Figure 1.

Schematic illustration of: a) Occupancy driven pharmacology – a small molecule-based drug, often an inhibitor, modulates protein function employing a non-catalytic MOA. b) Event-driven pharmacology (using PROTAC MOA as an example) – protein function is modulated by induced degradation. The PROTACs initiates a degradation cascade with POI ubiquitination followed by subsequent 26S proteasomal degradation of the POI. c) Schematic illustration of a PROTAC, POI ligand (royal blue) and an E3 ligand (dark blue), linker (black) and examples of PROTACs.