drug Optimization Expertise
Small molecule inhibitors have been used in a wide range of targeted therapies and display several advantages over traditional chemotherapy (selectivity, efficacy and tolerability) or biologics (mode of administration, cell penetration).
Targeted protein degraders – Less than 10% of human proteins are druggable due to their structural limitations or cellular location.
Protein degradation is a novel approach in cancer research, which leverages the body’s natural ubiquitin-proteasome system (UPS) to target and remove unwanted proteins associated with cancers and other diseases.
Approaches
Molecular Glues
Small molecules that stabilize the interaction between a protein and the E3 ubiquitin ligase complex and induce or accelerate the degradation of this protein through the ubiquitin-proteasome system (UPS)
Ligand-Directed Degraders (LDDs)
Bifunctional molecules (2 different ends connected by a linker) that bind to a protein and to the E3 ubiquitin ligase complex and redirect the ubiquitin-proteasome system (UPS) to degrade this protein