| Popis: |
Targeted protein degradation is arguably one of the most exciting novel therapeutic modalities in drug discovery. Moving away from occupancy-based pharmacology models and their challenges with selectivity, on/off target toxicities, and PK–PD limitations, it provides a novel and orthogonal therapeutic paradigm. The ability to induce degradation using a small molecule without the need to inhibit a specific protein function allows access to unexplored new areas of biology and targeting historically intractable protein targets. This chapter reviews the field especially focusing on heterobifunctional molecule-driven target degradation and highlights great progress but also gaps needed to be filled as the field moves toward clinical validation. |
