Designing Next Generation Medicines for the Clinic: Lessons from Targeted Protein Degradation in Cancer & Immune Disease
- Targeted protein degradation is emerging as a transformative therapeutic modality that expands the druggable proteome by leveraging the ubiquitin-proteasome system to selectively eliminate disease-driving proteins, offering the potential for deeper and more durable biological effects than occupancy-driven approaches
- Advances in E3 ligase biology, DNA-encoded library technologies, structural biology, and medicinal chemistry are enabling the rational design of orally bioavailable degraders with optimized ternary complex formation, degradation selectivity, and pharmacologic properties, accelerating translation from discovery to clinical development
- Clinical and preclinical case studies will illustrate how degrader-based medicines can address resistance mechanisms and complex disease biology across oncology and immunology, highlighting the broader potential of induced proximity approaches to generate first-in-class therapies