Discovery and Characterization of Novel Small Molecule Degraders of BRD4 That Act Through the Recruitment of DCAF11

Presentation

Keystone

June 12, 2022

Targeted protein degradation (TPD) through the ubiquitin proteasome system (UPS) is a rapidly growing drug discovery approach to eliminate pathogenic proteins. Strategies for TPD have focused on heterobifunctional degraders in which an E3 ligase and a target protein are brought into proximity. Optimization of drug-like properties has often been challenging. Monovalent degraders represent an alternative approach, in which small molecules are designed to bind to the target protein and induce its degradation through the recruitment of an E3 ligase complex…