Best Practices for PROTACs - UPS, MoA and Design of PROTACs (Part 1A)

In part 1A we describe an important cellular protein degradation pathway, the ubiquitin-proteasome system (UPS) and its components. Then we discuss the mode of action (MoA) and design of PROTACs to hijack the UPS to degrade a specific protein target (protein of interest = PoI). We compare this approach to traditional small molecule drug discovery and consider the three key components of PROTACs, the binder to POI, the binder to the E3 ligase and the linker.